Peplife 2.0 - Browse by Length

Browsing by half-Life: Above 86400 Seconds

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ID	PMID	YEAR	Sequence	Name	Length	N-ter MOD	C-ter MOD	Linear/Cyclic	Chirality	Chem-MOD	Origin	Nature	Incubation Time	Concentration	Half Life	Units Half Life	half-life(in Sec)	Protease	Assay	Test Sample	Vivo/Vitro	Reference	Patent No.	Activity
1184	10541299	1999	APPRLICDSRVLERYLLEAKEAENITTGCAEHCSLNENITVPDTKVNFYAWKRMEVGQQAVEVWQGLALLSEAVLRGQALLVNSSQPWEPLQLHVDKAVSGLRSLTTLLRALGAQKEAISPPDAASAAPLRTITADTFRKLFRVYSNFLRGKLKLYTGEACRTGDR	Novel erythropoiesis stimulating protein (NESP)	166	Free	Free	Cyclic	L	Five N-linked carbohydrate chains	Hyperglycosylated analogue of recombinant human erythropoietin	Stimulates erythropoiesis	Not mentioned	Not mentioned	25.3 ±2.2	hours	91080	Human blood proteases	ELISA	Subcutaneously injected into patients with end-stage renal failure	in vivo	http://www.drugbank.ca/drugs/DB00017	None	Not reported
1207	21244372	2010	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	PB-106 (ExC39PEG20kDa)	39	Free	Amidation	Linear	L	20 kDa PEG at Cys at 39th position	Analogue of exenatide	Regulate blood glucose	Not mentioned	5 µg ·mL-1 ·kg-1	49.4 ±7.7	hours	177840	Rat plasma proteases	ELISA	Intravenously injected into Sprague-Dawley rats at a dose of 5 µg ·mL-1 ·kg-1	in vivo	None	None	EC50 of 1.2nM for stimulation of intracellular cAMP in PC12 cells
1208	21244372	2010	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	PB-107 (ExC39PEG30kDa)	39	Free	Amidation	Linear	L	30 kDa PEG at Cys at 39th position	Analogue of exenatide	Regulate blood glucose	Not mentioned	5 µg ·mL-1 ·kg-1	70.5 ±2.6	hours	253800	Rat plasma proteases	ELISA	Intravenously injected into Sprague-Dawley rats at a dose of 5 µg ·mL-1 ·kg-1	in vivo	None	None	EC50 of 14.2nM for stimulation of intracellular cAMP in PC12 cells
1209	21244372	2010	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	PB-108 (ExC39PEG40kDa)	39	Free	Amidation	Linear	L	40 kDa PEG at Cys at 39th position	Analogue of exenatide	Regulate blood glucose	Not mentioned	5 µg ·mL-1 ·kg-1	76.4 ±7.4	hours	275040	Rat plasma proteases	ELISA	Intravenously injected into Sprague-Dawley rats at a dose of 5 µg ·mL-1 ·kg-1	in vivo	None	None	EC50 of 114.1nM for stimulation of intracellular cAMP in PC12 cells
1217	21114599	2010	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVK-Aib-R	[Aib8,35]hGLP-1(7-36)NH2	30	Free	Amidation	Linear	L	Aib--Aminoisobutyric acid	Analogue of glucagon like peptide1	Regulate blood glucose	Not mentioned	Not mentioned	66	hours	237600	Human plasma proteases	HPLC	Human plasma	in vitro	14759771	None	EC50=0.06 ±0.04nM for cAMP stimulation
1219	20587645	2010	VRRADRAAVPGGGGRG	PEG20k-HM-3	16	Methoxy-polyethylene glycol-Succinimidyl Carbonate (SC-mPEG, molecular weight 20 kDa, named SC-mPEG20k )	Free	Linear	L	None	HM-3 analogue	Anti-angiogenetic	Not mentioned	Not mentioned	>132	hours	475200	SD rat plasma proteases	RP-HPLC	SD rat plasma	in vitro	http://pubs.rsc.org/En/content/articlepdf/2014/tb/	None	44.35% inhibitory effect on mouse tumors
1227	20593470	2010	G-tBu-FAEGTFTSDVSSYLEGQAAKEFIAWLVKGRPSSGAPPPS	Peptide 7	41	Free	Amidation	Linear	L	tBu=tertiary butyl	Synthetic dipeptide extended GLP-analogs	Regulate blood glucose	168 hours	Not mentioned	>168	hours	604800	None	HPLC	PBS	in vitro	None	None	Not reported
1234	20593470	2010	FFFAEGTFTSDVSSYLEGQAAKEFIAWLVKGRPSSGAPPPS	Peptide 14	41	Free	Amidation	Linear	L	None	Synthetic dipeptide extended GLP-analogs	Regulate blood glucose	168 hours	Not mentioned	33.3	hours	119880	None	HPLC	PBS	in vitro	None	None	Not reported
1236	20593470	2010	FVFAEGTFTSDVSSYLEGQAAKEFIAWLVKGRPSSGAPPPS	Peptide 16	41	Free	Amidation	Linear	L	None	Synthetic dipeptide extended GLP-analogs	Regulate blood glucose	168 hours	Not mentioned	>168	hours	604800	None	HPLC	PBS	in vitro	None	None	Not reported
1237	20593470	2010	FvFAEGTFTSDVSSYLEGQAAKEFIAWLVKGRPSSGAPPPS	Peptide 17	41	Free	Amidation	Linear	L	None	Synthetic dipeptide extended GLP-analogs	Regulate blood glucose	168 hours	Not mentioned	50.6	hours	182160	None	HPLC	PBS	in vitro	None	None	EC50=0.04 ±0.06nM
1238	20593470	2010	FVFAEGTFTSDVSSYLEGQAAKEFIAWLVKGRPSSGAPPPS	Peptide 18	41	Free	Amidation	Linear	L	None	Synthetic dipeptide extended GLP-analogs	Regulate blood glucose	168 hours	Not mentioned	64	hours	230400	None	HPLC	PBS	in vitro	None	None	EC50=2.07 ±0.41nM
1761	16586064	2006	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	N-PEG/GLP-1	30	Free	Amidation	Linear	L	Pegylation at N terminus His7	Synthetically synthesized Glucagon-like peptide-1 analogues	Insulinotropic	Not reported	Not mentioned	7560 ±5635	minutes	453600	Rat plasma proteases	RP-HPLC	Rat plasma	in vitro	16505481	None	290 ([pmol/l] islet-1 h-1) insulin release at -7 (log [mol/l])
1764	16586064	2006	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	Lys-PEG/GLP-1	30	Free	Amidation	Linear	L	Pegylation on Lys34	Synthetically synthesized Glucagon-like peptide-1 analogues	Insulinotropic	Not reported	Not mentioned	4471 ±1822	minutes	268260	Rat plasma proteases	RP-HPLC	Rat plasma	in vitro	16505481	None	150 ([pmol/l] islet-1 h-1) insulin release at -7 (log [mol/l])
1767	16892368	2006	WDREINNYTSLIH	C46	13	Glycosylation	Amidation	Linear	L	None	Derived from T20	HIV-1 fusion inhibitory peptide	Not reported	40 ng peptide/200 mL plasma	4.75	days	410400	Mouse plasma proteases	ELISA	Mouse plasma	in vitro	None	None	IC50=90nM
1768	16892368	2006	WDREINNYTSLIH	C46	13	Glycosylation	Amidation	Linear	L	None	Derived from T20	HIV-1 fusion inhibitory peptide	Not reported	41 ng peptide/200 mL plasma	2	days	172800	Rat plasma proteases	ELISA	Rat plasma	in vitro	None	None	IC50=90nM
1770	16892368	2006	WDREINNYTSLIHWDREINNYTSLIH	Dimeric C46	26	Glycosylation	Amidation	Linear	L	None	Derived from T20	HIV-1 fusion inhibitory peptide	Not reported	40 ng peptide/200 mL plasma	1.75	days	151200	Mouse plasma proteases	ELISA	Mouse plasma	in vitro	None	None	Not given
1772	16892368	2006	WDREINNYTSLIHWDREINNYTSLIH	Dimeric C46	26	Glycosylation	Amidation	Linear	L	None	Derived from T20	HIV-1 fusion inhibitory peptide	Not reported	40 ng peptide/200 mL buffer	4.25	days	367200	Not mentioned	ELISA	PBS/1% BSA	in vitro	None	None	Not given
1841	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQEQQEKLEAVLREL	T-291022	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	28.6	hours	102960	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.022 µg/ml against IIIB virus
1842	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQEQQEKLEAVLREL	T-291022	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	28.6	hours	102960	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.049 µg/ml against 098 virus
1843	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQEQQEKLEAVLREL	T-291022	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	28.6	hours	102960	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.093 µg/ml against 098-T20 virus
1844	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQEQQEKLEAVLREL	T-291022	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	28.6	hours	102960	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.046 µg/ml against 098-T1249 virus
1845	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQEQQEKLEAVLREL	T-291022	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	28.6	hours	102960	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.242 µg/ml against 098-T651 virus
1856	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQELQEKLEAALREL	T-267228	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	30.8	hours	110880	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.172 µg/ml against IIIB virus
1857	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQELQEKLEAALREL	T-267228	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	30.8	hours	110880	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.600 µg/ml against 098 virus
1858	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQELQEKLEAALREL	T-267228	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	30.8	hours	110880	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.416 µg/ml against 098-T20 virus
1859	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQELQEKLEAALREL	T-267228	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	30.8	hours	110880	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.555 µg/ml against 098-T1249 virus
1860	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQELQEKLEAALREL	T-267228	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	30.8	hours	110880	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.987 µg/ml against 098-T651 virus
1861	17640899	2007	TTWEAWDRAIAEYAARIEALIRALQELQEKLEAILREL	T-267229	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	35.4	hours	127440	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=3.162 µg/ml against IIIB virus
1862	17640899	2007	TTWEAWDRAIAEYAARIEALIRALQELQEKLEAILREL	T-267229	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	35.4	hours	127440	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50>20 µg/ml against 098 virus
1863	17640899	2007	TTWEAWDRAIAEYAARIEALIRALQELQEKLEAILREL	T-267229	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	35.4	hours	127440	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50>20 µg/ml against 098-T20 virus
1864	17640899	2007	TTWEAWDRAIAEYAARIEALIRALQELQEKLEAILREL	T-267229	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	35.4	hours	127440	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50>20 µg/ml against 098-T1249 virus
1865	17640899	2007	TTWEAWDRAIAEYAARIEALIRALQELQEKLEAILREL	T-267229	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	35.4	hours	127440	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50>20 µg/ml against 098-T651 virus
1867	17994612	2007	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exendin-4 (Ex-4)	39	Free	Free	Linear	L	None	Salivary gland of the lizard Heloderma suspectum	Glucose-dependent insulin secretion, suppresses inappropriately elevated glucagon secretion, and slows down gastric emptying	Not reported	4.0 mg/kg	56.7	hours	204120	Not mentioned	Radioimmunoassay	Monkey (Intravenous injection)	in vivo	None	None	Not given
1868	17994612	2007	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exendin-4 (Ex-4)	39	Free	Free	Linear	L	None	Salivary gland of the lizard Heloderma suspectum	Glucose-dependent insulin secretion, suppresses inappropriately elevated glucagon secretion, and slows down gastric emptying	Not reported	4.0 mg/kg	77.4	hours	278640	Not mentioned	Radioimmunoassay	Monkey (Subcutaneous injection)	in vivo	None	None	CL/F =2.0 ml/h/kg
1894	18307313	2007	R-BIP-R	CAP 9	2	Free	Y= structure given in paper	Linear	L	BIP	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	35	hours	126000	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 7 µM for S.aureus
1895	18307313	2007	R-Bip-R	CAP 9	2	Free	Y= structure given in paper	Linear	L	BIP	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	35	hours	126000	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 7 µM for Methicillin- resistant S.aureus
1896	18307313	2007	R-Bip-R	CAP 9	2	Free	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	35	hours	126000	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 6 µM for Methicillin- resistant S.epidermis
1903	18307313	2007	R-Bip-R	CAP 12	2	Free	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	30	hours	108000	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 8 µM for S.aureus
1904	18307313	2007	R-Bip-R	CAP 12	2	Free	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	30	hours	108000	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 8 µM for Methicillin- resistant S.aureus
1905	18307313	2007	R-Bip-R	CAP 12	2	Free	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	30	hours	108000	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 5 µM for Methicillin- resistant S.epidermis
1927	18307313	2007	R-X-R	CAP 18	2	Free	CH2CH2Ph	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	30	hours	108000	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 4 µM for S.aureus
1928	18307313	2007	R-X-R	CAP 18	2	Free	CH2CH2Ph	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	30	hours	108000	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC<3 µM for Methicillin- resistant S.aureus
1929	18307313	2007	R-X-R	CAP 18	2	Free	CH2CH2Ph	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	30	hours	108000	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC<3 µM for Methicillin- resistant S.epidermis
1930	18307313	2007	R-Bip-R	CAP 18	2	Acetylation	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	30	hours	108000	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 4 µM for S.aureus
1931	18307313	2007	R-Bip-R	CAP 18	2	Acetylation	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	30	hours	108000	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC<3 µM for Methicillin- resistant S.aureus
1932	18307313	2007	R-Bip-R	CAP 18	2	Acetylation	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	30	hours	108000	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC<3 µM for Methicillin- resistant S.epidermis
1945	18307313	2007	R-X-R	CAP 21	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	116	hours	417600	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC>100 µM for S.aureus
1946	18307313	2007	R-X-R	CAP 21	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	116	hours	417600	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC>100 µM for Methicillin- resistant S.aureus
1947	18307313	2007	R-X-R	CAP 21	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	116	hours	417600	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC>100 µM for Methicillin- resistant S.epidermis
1951	18307313	2007	R-X-R	CAP 23	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	67	hours	241200	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 25 µM for S.aureus
1952	18307313	2007	R-X-R	CAP 23	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	67	hours	241200	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 25 µM for Methicillin- resistant S.aureus
1953	18307313	2007	R-X-R	CAP 23	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	67	hours	241200	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 5 µM for Methicillin- resistant S.epidermis
1957	18307313	2007	R-X-R	CAP 25	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	88	hours	316800	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC>100 µM for S.aureus
1958	18307313	2007	R-X-R	CAP 25	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	88	hours	316800	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC>100 µM for Methicillin- resistant S.aureus
1959	18307313	2007	R-X-R	CAP 25	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	88	hours	316800	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC>100 µM for Methicillin- resistant S.epidermis
1972	19053766	2008	WVTH[Cit]LAGLLS[Cit]SGGVV[hArg]KN[2-Nal]V[Oic]TDVG[Oic]FA[2-Nal]	CGRP(8-37)-NH2 derivative 32	30	Acetylation	Amidation	Linear	L	None	Calcitonin gene-related peptide	Neuropeptide	Not reported	10 µg/ml	38	hours	136800	Monkey plasma proteases	ELISA	Monkey plasma	in vitro	None	None	IC50=3.57 ± 0.04 nM
1973	19053766	2008	WVTH[Cit]LAGLLS[Cit]SGGVV[hArg]KN[2-Nal]V[Oic]TDVG[Oic]FA[2-Nal]	CGRP(8-37)-NH2 derivative 32	30	Acetylation	Amidation	Linear	L	None	Calcitonin gene-related peptide	Neuropeptide	Not reported	10 µg/ml	68	hours	244800	Human plasma proteases	ELISA	Human plasma	in vitro	None	None	IC50=3.57 ± 0.04 nM
1982	19552923	2011	HGEGTFTSDVSSYLEGQAAKEFIAWLVAGR	GLP-1-Tf	30	Human transferrin protein	Amidation	Linear	L	None	Proglucagon molecule	Insulinomimetic and insulinotropic	Not reported	27.9 ± 5.8 Î¼g/ml	27	hours	97200	Rabbit blood proteases	ELISA	Rabbit serum (Intravenous injection)	in vivo	None	None	Not available
2059	21664938	2011	HAECTFTSDVSSYLEGQAAKEFIAWLCKGRGCPSSGAPPPSGGGGG	GLP715a	46	Free	Free	Linear	L	None	Proglucagon molecule	Anti-hyperglycemic hormone	Not reported	300 Î¼g/kg	48	hours	172800	Rat blood proteases	ELISA	Serum of rats (Subcutaneous injection)	in vivo	None	None	Binding constants to the GLP-1 receptor= 6.18 ± 1.27nM
2065	23318685	2013	GGLYACHMGPIT-Nal-VYQPLRS-Peg-SRLPQYV-Nal-TIPGMHCAYLGG	Peginesatide	40	Acetylation	Dimerization using PEGylation	Cyclic (C6-C15, C26-C35)	L	Nal, Pegylation	Synthetic peptide	Erythropoiesis-stimulating agent	Not reported	0.5 mg/kg	34.0 ± 5.9	hours	122400	Monkey blood proteases	ELISA	Monkey blood plasma	in vitro	None	None	Increase in RBCs of 1.67 106/ µl 21 days after the administration
2066	23318685	2013	GGLYACHMGPIT-Nal-VYQPLRS-Peg-SRLPQYV-Nal-TIPGMHCAYLGG	Peginesatide	40	Acetylation	Dimerization using PEGylation	Cyclic (C6-C15, C26-C35)	L	Nal, Pegylation	Synthetic peptide	Erythropoiesis-stimulating agent	Not reported	5 mg/kg	99.0 ± 37.1	hours	356400	Monkey blood proteases	ELISA	Monkey blood plasma	in vitro	None	None	Increase in RBCs of 1.67 106/ µl 21 days after the administration
2067	23318685	2013	GGLYACHMGPIT-Nal-VYQPLRS-Peg-SRLPQYV-Nal-TIPGMHCAYLGG	Peginesatide	40	Acetylation	Dimerization using PEGylation	Cyclic (C6-C15, C26-C35)	L	Nal, Pegylation	Synthetic peptide	Erythropoiesis-stimulating agent	Not reported	5[C14] mg/kg	84.0 ± 9.56	hours	302400	Monkey blood proteases	ELISA	Monkey blood plasma	in vitro	None	None	Increase in RBCs of 1.73 106/ µl 21 days after the administration
2104	EP2090589A1	2009	EACNLPIVRGPCIAFFPRWAFDAVKGKCVLFPYGGCQGNGNKFYSEKECREYCGVP	Human Serum Albumin-DX-890	56	Human serum albumin	Free	Linear	L	None	Kunitz domain peptide	Protease inhibitor	N.A.	Not mentioned	3500	minutes	210000	Rabbit blood proteases	I-125 radiolabelling method	Rabbit plasma (Intravenous)	in vivo	None	EP2090589A1	Inhibition constt (Ki) 7 ±1 pM
2178	15817669	2007	YaDAIFTQSYRKVLAQLSARKLLQDILSRL	Derivative of Growth hormone releasing factor	30	Free	Addition of maleimidopropionic acid (MPA) and amidation	Linear	Mix	None	GRF peptide	Growth harmone and somatostatin releasing factor	N.A.	1microM/ Kg	25.8	hours	92880	Not mentioned	Radioimmunoassay	Rat plasma (Subcutaneous)	in vivo	None	US7268113B2	Area under curve (AUC) for growth hormone (GH) release >10000 (ng/ml)*minute
2185	20503261	2001	HVEGTFTSDVSSYLEGQAAKEFIAWLVKGRG	Val8-GLP-1-Fc	31	Free	Addition of Fc	Linear	L	None	Glucagon like peptide1	Insulinotropic peptide	N.A.	5.6 nM/ Kg	45	hours	162000	Monkey blood proteases	Radioimmunoassay	Monkey plasma (Intravenous)	in vivo	None	EP1355942B1	Activation of GLP1 receptor (with respect to Val8-GLP-1(7-37)OH) 1.00%
2186	20503261	2001	HVEGTFTSDVSSYLEGQAAKEFIAWLVKGRG	Val8-GLP-1-Human serum albumin (HSA)	31	Free	Human serum albumin	Linear	L	None	Glucagon like peptide1	Insulinotropic peptide	N.A.	5.6 nM/ Kg	87	hours	313200	Monkey blood proteases	Radioimmunoassay	Monkey plasma (Intravenous)	in vivo	None	EP1355942B1	Not mentioned
2187	20503261	2001	HGEGTFTSDVSSYLEEQAAKEFIAWLVKGRG	Gly8-Glu22-GLP-1-CEx-Linker-IgG1	31	Free	Linking IgG1 using CEx-Linker (SSGAPPPS-GGGGSGGGGSGGGGS)	Linear	L	None	Glucagon like peptide1	Insulinotropic peptide	N.A.	0.1 mg/ Kg	55	hours	198000	Dog blood proteases	Radioimmunoassay	Dog plasma (Intravenous)	in vivo	None	EP1355942B1	Activation of GLP1 receptor (with respect to Val8-GLP-1(7-37)OH) 150.00%
2188	20503261	2001	HGEGTFTSDVSSYLEEQAAKEFIAWLVKGRG	Gly8-Glu22-GLP-1-CEx-Linker-IgG1	31	Free	Linking IgG1 using CEx-Linker (SSGAPPPS-GGGGSGGGGSGGGGS)	Linear	L	None	Glucagon like peptide1	Insulinotropic peptide	N.A.	0.1 mg/ Kg	38	hours	136800	Not mentioned	Radioimmunoassay	Dog plasma (Subcutaneous)	in vivo	None	EP1355942B1	Not mentioned
2189	20503261	2010	HVEGTFTSDVSSYLEEQAAKEFIAWLIKGGPSSGAPPPCC	GLP-1-PEG	40	Free	Addition of NH2-PEG at Cys40	Linear	L	None	Glucagon like peptide1	Insulinotropic peptide	N.A.	0.1 mg/ Kg	25.8	hours	92880	Rat blood proteases	Radioimmunoassay	Rat plasma (Intravenous)	in vivo	None	EP1881850B1	EC50= 0.36 nM
2190	20503261	2010	HVEGTFTSDVSSYLEEQAAKEFIAWLIKGGPSSGAPPPCC	GLP-1-PEG	40	Free	Addition of NH2-PEG at Cys40	Linear	L	None	Glucagon like peptide1	Insulinotropic peptide	N.A.	0.1 mg/ Kg	28.3	hours	101880	Not mentioned	Radioimmunoassay	Rat plasma (Subcutaneous)	in vivo	None	EP1881850B1	Not mentioned
2191	20503261	2010	HVEGTFTSDVSSYLEEQAAKEFIAWLIKGGPSSGAPPPCC	GLP-1-PEG	40	Free	Addition of NH2-PEG at Cys40	Linear	L	None	Glucagon like peptide1	Insulinotropic peptide	N.A.	0.01 mg/ Kg	75.69	hours	272484	Not mentioned	Radioimmunoassay	Monkey plasma (Subcutaneous)	in vivo	None	EP1881850B1	Not mentioned
2192	EP1605897B1	2012	HVEGTFTSDVSSYLEEQAAKEFIAWLIKGGPSSGAPPPC	V8E22I33C45-40kDa PEG	39	Free	Pegylation	Linear	L	None	Glucagon like peptide1	Insulinotropic peptide	N.A.	0.1 mg/ kg	1.5	day	129600	Rat blood proteases	Radioimmunoassay	Rat plasma (Intravenous)	in vivo	None	EP1605897B1	EC50= 9.4% with respect to Val8-GLP-1-OH
2193	EP1605897B1	2012	HVEGTFTSDVSSYLEEQAAKEFIAWLIKGGPSSGAPPPC	V8E22I33C45-40kDa PEG	39	Free	Pegylation	Linear	L	None	Glucagon like peptide1	Insulinotropic peptide	N.A.	0.1 mg/ Kg	1.3	day	112320	Not mentioned	Radioimmunoassay	Rat plasma (Subcutaneous)	in vivo	None	EP1605897B1	EC50= 9.4% with respect to Val8-GLP-1-OH
2195	EP1605897B1	2012	HVEGTFTSDVSSYLEEQAAKEFIAWLIKGGPSSGAPPPC	V8E22I33C45-40kDa PEG	39	Free	Pegylation	Linear	L	None	Glucagon like peptide1	Insulinotropic peptide	N.A.	0.1 mg/ Kg	59.5	hours	214200	Monkey blood proteases	Radioimmunoassay	Monkey plasma (Intravenous)	in vivo	None	EP1605897B1	EC50= 9.4% with respect to Val8-GLP-1-OH
2196	EP1605897B1	2012	HVEGTFTSDVSSYLEEQAAKEFIAWLIKGGPSSGAPPPC	V8E22I33C45-40kDa PEG	39	Free	Pegylation	Linear	L	None	Glucagon like peptide1	Insulinotropic peptide	N.A.	0.1 mg/ Kg	61.6	hours	221760	Not mentioned	Radioimmunoassay	Monkey plasma (Subcutaneous)	in vivo	None	EP1605897B1	EC50= 9.4% with respect to Val8-GLP-1-OH
2198	EP2114438B1	2012	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exendin-4(N)-PEG-Fc	39	Pegylation	Addition of Fc	Linear	L	None	Venom of Heloderma horridum	Insulinotropic peptide	N.A.	Not mentioned	62	hours	223200	Not mentioned	Not mentioned	blood	Not mentioned	None	EP2114438B1	EC50= <0.2 % with respect to Exendin-4
2199	EP2114438B1	2012	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exendin-4(Lys27)-PEG-Fc	39	Free	Addition of Fc	Linear	L	Pegylation at K27	Venom of Heloderma horridum	Insulinotropic peptide	N.A.	Not mentioned	61	hours	219600	Not mentioned	Not mentioned	blood	Not mentioned	None	EP2114438B1	EC50= 13.2 % with respect to Exendin-4
2200	EP2114438B1	2012	GEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	DM exendin-4(Lys27)-PEG-Fc	38	Modification of His1 of Exendin-4 into dimethylhistidyl (DM) group	Addition of Fc	Linear	L	Pegylation at K27	Venom of Heloderma horridum	Insulinotropic peptide	N.A.	Not mentioned	69	hours	248400	Not mentioned	Not mentioned	blood	Not mentioned	None	EP2114438B1	EC50= 2.6 % with respect to Exendin-4
2201	EP2114438B1	2012	GEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	DA exendin-4(Lys27)-PEG-Fc	38	Modification of His1 of Exendin-4 into desaminohistidyl (DA) group	Addition of Fc	Linear	L	Pegylation at K27	Venom of Heloderma horridum	Insulinotropic peptide	N.A.	Not mentioned	54	hours	194400	Not mentioned	Not mentioned	blood	Not mentioned	None	EP2114438B1	EC50= 13.2 % with respect to Exendin-4
2202	EP2114438B1	2012	GEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	HY exendin-4(Lys27)-PEG-Fc	38	Modification of His1 of Exendin-4 into betahydroxylamidazolpropionyl (HY)	Addition of Fc	Linear	L	Pegylation at K27	Venom of Heloderma horridum	Insulinotropic peptide	N.A.	Not mentioned	52	hours	187200	Not mentioned	Not mentioned	blood	Not mentioned	None	EP2114438B1	EC50= 7.6 % with respect to Exendin-4
2203	EP2114438B1	2012	GEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	CA exendin-4(Lys27)-PEG-Fc	38	Modification of His1 of Exendin-4 into imidazoacetyl (CA) group	Addition of Fc	Linear	L	Pegylation at K27	Venom of Heloderma horridum	Insulinotropic peptide	N.A.	Not mentioned	52	hours	187200	Not mentioned	Not mentioned	blood	Not mentioned	None	EP2114438B1	EC50= 8.5 % with respect to Exendin-4
2204	EP2114438B1	2012	VEGTFTSDVSSYLEEQAAKEFIAWLIKGGPSSGAPPPCC	DA GLP-1 (Lys20,28)-PEG-Fc	39	Modification of His1 of Exendin-4 into desaminohistidyl (DA) group	Addition of Fc	Linear	L	Pegylation at K20 and K28	Glucagon like peptide1	Insulinotropic peptide	N.A.	Not mentioned	27	hours	97200	Not mentioned	Not mentioned	blood	Not mentioned	None	EP2114438B1	EC50= 2 % with respect to Exendin-4
2216	15369394	2004	CDLPQTHSLGSRRTLMLLAQMRKISLFSCLKDRHDFGFPQEEFGNQFQKAETIPVLHEMIQQIFNLFSTKDSSAAWDETLLDKFYTELYQQLNDLEACVIQGVGVTETPLMKEDSILAVRKYFQRITLYLKEKKYSPCAWEVVRAEIMRSFSLSTNLQESLRSKE	PEG40-FMS-IFNÎ±2	146	Pegylation [40kdaPEG linked to INFÎ±2 via 2-sulfo-9-fluorenylmethoxycarbonyl (FMS)]	Free	Cyclic(C1-C98, C29-138)	L	None	IFNÎ±2 derivative	Antiviral and antiproliferative	0-150 hours	10 µg	65 (t1/2 of rate of regeneration of native interferon)	hours	234000	Rat blood proteases	BIAcore binding assay	Intravenously administered to wistar rats	in vivo	http://www.drugbank.ca/drugs/DB00105	None	Following subcutaneous administration to rats and monitoring circulating antiviral activity, active IFNÎ±2 levels peaked at 50 h, with substantial levels still being detected 200 h after administration.
2323	7418787	1979	CYFQNCPRG	Lysine vasopressin	9	Free	Free	Cyclic (C1-C6)	L	None	Human Pituitary	Regulator of fluid and water balance	Not given	0.2 mg	47.4 (t1/2 of specific radioactivity)	month	1.25E+08	None	Liquid scintillation spectrometer	Weakly acidic solution (pH 4.0, acetic acid)	in vitro	None	None	Not reported
2423	11778971	2001	AGCKNFFWKTFTSC	Glycosylated sms-14	14	Dextran 70kDa conjugation	Free	Cyclic (C3-C14)	L	Glycosylation	Somatostatin derivative	Growth Hormone	24 hours	100 Î¼l	27	hours	97200	Mice blood protease	HPLC	Subcutaneously injected in mice	in vivo	None	None	It inhibits tumor growth at IC50 ~2.5 nM
2566	16828890	2006	pGlu-NSPR	NC-1900 (Analogue of arginine vasopressin)	5	Free	Addition of lycinamide	Linear	L	conjugated with cationic bovine serum albumin conjugated pegylated nanoparticles (CBSA-NPs), pGlu=pyroglutamic acid	Synthetic analogue of arginine vasopressin	Neuropeptide	0.5, 1, 2, 3, 4, 6, 9, 12, 24, 36 and 48 h	0.55mM	78	hours	280800	Mice blood proteases	HPLC-UV	Subcutaneously and Intravenously injected in mice	in vitro	None	None	The memory impairments were greatly improved, and then to normal when the mice were treated with NC-1900 loaded in CBSA-NPs
2599	16982323	2006	(GGLYACHMGPITX1AVCQPLRX2)2Beta-ala-PEG	Hematide	42	Acetylation	Beta-alanine-PEG	Linear	L	X1-Napthyl-alanine, X2-Sarcosine	Synthetic dimeric peptide	Erythropoiesis stimulating agent	Not mentioned	6.9 mg/kg	27.5 ±3.7	hours	99000	Rat plasma proteases	Competitive ELISA	Rat plasma (Dose i/v adminstered)	in vivo	None	None	IC50 = 37pM for HuEPOr/125I-EPO competition binding assay, EC50 =460 pM for cell proliferation stimulation
2600	16982323	2006	(GGLYACHMGPITX1AVCQPLRX2)2Beta-ala-PEG	Hematide	42	Acetylation	Beta-alanine-PEG	Linear	L	X1-Napthyl-alanine, X2-Sarcosine	Synthetic dimeric peptide	Erythropoiesis stimulating agent	Not mentioned	13.8 mg/kg	30.7 ±2.6	hours	110520	Rat plasma proteases	Competitive ELISA	Rat plasma (Dose i/v adminstered)	in vivo	None	None	IC50 = 37pM for HuEPOr/125I-EPO competition binding assay, EC50 =460 pM for cell proliferation stimulation
2601	16982323	2006	(GGLYACHMGPITX1AVCQPLRX2)2Beta-ala-PEG	Hematide	42	Acetylation	Beta-alanine-PEG	Linear	L	X1-Napthyl-alanine, X2-Sarcosine	Synthetic dimeric peptide	Erythropoiesis stimulating agent	Not mentioned	9.87 mg/kg	47.8	hours	172080	Rat plasma proteases(rat chronic renal insufficiency (CRI) model)	Competitive ELISA	Rat(rat chronic renal insufficiency (CRI) model) plasma (Dose i/v adminstered)	in vivo	None	None	IC50 = 37pM for HuEPOr/125I-EPO competition binding assay, EC50 =460 pM for cell proliferation stimulation
2604	16982323	2006	(GGLYACHMGPITX1AVCQPLRX2)2Beta-ala-PEG	Hematide	42	Acetylation	Beta-alanine-PEG	Linear	L	X1-Napthyl-alanine, X2-Sarcosine	Synthetic dimeric peptide	Erythropoiesis stimulating agent	Not mentioned	0.475 mg/kg	29.9 ±9.4	hours	107640	Monkey plasma proteases	Competitive ELISA	Monkey plasma (Dose i/v adminstered)	in vivo	None	None	IC50 = 37pM for HuEPOr/125I-EPO competition binding assay, EC50 =460 pM for cell proliferation stimulation
2605	16982323	2006	(GGLYACHMGPITX1AVCQPLRX2)2Beta-ala-PEG	Hematide	42	Acetylation	Beta-alanine-PEG	Linear	L	X1-Napthyl-alanine, X2-Sarcosine	Synthetic dimeric peptide	Erythropoiesis stimulating agent	Not mentioned	1.35 mg/kg	59.7 ±2.9	hours	214920	Monkey plasma proteases	Competitive ELISA	Monkey plasma (Dose i/v adminstered)	in vivo	None	None	IC50 = 37pM for HuEPOr/125I-EPO competition binding assay, EC50 =460 pM for cell proliferation stimulation
2669	22186872	2011	CYFQNCPRG	Vasopressin	9	Free	Amidation	Cyclic (C1-C6)	L	None	Anti-diuretic hormone secreted by pitutiary gland	Anti-diuretic and regulates retention of water	Room Temperature	1mg/mL	>7	days	604800	Hydolytic activity of bacterial strain B-9	HPLC and LC/ITMS	Bacterial strain B-9 cell culture	in vitro	None	None	Not reported
2692	25039358	2014	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	Coumarin-modified GLP-1 derivative 7	30	Free	Amidation	Linear	L	X-2 = Cys- conjugated-7-hydroxyCoumarin maleimide	Analog of human GLP-1	Hypoglycaemic	37 °C for 2-72 hours	1000ng/ml	52.2	hours	187920	Rat plasma proteases	LC-MS/MS	Rat Plasma	in vitro	None	None	GLP-1 receptor Activation potency with EC50 = 18.6 ± 1.3 pM in HEK-293 cells
2703	25243635	2014	HAEGTFTSDVSCYLEGQAACEFIAWLVKGRGKKK	VGLP1K3 (Glucagon like peptide 1 derivative)	34	Free	Free	Cyclic (C18-C26)	L	None	Glucagon Like protein-1 (GLP-1)	Antihyperglycemic	37 °C for 0.1-24 hours	500Î¼g	<80	hours	288000	DPP IV	ELISA	DPP IV	in vitro	None	None	Not reported
2704	25243635	2014	HAEGTFTSDVSCYLEGQAACEFIAWLVKGRGKKKKKK	VGLP1K6 (Glucagon like peptide 1 derivative)	37	Free	Free	Cyclic (C12-C20)	L	None	Glucagon Like protein-1 (GLP-1)	Antihyperglycemic	37 °C for 0.1-24 hours	500Î¼g	~ 70	hours	252000	DPP IV	ELISA	DPP IV	in vitro	None	None	The insulin levels were increased dramatically to 906.53b ± 22.18pmol/L within 60 min after GLP-1 administration
2708	25243635	2014	HAEGTFTSDVSCYLEGQAACEFIAWLVKGRGKKKKKK	VGLP1K6 (Glucagon like peptide 1 derivative)	37	Free	Free	Cyclic (C12-C20)	L	None	Glucagon Like protein-1 (GLP-1)	Antihyperglycemic	5-90 hours	300Î¼g/Kg body weight of rats	~ 70	hours	252000	Rat serum proteases	ELISA	Subcutaneously injected in Sprague ˆ’Dawley (SD) rats	in vivo	None	None	The insulin levels were increased dramatically to 906.53b ± 22.18pmol/L within 60 min after GLP-1 administration
2726	25900863	2015	TTWEAWDRAIAEYAARIEALLRALQEQQEKNEAALREL	PEG-TRI-1144	38	Acetylation	Amidation	Linear	L	Conjugated with PEG(40KDa) thro µgh Lys-30	Synthetic derived from SPPS with an acetylated N-terminus and amidated C-terminus.	HIV-fusion inhibitor	Blood sample collected after 1-168 hours after the infusion of peptide	800nmol/Kg dose injected	34	hours	122400	Rat plasma proteases	LC-MS/MS	Intravenously administered to Sprague €“Dawley rats	in vivo	None	None	Not reported
2727	25900863	2015	TTWEAWDRAIAEYAARIEALLRALQEQQEKNEAALREL	PEG-TRI-1144	38	Acetylation	Amidation	Linear	L	Conjugated with PEG(40KDa) thro µgh Lys-30	Synthetic derived from SPPS with an acetylated N-terminus and amidated C-terminus.	HIV-fusion inhibitor	Not mentioned	Not mentioned	70	hours	252000	Human plasma proteases	LC-MS/MS	Human Plasma	in vivo	None	None	Not reported
2728	25900863	2015	TTWEAWDRAIAEYAARIEALLRALQEQQEKNEAALREL	PEG40kDa[ClPhSO2]TRI-1144	38	Acetylation	Amidation	Linear	L	Conjugated with ClPhSO2 conjugate thro µgh Lys-30	Synthetic derived from SPPS with an acetylated N-terminus and amidated C-terminus.	HIV-fusion inhibitor	Not mentioned	Not mentioned	150 (t1/2Î²)	hours	540000	Human plasma proteases	LC-MS/MS	Human Plasma	in vivo	None	None	Not reported
2729	25900863	2015	TTWEAWDRAIAEYAARIEALLRALQEQQEKNEAALREL	PEG40kDa[ClPhSO2]TRI-1144	38	Acetylation	Amidation	Linear	L	Conjugated with ClPhSO2 conjugate thro µgh Lys-30	Synthetic derived from SPPS with an acetylated N-terminus and amidated C-terminus.	HIV-fusion inhibitor	Blood sample collected after 1-168 hours after the infusion of peptide	800nmol/Kg dose injected	150 (t1/2 linker cleavage)	hours	540000	Rat plasma proteases	LC-MS/MS	Intravenously administered to Sprague €“Dawley rats	in vivo	None	None	Not reported
2730	25900863	2015	TTWEAWDRAIAEYAARIEALLRALQEQQEKNEAALREL	PEG40kDa[MorphSO2]TRI-1144	38	Acetylation	Amidation	Linear	L	Conjugated with MorphSO2 conjugate thro µgh Lys-30	Synthetic derived from SPPS with an acetylated N-terminus and amidated C-terminus.	HIV-fusion inhibitor	Blood sample collected after 1-168 hours after the infusion of peptide	800nmol/Kg dose injected	44 (t1/2Î² of releasable PEG-TRI-1144 conjugate)	hours	158400	Rat plasma proteases	LC-MS/MS	Intravenously administered to Sprague €“Dawley rats	in vivo	None	None	Not reported
2740	26222180	2015	HA/EGTFTSDVSSYLEGQAAKEFIAWLVKGR	G36A or [GLP-1(7-36A)]	30	Free	Amidation	Linear	L	None	Glucagon-like peptide 1 (GLP-1)	Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner)	Room Temp and on Ice	0.4 µM	>96	hours	345600	Human plasma proteases + DPP IV	MS, ELISA	P700 plasma	in vitro	None	None	Not reported
2741	26222180	2015	HA/EGTFTSDVSSYLEGQAAKEFIAWLVKGR	G36A or [GLP-1(7-36A)]	30	Free	Amidation	Linear	L	None	Glucagon-like peptide 1 (GLP-1)	Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner)	Room Temp and on Ice	0.4 µM	>96	hours	345600	Human plasma proteases + DPP IV	MS, ELISA	P800 plasma	in vitro	None	None	Not reported
2747	26222180	2015	HA/EGTFTSDVSSYLEGQAAKEFIAWLVKGR	G36A or [GLP-1(7-36A)]	30	Free	Amidation	Linear	L	None	Glucagon-like peptide 1 (GLP-1)	Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner)	On ice	0.4 µM	37-96	hours	239400	Human blood proteases + DPP IV	MS	P800 whole blood	in vitro	None	None	Not reported
2749	26222180	2015	HA/EGTFTSDVSSYLEGQAAKEFIAWLVKGRG	G 37 or [GLP-1(7 €“37)]	31	Free	Free	Linear	L	None	Glucagon-like peptide 1 (GLP-1)	Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner)	Room Temp	0.4 µM	>96	hours	345600	Human plasma proteases + DPP IV	MS, ELISA	P700 plasma	in vitro	None	None	Not reported
2750	26222180	2015	HA/EGTFTSDVSSYLEGQAAKEFIAWLVKGRG	G 37 or [GLP-1(7 €“37)]	31	Free	Free	Linear	L	None	Glucagon-like peptide 1 (GLP-1)	Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner)	Room Temp	0.4 µM	>96	hours	345600	Human plasma proteases + DPP IV	MS, ELISA	P800 plasma	in vitro	None	None	Not reported
2754	26222180	2015	HA/EGTFTSDVSSYLEGQAAKEFIAWLVKGRG	G 37 or [GLP-1(7 €“37)]	31	Free	Free	Linear	L	None	Glucagon-like peptide 1 (GLP-1)	Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner)	On ice	0.4 µM	41 ±5.0	hours	147600	Human blood proteases + DPP IV	MS	P800 whole blood	in vitro	None	None	Not reported
2757	26222180	2015	YA/EGTFISDYSIAMDKIHQQDFVNWLLAQKGKKNDWKHNITQ	GIP (1-42) (Glucosedependent insulinotropic polypeptide)	42	Free	Free	Linear	L	None	Proprotein of gastrointestinal tract	Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner)	Room Temp	0.4 µM	>96	hours	345600	Human plasma proteases + DPP IV	MS	P800 plasma	in vitro	None	None	Not reported
2759	26222180	2015	HS/QGTFTSDYSKYLDSRRAQDFVQWLMNTKRNRNNIA	OXM(1-37) (Oxyntomodulin)	37	Free	Free	Linear	L	None	Peptide Hormone of colon	Anti-apetizer	Room Temp	0.4 µM	>72	hours	259200	Human plasma proteases + DPP IV	MS	P800 plasma	in vitro	None	None	Not reported
2761	26222180	2015	HS/QGTFTSDYSKYLDSRRAQDFVQWLMNT	Glucagon	29	Free	Free	Linear	L	None	Peptide hormone of pancrease	Regulates hypoglycemia	Room Temp	0.4 µM	45	hours	162000	Human plasma proteases + DPP IV	MS	P800 plasma	in vitro	None	None	Not reported
2766	26308095	2015	HDEFERH-alpha-aminoisobutyric acid-EGTFTSDVSSYLEGQAAKEFIAWLVRGR	semaglutide	36	Free	Amidation	Linear	L	Alpha-aminoisobutyric acid at 8th position, Acylation of peptide at K-26 with C-18 fatty di-acid chain	Glucagon-like peptide 1 (GLP-1) analogue	Regulates blood glucose by upregulating the insulin secretion	Blood sample collected after7-288 hours after the injection of peptide	1 -2 nmol/Kg	165	hours	594000	Human plasma proteases	ELISA, LC/MS	Human plasma (Dose s/c injected)	in vivo	25475122	None	Semaglutide was the most potent with an ED50 of < 2 nmol/kg
2767	26308095	2015	HDEFERH-alpha-aminoisobutyric acid-EGTFTSDVSSYLEGQAAKEFIAWLVRGR	semaglutide	36	Free	Amidation	Linear	L	Acylation of peptide at K-26 with C-18 fatty di-acid chain	Glucagon-like peptide 1 (GLP-1) analogue	Regulates blood glucose by upregulating the insulin secretion	Blood sample collected after 1-96 hours after the injection of peptide	5nmol/Kg	46	hours	165600	Mini-pig plasma proteases	ELISA, LC/MS	Mini-pigs plasma (Dose s/c injected)	in vivo	25475122	None	Semaglutide was the most potent with an ED50 of < 2 nmol/kg
2805	25453979	2014	SCSlPQT	MA(D-Leu-4)OB3	7	Myristoylation	Free	Linear	Mix	None	Synthetic peptide amide with leptin-like activity	Regulate energy balance by inhibiting hunger	Not mentioned	Peptide was dissolved in 0.3% Intravail ® reconstituted in sterile deion-ized water at a concentratio	28.9	hours	104040	Mice serum proteases	Competitive ELISA	Male Swiss Webster mice serum (Oral route of delivery)	in vivo	None	None	Efficacy of MA-[D-Leu-4]-OB3 on blood glucose levels in db/dbmice following oral delivery in 0.3% DDM
2815	16266798	2005	k(Nic)-P-Pal-Pf(Cl2)-NwFwL-Nle	Spantide II (Neurokinin-1 receptor (NK-1R) antagonist)	11	Nicotinoylation	Amidation	Linear	Mix	Pal=3-(2-Pyridyl)-L-alanine , k(Nic)=Nicotinoyl)Lys , Nle=NorLeucine, Dichloro at 5th Phenyl	Neurokinin-1 receptor (NK-1R) antagonist	Anti-inflammatory	Not mentioned	5mg/ml	95 days at pH 3 at 60 C	days	8208000	None	HPLC, LC-MS	Ethanol -water mixture	in vitro	None	None	Not reported
2859	1904406	1991	YADAIFTNSYRKVLGQLSARKLLQDILSRQQG	[Leu27] hGRF( 1-32)NH2 (Growth hormone releasing factor analog)	32	Free	Amidation	Linear	L	None	Human growth hormone releasing factor analog	Growth hormone(GH) release	37 °C, phosphate buffer pH 7.4	0.2mM	202	hours	727200	Collagenase pancreatin	HPLC	Cultured bovine anterior pituitary cells	in vitro	None	None	EC50=0.24 ± 0.045(GH release)
2860	1904406	1991	YADAIFTNSYRKVLGQLSARKLLQDILSRQQG	[Leu27, Asn28]hGRF(I-32)NH2 (Growth hormone releasing factor analog)	32	Free	Amidation	Linear	L	None	Human growth hormone releasing factor analog	Growth hormone(GH) release	37 °C, phosphate buffer pH 7.4	0.2mM	150	hours	540000	Collagenase pancreatin	HPLC	Cultured bovine anterior pituitary cells	in vitro	None	None	EC50=0.32 ± 0.059(GH release)
2861	1904406	1991	YADAIFTNSYRKVLGQLSARKLLQDILSRQQG	[Ser8, Leu27, Asn28]hGRF(I-32)NH2 (Growth hormone releasing factor analog)	32	Free	Amidation	Linear	L	None	Human growth hormone releasing factor analog	Growth hormone(GH) release	37 °C, phosphate buffer pH 7.4	0.2mM	746	hours	2685600	Collagenase pancreatin	HPLC	Cultured bovine anterior pituitary cells	in vitro	None	None	EC50=0.26 ± 0.040(GH release)
2862	1904406	1991	YADAIFTNSYRKVLGQLSARKLLQDILSRQQG	[Ser8, Leu27]hGRF(I-32)NH2 (Growth hormone releasing factor analog)	32	Free	Amidation	Linear	L	None	Human growth hormone releasing factor analog	Growth hormone(GH) release	37 °C, phosphate buffer pH 7.4	0.2mM	1550	hours	5580000	Collagenase pancreatin	HPLC	Cultured bovine anterior pituitary cells	in vitro	None	None	EC50=0.44 ± 0.014(GH release)
2937	2298867	1990	D-Nal-FASKkLKPA	Antide(Nal-Lys)	10	Acetylation	Amidation	Linear	Mix	None	Nal-Lys GnRH antagonist	Regulates or inhibits LH release or gonadotropins	Blood collected upto 30 days after peptide injection	3.5mg/kg injected i/v	6.5	days	561600	Proteases from OVX monkey serum	Radioactive assay	(Dose i/v injected)OVX monkey Serum	in vivo	None	None	Gonadotropin inhibition;Following sc or iv Antide injection, peripheral Luteinizing hormone (LH) levels declined from 281 + 19 ng/ml to 29 + 3 ng/ml within one day
2967	2556215	1989	DRVYIHPFHL	Angiotensin I (AI)	10	Free	Free	Linear	L	None	Derived from angiotensin	Precusor of angiotensin- II (AII)	37 °C	100 - 2000 ng/ml	44.6	hours	160560	Fetal calf serum proteases	Radioimmunoassay	Primary endothelial cells + Fetal calf Serum (2.5%) + converting enzyme inhibitor (MK422) with conc 10-6 M	in vitro	None	None	Not mentioned
3023	26308095	2015	H-Aib-EGTFTSDVSSYLEGQAAKEEFIIAWLVKGRG	Semaglutide	31	Free	Free	Linear	L	Aib =2-Aminoisobutyric acid; Acylation of peptide at K-26 with fatty acid side chain i.e. N6-[N-(17-carboxy-1-oxoheptadecyl-L-c-glutamyl[2- (2-aminoethoxy)ethoxy]acetyl[2-(2 aminoethoxy)ethoxy]acetyl	GLP-1 (Glucagon like peptide-1) analogue	Regulate blood glucose level	Blood samples collected upto 96 hous	1 -2 nmol/Kg	165	hours	594000	Proteases from Human plasma	ELISA, LC/MS	(Dose s/c injected)Human plasma	in vivo	23743288	None	Semaglutide was the most potent to lower blood glucose with an ED50 of < 2 nmol/kg
3024	26308095	2015	H-Aib-EGTFTSDVSSYLEGQAAKEEFIIAWLVKGRG	Semaglutide	31	Free	Free	Linear	L	Aib =2-Aminoisobutyric acid; Acylation of peptide at K-26 with fatty acid side chain i.e. N6-[N-(17-carboxy-1-oxoheptadecyl-L-c-glutamyl[2- (2-aminoethoxy)ethoxy]acetyl[2-(2 aminoethoxy)ethoxy]acetyl	GLP-1 (Glucagon like peptide-1) analogue	Regulate blood glucose level	Blood samples collected upto 96 hous	5nmol/Kg	46	hours	165600	Proteases from mini-pig plasma	ELISA, LC/MS	(Dose i/v injected)Mini-pigs plasma	in vivo	23743288	None	Semaglutide was the most potent to lower blood glucose with an ED50 of < 2 nmol/kg
3029	1911217	1991	SCNTATCVTHRLAGLLSRSGGVVKDNFVPTNVGSEAF	CGRP (Calcitonin gene-related peptide)	37	Free	Amidation	Cyclic (C2-C7)	L	None	Alernative spliced product of calcitonon produced by thyroid gland	Vasodilator and cause tumor hypoxia	Not mentioned	300-600pmol	30 (biological half-life)	hours	108000	Not mentioned	Not mentioned	Human Plasma	in vivo	None	None	Not reported
3051	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	48 hours	500Î¼g/kg	30.2	hours	108720	Rats blood proteases	Radioimmunoassay	Intravenous injection of the peptide in Hans Wistar Female rat	in vivo	None	None	Platelet count increased from 1,504Ã—103/mm3 to 2,262Ã—103/mm3,Neutophil count increased from 941/mm3 to 19,802/mm3,Monocyte count increased from 160/mm3 to 7,917/mm3,Eosinophil count increased from 86/mm3 to 1067/mm3,Basophil count increased from 11/mm3 to 653/mm3,Lymphocyte count increased from 4,210/mm3 to 24,759/mm3,RBC count decreased form 7.05Ã—106/mm3 to 5.56Ã—106/mm3,Prothrombin time increased from 13.7 to 16.7 seconds.
3056	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	Not reported	10Î¼g/kg	37	hours	133200	Monkey blood proteases	Radioimmunoassay	Intravenous injection in cynomolgus monkeys	in vivo	None	None	Not mentioned
3057	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	Not reported	2Î¼g/kg	68	hours	244800	Monkey blood proteases	Radioimmunoassay	Subcutaneous injection in cynomolgus monkeys	in vivo	None	None	Not mentioned
3058	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	Not reported	10Î¼g/kg	47	hours	169200	Monkey blood proteases	Radioimmunoassay	Subcutaneous injection in cynomolgus monkeys	in vivo	None	None	Not mentioned
3059	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	Not reported	25Î¼g/kg	45	hours	162000	Monkey blood proteases	Radioimmunoassay	Subcutaneous injection in cynomolgus monkeys	in vivo	None	None	Not mentioned
3060	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	Not reported	100Î¼g/kg	45	hours	162000	Monkey blood proteases	Radioimmunoassay	Subcutaneous injection in cynomolgus monkeys	in vivo	None	None	Not mentioned
3061	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	Not reported	2Î¼g/kg	39	hours	140400	Monkey blood proteases	Radioimmunoassay	Subcutaneous injection in cynomolgus monkeys	in vivo	None	None	Not mentioned
3062	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	Not reported	10Î¼g/kg	45	hours	162000	Monkey blood proteases	Radioimmunoassay	Subcutaneous injection in cynomolgus monkeys	in vivo	None	None	Not mentioned
3063	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	48 hours	500Î¼g/kg following dose 1	26.1	hours	93960	Monkey blood proteases	Radioimmunoassay	Intravenous injection in cynomolgus male monkey	in vivo	None	None	Platelet count increased from 381Ã—103/mm3 to 1,811Ã—103/mm3,Neutophil count increased from 4,400/mm3 to 6,900/mm3,Monocyte count increased from 450/mm3 to 1,150/mm3,Eosinophil count increased from 150/mm3 to 450/mm3,Lymphocyte count increased from 5,900/mm3 to 9,400/mm3,RBC count decreased form 5.96Ã—106/mm3 to 5.53Ã—106/mm3,Prothrombin time increased from 19.8 to 21.2 seconds.
3064	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	48 hours	500Î¼g/kg following dose 1	25.4	hours	91440	Monkey blood proteases	Radioimmunoassay	Intravenous injection in cynomolgus female monkey	in vivo	None	None	Platelet count increased from 381Ã—103/mm3 to 1,811Ã—103/mm3,Neutophil count increased from 4,400/mm3 to 6,900/mm3,Monocyte count increased from 450/mm3 to 1,150/mm3,Eosinophil count increased from 150/mm3 to 450/mm3,Lymphocyte count increased from 5,900/mm3 to 9,400/mm3,RBC count decreased form 5.96Ã—106/mm3 to 5.53Ã—106/mm3,Prothrombin time increased from 19.8 to 21.2 seconds.
3067	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	48 hours	2000Î¼g/kg following dose 1	33.8	hours	121680	Monkey blood proteases	Radioimmunoassay	Intravenous injection in cynomolgus male monkey	in vivo	None	None	Platelet count increased from 381Ã—103/mm3 to 2,405Ã—103/mm3,Neutophil count increased from 4,400/mm3 to 5,700/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 350/mm3,Lymphocyte count increased from 5,900/mm3 to 11,300/mm3,RBC count decreased form 5.96Ã—106/mm3 to 5.87Ã—106/mm3,Prothrombin time increased from 19.8 to 23.3 seconds.
3068	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	48 hours	2000Î¼g/kg following dose 1	24.2	hours	87120	Monkey blood proteases	Radioimmunoassay	Intravenous injection in cynomolgus female monkey	in vivo	None	None	Platelet count increased from 381Ã—103/mm3 to 2,405Ã—103/mm3,Neutophil count increased from 4,400/mm3 to 5,700/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 350/mm3,Lymphocyte count increased from 5,900/mm3 to 11,300/mm3,RBC count decreased form 5.96Ã—106/mm3 to 5.87Ã—106/mm3,Prothrombin time increased from 19.8 to 23.3 seconds.
3069	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	48 hours	500Î¼g/kg following dose 14	27.2	hours	97920	Monkey blood proteases	Radioimmunoassay	Intravenous injection in cynomolgus male monkey	in vivo	None	None	Platelet count increased from 381Ã—103/mm3 to 1,811Ã—103/mm3,Neutophil count increased from 4,400/mm3 to 6,900/mm3,Monocyte count increased from 450/mm3 to 1,150/mm3,Eosinophil count increased from 150/mm3 to 450/mm3,Lymphocyte count increased from 5,900/mm3 to 9,400/mm3,RBC count decreased form 5.96Ã—106/mm3 to 5.53Ã—106/mm3,Prothrombin time increased from 19.8 to 21.2 seconds.
3070	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	48 hours	500Î¼g/kg following dose 14	32.7	hours	117720	Monkey blood proteases	Radioimmunoassay	Intravenous injection in cynomolgus female monkey	in vivo	None	None	Platelet count increased from 381Ã—103/mm3 to 1,811Ã—103/mm3,Neutophil count increased from 4,400/mm3 to 6,900/mm3,Monocyte count increased from 450/mm3 to 1,150/mm3,Eosinophil count increased from 150/mm3 to 450/mm3,Lymphocyte count increased from 5,900/mm3 to 9,400/mm3,RBC count decreased form 5.96Ã—106/mm3 to 5.53Ã—106/mm3,Prothrombin time increased from 19.8 to 21.2 seconds.
3071	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	48 hours	1000Î¼g/kg following dose 14	44	hours	158400	Monkey blood proteases	Radioimmunoassay	Intravenous injection in cynomolgus male monkey	in vivo	None	None	Platelet count increased from 381Ã—103/mm3 to 2,820Ã—103/mm3,Neutophil count increased from 4,400/mm3 to 7,300/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 800/mm3,Lymphocyte count increased from 5,900/mm3 to 8,100/mm3,RBC count increased form 5.96Ã—106/mm3 to 6.16Ã—106/mm3,Prothrombin time increased from 19.8 to 21.7 seconds.
3072	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	48 hours	1000Î¼g/kg following dose 14	25.1	hours	90360	Monkey blood proteases	Radioimmunoassay	Intravenous injection in cynomolgus female monkey	in vivo	None	None	Platelet count increased from 381Ã—103/mm3 to 2,820Ã—103/mm3,Neutophil count increased from 4,400/mm3 to 7,300/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 800/mm3,Lymphocyte count increased from 5,900/mm3 to 8,100/mm3,RBC count increased form 5.96Ã—106/mm3 to 6.16Ã—106/mm3,Prothrombin time increased from 19.8 to 21.7 seconds.
3073	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	48 hours	2000Î¼g/kg following dose 14	39.3	hours	141480	Monkey blood proteases	Radioimmunoassay	Intravenous injection in cynomolgus male monkey	in vivo	None	None	Platelet count increased from 381Ã—103/mm3 to 2,405Ã—103/mm3,Neutophil count increased from 4,400/mm3 to 5,700/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 350/mm3,Lymphocyte count increased from 5,900/mm3 to 11,300/mm3,RBC count decreased form 5.96Ã—106/mm3 to 5.87Ã—106/mm3,Prothrombin time increased from 19.8 to 23.3 seconds.
3074	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	48 hours	2000Î¼g/kg following dose 14	31.3	hours	112680	Monkey blood proteases	Radioimmunoassay	Intravenous injection in cynomolgus female monkey	in vivo	None	None	Platelet count increased from 381Ã—103/mm3 to 2,405Ã—103/mm3,Neutophil count increased from 4,400/mm3 to 5,700/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 350/mm3,Lymphocyte count increased from 5,900/mm3 to 11,300/mm3,RBC count decreased form 5.96Ã—106/mm3 to 5.87Ã—106/mm3,Prothrombin time increased from 19.8 to 23.3 seconds.
3114	20687610	2010	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	c[E18,K22]-c[E30,K34]GLP-1(7-36)-NH2	30	Free	Amidation	Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K41)	L	None	Analog of GLP-1	Diagnosis and treatment of diabetes	24 hours	100Î¼M	>96	hours	345600	Neutral endopeptidase 24.11	HPLC	GLP-1 analogue (100 Î¼M) was incubated with the recombinant human NEP 24.11 enzyme (1.0 Î¼g/mL) in HEPES buffer (50 mM, pH 7.4, 50 mM NaCl) at 37 °C	in vitro	http://www.drugbank.ca/drugs/DB00133	None	EC50=1.9nM,pEC50=8.7 ±0.14
3118	20687610	2010	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	c[E16,K20]-c[E22,K26]-c[E30,K34]GLP-1(7-36)-NH2	30	Free	Amidation	Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K45)	L	None	Analog of GLP-1	Diagnosis and treatment of diabetes	24 hours	100Î¼M	>96	hours	345600	Neutral endopeptidase 24.11	HPLC	GLP-1 analogue (100 Î¼M) was incubated with the recombinant human NEP 24.11 enzyme (1.0 Î¼g/mL) in HEPES buffer (50 mM, pH 7.4, 50 mM NaCl) at 37 °C	in vitro	http://www.drugbank.ca/drugs/DB00137	None	EC50=1.8nM,pEC50=8.7 ±0.09
3120	21036718	2010	QWAVGHLM	177Lu-AMBA	9	177Lu,DO3A-CH2CO-G-(4-aminobenzoyl)	Amidation	Linear	L	None	Synthetic Bombesin like peptide	Clinical trials for use as systemic radiotherapy for hormone refractory prostate cancer (HRPC) patients.	Not mentioned	10Î¼g/mouse	26.6 ±11.7(t1/2Î²)	hours	95760	Mice plasma proteases	Radio-HPLC	Intravenous injection in PC-3M-luc-C6 tumour-bearing mice	in vivo	http://www.drugbank.ca/drugs/DB00139	None	In vitro stability =24.3 ±21.9% after 48 hours
3166	24133142	2013	HGDGSFSDEMNTILDNLAARDFINWLIQTKITDK	GLP2-2G-XTEN (Glucagon like peptide-2-2G-XTEN)	34	Free	Ahx-6-aminohexanoic acid, Mpa-3-maleimidopropionic acid conjugated to the amino group of Ahx,XTEN protein	Linear	L	None	Glucagon-like peptide 2 variant	Treatment of short bowel syndrome	Aliquots were collected at 0.08, 4, 8, 24, 48, 72, 96, 120 and 168 h	2mg/kg of rats	38.5 ±7.4	hours	138600	Rats blood proteases	ELISA,RP-HPLC	Subcutaneous injection in female Sprague €“ Dawley strain rats	in vivo	http://www.drugbank.ca/drugs/DB00185	None	GPCR Ca2+ flux mobilization assay, relative activity=1.43%
4001	38917331	2024	DHYLSTQTILSKDPNEEK-DBCO-N3-TTAATTCTGGGGGAGCCTTTTGTGGGTAGGGTTTTGTGGGTAGGGCGGGTTGGTTTTCGGGTTGGTTTTGCCCCGGAGGAGGAATT-N3-DBCO-RDHMVLLESVTAAGIT	Aptamer-split peptide conjugate	34	DBCO modified S10 at C terminus	DBCO modified S11 peptide at N terminus	Linear	L	Azide-modified aptamer fragments (5 SSA and 3 SSA) "TTAATTCTGGGGGAGCCTTTTGTGGGTAGGGTTTTGTGGGTAGGGCGGGTTGGTTTTCGGGTTGGTTTTGCCCCGGAGGAGGAATT" are conjugated with DBCO-modified peptides (S10 and S11) , DBCO = Dibenzocyclooctyne	Aptamer-peptide complex	Hetero modulator for split GFP in response to ATP	Samples were collected every 24 h for 7 days	1 μM	4	Days	345600	C57Bl/6N Mice serum protease	Serum stability assay	C57BL/6N Mice serum	In Vitro	None	None	A shorter antisense DNA of 11 nucleotides (aptamer) showed an EC50 value of 238 μM
4002	38807146	2024	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRGHAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG	TG103	62	Free	Fc region of IgG joined through (CH2-CH3) IgD	Linear	L	GLP-1 dimerization	GLP-1 analogs	Antiobesity	Blood sampling time points:(1) Within 2 h before dosing on day 1 and day 8,(2) 6, 12, 24, 36, 48, 72, 96, 144 and 168 h (before dosing on day 15) after dosing on day 8 (3)Within 2 h before dosing on day 64, day 71 and day 78 (4)6, 12, 24, 36, 48, 72, 96, 144, 168, 336 and 504 h after dosing on day 78.	15.0 mg	116 ± 10.8 (Terminal Half Life)	Hours	417600	Human serum protease	Double-antibody sandwich assay	Human serum	In Vivo	None	None	N.A.
4003	38807146	2024	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRGHAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG	TG103	62	Free	Fc region of IgG joined through (CH2-CH3) IgD	Linear	L	GLP-1 dimerization	GLP-1 analogs	Antiobesity	Blood sampling time points:(1) Within 2 h before dosing on day 1, day 8 and day 15, (2) 6, 12, 24, 36, 48, 72, 96, 144 and 168 h (before dosing on day 22) after dosing on day 15 (3)Within 2 h before dosing on day 64, day 71 and day 78 (4) 6, 12, 24, 36, 48, 72, 96, 144, 168, 336 and 504 h after dosing on day 78.	22.5 mg	110 ± 11.9 (Terminal Half Life)	Hours	396000	Human serum protease	Double-antibody sandwich assay	Human serum	In Vivo	None	None	N.A.
4004	38807146	2024	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRGHAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG	TG103	62	Free	Fc region of IgG joined through (CH2-CH3) IgD	Linear	L	GLP-1 dimerization	GLP-1 analogs	Antiobesity	Blood sampling time points: (1) Within 2 h before dosing on day 1, day 8, day 15 and day 22, (2)6, 12, 24, 36, 48, 72, 96, 144 and 168 h (before dosing on day 29) after dosing on day 22,(3)Within 2 h before dosing on day 64, day 71 and day 78 (4) 6, 12, 24, 36, 48, 72, 96, 144, 168, 336 and 504 h after dosing on day 78.	30.0 mg	116 ± 9.34 (Terminal Half Life)	Hours	396000	Human serum protease	Double-antibody sandwich assay	Human serum	In Vivo	None	None	N.A.
4013	38785334	2024	IsoV-DTHFPCIKFEPRSKGCK	Rusfertide (PTG-300)	18	IsoV = Isovaeryl at position 1	Amidation	Cyclic(C7-C17 Disulfide Linkage)	L	Lys8 conjugation with palmitoyl-Glu(2)-OH	Synthetic	Provides therapy for PV and Hemochromatosis	N.A.	10 mg	26.1 ± 7.0	Hours	93960	Human plasma protease	HPLC-MS	Human plasma	In Vivo	None	None	N.A.
4014	38785334	2024	IsoV-DTHFPCIKFEPRSKGCK	Rusfertide (PTG-300)	18	IsoV = Isovaeryl at position 1	Amidation	Cyclic(C7-C17 Disulfide Linkage)	L	Lys8 conjugation with palmitoyl-Glu(2)-OH	Synthetic	Provides therapy for PV and Hemochromatosis	N.A.	20 mg	35.4 ± 9.6	Hours	127440	Human plasma protease	HPLC-MS	Human plasma	In Vivo	None	None	N.A.
4015	38785334	2024	IsoV-DTHFPCIKFEPRSKGCK	Rusfertide (PTG-300)	18	IsoV = Isovaeryl at position 1	Amidation	Cyclic(C7-C17 Disulfide Linkage)	L	Lys8 conjugation with palmitoyl-Glu(2)-OH	Synthetic	Provides therapy for PV and Hemochromatosis	N.A.	40 mg	45.0 ± 13	Hours	162000	Human plasma protease	HPLC-MS	Human plasma	In Vivo	None	None	N.A.
4016	38785334	2024	IsoV-DTHFPCIKFEPRSKGCK	Rusfertide (PTG-300)	18	IsoV = Isovaeryl at position 1	Amidation	Cyclic(C7-C17 Disulfide Linkage)	L	Lys8 conjugation with palmitoyl-Glu(2)-OH	Synthetic	Provides therapy for PV and Hemochromatosis	N.A.	80 mg	52.5 ± 17	Hours	189000	Human plasma protease	HPLC-MS	Human plasma	In Vivo	None	None	N.A.
4017	38785334	2024	IsoV-DTHFPCIKFEPRSKGCK	Rusfertide (PTG-300)	18	IsoV = Isovaeryl at position 1	Amidation	Cyclic(C7-C17 Disulfide Linkage)	L	Lys8 conjugation with palmitoyl-Glu(2)-OH	Synthetic	Provides Therapy For Pv And Hemochromatosis	N.A.	40 mg	49.6 ± 18	Hours	178560	Human Plasma Protease	high-performance liquidchromatography–tandem mass spectrometry method	Human plasma after 2 once weekly repeated dose	In Vivo	None	None	N.A.
4018	38785334	2024	IsoV-DTHFPCIKFEPRSKGCK	Rusfertide (PTG-300)	18	IsoV = Isovaeryl at position 1	Amidation	Cyclic(C7-C17 Disulfide Linkage)	L	Lys8 conjugation with palmitoyl-Glu(2)-OH	Synthetic	Provides Therapy For Pv And Hemochromatosis	N.A.	40 mg	36.1 ± 21	Hours	129960	Human Plasma Protease	high-performance liquidchromatography–tandem mass spectrometry method	Human plasma after 2 once weekly repeated dose	In Vivo	None	None	N.A.
4026	38721043	2024	SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNFC	EXT607 (R=OH)	35	Free	Cys modified PTH-1 linked with VitD3 through (PEG)36	Linear	L	R= OH for Cys35	PTH-1 derivative	Treatment of Hypoparathyroidism	Blood samples were collected at 0 (pre-dose), 0.083 (IV only), 0.25, 0.5, 1, 2, 4, 6, 12, 24, 36, 48, 60, and 72 h post-dose	0.02 mg/kg	32.3	Hours	116280	Cynomolgus monkeys plasma protease	ELISA	Cynomolgus monkeys plasma	In Vivo	None	None	EC50(nM) = 23.7 (Calcium responses of EXT607 in mammalian cells overexpressing human PTHR1)
4028	38721043	2024	SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNFC	EXT607 (R=OH)	35	Free	Cys modified PTH-1 linked with VitD3 through (PEG)36	Linear	L	R= OH for Cys35	PTH-1 derivative	Treatment of Hypoparathyroidism	Blood samples were collected at 0 (pre-dose), 0.083 (IV only), 0.25, 0.5, 1, 2, 4, 6, 12, 24, 36, 48, 60, and 72 h post-dose	0.02 mg/kg	24.3	Hours	87480	Cynomolgus monkeys plasma protease	ELISA	Cynomolgus monkeys plasma	In Vivo	None	None	EC50(nM) = 23.7 (Calcium responses of EXT607 in mammalian cells overexpressing human PTHR1)
4029	38721043	2024	SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNFC	EXT607 (R=OH)	35	Free	Cys modified PTH-1 linked with VitD3 through (PEG)36	Linear	L	R= OH for Cys35	PTH-1 derivative	Treatment of Hypoparathyroidism	Blood samples were collected at 0 (pre-dose), 0.083 (IV only), 0.25, 0.5, 1, 2, 4, 6, 12, 24, 36, 48, 60, and 72 h post-dose	0.07 mg/kg	27.7	Hours	99720	Cynomolgus monkeys plasma protease	ELISA	Cynomolgus monkeys plasma	In Vivo	None	None	EC50(nM) = 23.7 (Calcium responses of EXT607 in mammalian cells overexpressing human PTHR1)
4046	38486997	2024	HsQGTFTSDKSKYLE-Aib-KAAQDFVEWLKAGGPSSGAPPPS	1907-B	40	Free	Replacing the amide bond with a C-terminal acid	Cyclic (Lactam Bridge K17 & D21)	Mix	At position 10 of the peptide sequence, modifications involving octadecanedioic acid (C18) and a glycine/serine-based linker "GGSGSG" were introduced, Aib modification,D-serine	GLP-1 analogs	Antidiabetes	N.A.	25.0 μg/kg	84	Hours	302400	Cynomolgus monkeys plasma protease	HPLC-MS/MS	Cynomolgus monkeys plasma	In Vivo	None	None	GLP-1R EC50 (nmol/L) = 0.088 (for 1907-B)
4048	38399408	2024	None	BI-X	None	N.A.	N.A.	N.A.	N.A.	N.A.	Synthetic	Treatment Of Human Ocular Disease	serial blood samples were taken in EDTA anticoagulant pre-dose and at 1 h, 2 h, 4 h, 24 h, 48 h, 72 h, 96 h, and 168 h and 2, 4, 6, 8, and 10 weeks after dosing or until the last in-life timepoint of the animals.	0.25 mg/eye	3	Days	259200	Cynomolgus Monkeys Plasma Protease	Immunocapture-LC-MS/MS	Cynomolgus monkeys plasma	In Vivo	None	None	Affinity binding site to human albumin (KD = 1.4 nM)
4049	38399408	2024	None	BI-X	None	N.A.	N.A.	N.A.	N.A.	N.A.	Synthetic	Treatment Of Human Ocular Disease	serial blood samples were taken in EDTA anticoagulant pre-dose and at 1 h, 2 h, 4 h, 24 h, 48 h, 72 h, 96 h, and 168 h and 2, 4, 6, 8, and 10 weeks after dosing or until the last in-life timepoint of the animals.	0.25 mg/eye	13.2	Days	1140480	Cynomolgus Monkeys Plasma Protease	Immunocapture-LC-MS/MS	Cynomolgus monkeys plasma	In Vivo	None	None	Affinity binding site to human albumin (KD = 1.4 nM)
4050	38399408	2024	None	BI-X	None	N.A.	N.A.	N.A.	N.A.	N.A.	Synthetic	Treatment Of Human Ocular Disease	serial blood samples were taken in EDTA anticoagulant pre-dose and at 1 h, 2 h, 4 h, 24 h, 48 h, 72 h, 96 h, and 168 h and 2, 4, 6, 8, and 10 weeks after dosing or until the last in-life timepoint of the animals.	0.25 mg/eye	11.8	Days	1019520	Cynomolgus Monkeys Plasma Protease	Immunocapture-LC-MS/MS	Cynomolgus monkeys plasma	In Vivo	None	None	Affinity binding site to human albumin (KD = 1.4 nM)
4051	38356317	2024	Y-Aib-EGTFTSDYSI-Aib-LDKIAQKAFVQWLIAGGPSSGAPPPS	Tirzepatide	39	Free	Amidation	Linear	L	C20 fatty diacid moiety conjugated with Lys20, Aib modification at position 2,13	GLP-1 analogs	Antidiabetes	PK samples were collected after single and multiple doses, up to 109 weeks of continuous tirzepatide treatment	2–500 ng/mL.	5.4	Days	466560	Human plasma protease	LC-MS	Human plasma	In Vivo	None	None	N.A.
4053	38340726	2024	IEEQAKTFLDKFNHEAEDLFYQSSLGGSKGDFRGGGGSGGGGSGGGGSGGGGSGGGGSGGGGSGGGGSDVDLGDISGINASVVNIQKEIDRLNEVAKNLNESLIDLQELGKYEQ	A1L35HR2m-Chol	114	Conjugation of angiotensin-converting enzyme 2 (ACE2)-derived peptide A1 to the N terminus of the viral HR2-derived peptide HR2m through a long flexible linker,	Chol conjugation at C terminal	Linear	L	None	fusion protein of A1 and HR2m	Antiviral (Inhibits Coronaviruses)	Sera were collected from these mice before (0 h) and 2, 4, 8, 12, 24, 48, 72, 120, 168, 240 and 336 h after injection	5 mg/kg	81.83	Hours	294588	Balb/c mice serum protease	N.A.	BALB/c mice serum	In Vivo	None	None	A1L35HR2m was highly potent in inhibiting SARS-CoV-2 infection with an IC50 value of 27 nM
4054	38340726	2024	IEEQAKTFLDKFNHEAEDLFYQSSLGGSKGDFRGGGGSGGGGSGGGGSGGGGSGGGGSGGGGSGGGGSDVDLGDISGINASVVNIQKEIDRLNEVAKNLNESLIDLQELGKYEQ	A1L35HR2m-Chol	114	Conjugation of angiotensin-converting enzyme 2 (ACE2)-derived peptide A1 to the N terminus of the viral HR2-derived peptide HR2m through a long flexible linker,	Chol conjugation at C terminal	Linear	L	None	fusion protein of A1 and HR2m	Antiviral (Inhibits Coronaviruses)	N.A.	5 mg/kg	89.8	Hours	323280	Balb/c mice serum protease	N.A.	Balb/c mice lung tissue homogenate	In Vivo	None	None	A1L35HR2m was highly potent in inhibiting SARS-CoV-2 infection with an IC50 value of 27 nM
4056	38340726	2024	IEEQAKTFLDKFNHEAEDLFYQSSLGGSKGDFRGGGGSGGGGSGGGGSGGGGSGGGGSGGGGSGGGGSDVDLGDISGINASVVNIQKEIDRLNEVAKNLNESLIDLQELGKYEQ	A1L35HR2m-Chol	114	Conjugation of angiotensin-converting enzyme 2 (ACE2)-derived peptide A1 to the N terminus of the viral HR2-derived peptide HR2m through a long flexible linker,	Chol conjugation at C terminal	Linear	L	None	fusion protein of A1 and HR2m	Antiviral (Inhibits Coronaviruses)	N.A.	5 mg/kg	49	Hours	176400	Balb/c mice serum protease	N.A.	Balb/c mice nose tissue homogenate	In Vivo	None	None	A1L35HR2m was highly potent in inhibiting SARS-CoV-2 infection with an IC50 value of 27 nM
4062	38006944	2024	CGKGGGGGIEGPTLRQWLAARAGGGGGGGGIEGPTLRQWLAARA	Fatty Acid Modified TMP	108	Free	Free	Linear	L	C41H70O15N4 fatty acid modification	TMP analogue	Treatment of Thrombocytopenia	N.A.	100 μg/kg	128.5	Hours	462600	Beagle dogs plasma protease	ELISA	Beagle dogs plasma	In Vivo	None	None	The modified TMPs, particularly the C41H70O15N4 group, showed enhanced and prolonged activity, reaching peak platelet counts of 5047 × 10⁹/L at 216 hours (enhanced platelet counts)
4065	US 2023/0072968 W	2024	Y-Aib-EGT-aMeF-TSD-4Pal-SI-aMeL-LDOKAQ-Aib-EFIq-aMeY-LIEGGPSSGAPPPS	Compound 1	43	Free	Amidation	Linear	Mix	Aib2, aMeF(2F)6, 4PallO, aMeL13, Ornl6, K17, Aib20, D-Glu24 aMeY25, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H)	Incretin Analog	Antidiabetes	Blood sample collected over 36 Hours	4.06 nmol/kg	68	Hours	244800	Dogs plasma protease	LC-MS	Dogs plasma	In Vivo	None	US 2023/0072968 W	N.A.
4066	US 2023/0072968 W	2024	Y-Aib-EGT-aMeF-TSD-4Pal-SI-aMeL-LDOKAQ-Aib-EFIq-aMeY-LIEGGPSSGAPPPS	Compound 1	43	Free	Amidation	Linear	Mix	Aib2, aMeF(2F)6, 4PallO, aMeL13, Ornl6, K17, Aib20, D-Glu24 aMeY25, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H)	Incretin Analog	Antidiabetes	Blood sample collected over 168 Hours	386.4 nmol/kg	64	Hours	230400	Dogs plasma protease	LC-MS	Dogs plasma	In Vivo	None	US 2023/0072968 W	N.A.
4067	US 2023/0072968 W	2024	Y-Aib-EGT-aMeF-TSD-4Pal-SI-aMeL-LDOKAQ-Aib-EFIq-aMeY-LIEGGPSSGAPPPS	Compound 1	43	Free	Amidation	Linear	Mix	Aib2, aMeF(2F)6, 4PallO, aMeL13, Ornl6, K17, Aib20, D-Glu24 aMeY25, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H)	Incretin Analog	Antidiabetes	Blood sample collected over 168 Hours	350.4 nmol/kg	77	Hours	277200	Dogs plasma protease	LC-MS	Dogs plasma	In Vivo	None	US 2023/0072968 W	N.A.
4068	US 2023/0072968 W	2024	Y-Aib-EGT-aMeF-TSD-4Pal-SI-aMeL-LDOKAQ-Aib-EFIq-aMeY-LIEGGPSSGAPPPS	Compound 1	43	Free	Amidation	Linear	Mix	Aib2, aMeF(2F)6, 4PallO, aMeL13, Ornl6, K17, Aib20, D-Glu24 aMeY25, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H)	Incretin Analog	Antidiabetes	Blood sample collected over 168 Hours	352.5 nmol/kg	76	Hours	273600	Dogs plasma protease	LC-MS	Dogs plasma	In Vivo	None	US 2023/0072968 W	N.A.
4069	US 2023/0072968 W	2024	Y-Aib-EGT-aMeF-TSD-4Pal-SI-aMeL-LDOKAQ-Aib-EFIq-aMeY-LIEGGPSSGAPPPS	Compound 1	43	Free	Amidation	Linear	Mix	Aib2, aMeF(2F)6, 4PallO, aMeL13, Ornl6, K17, Aib20, D-Glu24 aMeY25, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H)	Incretin Analog	Antidiabetes	Blood sample collected over 168 Hours	375.7 nmol/kg	46	Hours	165600	Dogs plasma protease	LC-MS	Dogs plasma after food is provided 1 min post dose	In Vivo	None	US 2023/0072968 W	N.A.
4070	US 2023/0072968 W	2024	Y-Aib-EGT-aMeF-TSD-4Pal-SI-aMeL-LDOKAQ-Aib-EFIq-aMeY-LIEGGPSSGAPPPS	Compound 1	43	Free	Amidation	Linear	Mix	Aib2, aMeF(2F)6, 4PallO, aMeL13, Ornl6, K17, Aib20, D-Glu24 aMeY25, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H)	Incretin Analog	Antidiabetes	Blood sample collected over 168 Hours	377.1 nmol/kg	55	Hours	198000	Dogs plasma protease	LC-MS	Dogs plasma after food is provided 30 min post dose	In Vivo	None	US 2023/0072968 W	N.A.
4071	US 2023/0072968 W	2024	Y-Aib-EGT-aMeF-TSDYSI-aMeL-LDOKAQ-Aib-EFIqYLIEGGPSSGAPPPS	Compound 2	40	Free	Amidation	Linear	Mix	Aib2, aMeF(2F)6, aMeL13, Ornl6, K17, Aib20, D-Glu24, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H)	Incretin Analog	Antidiabetes	Blood sample collected over 336 Hours	4.06 nmol/kg	105	Hours	378000	Dogs plasma protease	LC-MS	Dogs plasma after food is provided 30 min post dose	In Vivo	None	US 2023/0072968 W	N.A.
4072	US 2023/0072968 W	2024	Y-Aib-EGT-aMeF-TSDYSI-aMeL-LDOKAQ-Aib-EFIqYLIEGGPSSGAPPPS	Compound 2	40	Free	Amidation	Linear	Mix	Aib2, aMeF(2F)6, aMeL13, Ornl6, K17, Aib20, D-Glu24, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H)	Incretin Analog	Antidiabetes	Blood sample collected over 168 Hours	389 nmol/kg	96	Hours	345600	Dogs plasma protease	LC-MS	Dogs plasma after treatment with Sodium Caprate (C10, 280Mg)	In Vivo	None	US 2023/0072968 W	N.A.
4073	US 2023/0072968 W	2024	Y-Aib-EGTFTSDYSI-Aib-LDKIAQKA-Nal-VQWLIAGGPSSGAPPPS	Compound 3	40	Free	Amidation	Linear	L	Aib2, Aibl3 and 1-Nal22 substituitions, Lys20 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)18-CO2H)	Incretin Analog	Antidiabetes	Blood sample collected over 336 Hours	4.01 nmol/kg	104	Hours	374400	Dogs plasma protease	LC-MS	Dogs plasma	In Vivo	None	US 2023/0072968 W	N.A.
4074	US 2023/0072968 W	2024	Y-Aib-EGTFTSDYSI-Aib-LDKIAQKA-Nal-VQWLIAGGPSSGAPPPS	Compound 3	40	Free	Amidation	Linear	L	Aib2, Aibl3 and 1-Nal22 substituitions, Lys20 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)18-CO2H)	Incretin Analog	Antidiabetes	Blood sample collected over 336 Hours	20 mg	111	Hours	399600	Dogs plasma protease	LC-MS	Dogs plasma	In Vivo	None	US 2023/0072968 W	N.A.
4075	US 2023/0072968 W	2024	Y-Aib-EGTFTSDYSI-Aib-LDKIAQKA-Nal-VQWLIAGGPSSGAPPPS	Compound 3	40	Free	Amidation	Linear	L	Aib2, Aibl3 and 1-Nal22 substituitions, Lys20 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)18-CO2H)	Incretin Analog	Antidiabetes	Blood sample collected over 336 Hours	20 mg	104	Hours	374400	Dogs plasma protease	LC-MS	Dogs plasma	In Vivo	None	US 2023/0072968 W	N.A.
4076	US 2023/0072968 W	2024	Y-Aib-EGTFTSDYSI-Aib-LDKIAQKAFVQWLIAGGPSSGAPPPS	TZP	40	Free	Amidation	Linear	L	Aib2, Aibl3 substituitions, Lys20 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)1-CO-(CH2)18-CO2H)	Incretin Analog	Antidiabetes	Blood sample collected over 336 Hours	4.15 nmol/kg	70	Hours	252000	Dogs plasma protease	LC-MS	Dogs plasma	In Vivo	None	US 2023/0072968 W	N.A.
4077	US 2023/0072968 W	2024	Y-Aib-EGTFTSDYSI-Aib-LDKIAQKAFVQWLIAGGPSSGAPPPS	TZP	40	Free	Amidation	Linear	L	Aib2, Aibl3 substituitions, Lys20 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)1-CO-(CH2)18-CO2H)	Incretin Analog	Antidiabetes	Blood sample collected over 336 Hours	4.15 nmol/kg	159	Hours	572400	Dogs plasma protease	LC-MS	Dogs plasma	In Vivo	None	US 2023/0072968 W	N.A.
4078	US 2023/0072968 W	2024	Y-Aib-EGTFTSDYSI-Aib-LDKIAQKAFVQWLIAGGPSSGAPPPS	TZP	40	Free	Amidation	Linear	L	Aib2, Aibl3 substituitions, Lys20 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)1-CO-(CH2)18-CO2H)	Incretin Analog	Antidiabetes	Blood sample collected over 336 Hours	20 mg	97	Hours	349200	Dogs plasma protease	LC-MS	Dogs plasma	In Vivo	None	US 2023/0072968 W	N.A.
4129	38288338	2024	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Efpeglenatide	39	N terminal amine group of His replaced by imidazo-acetyl	Amidation	Linear	L	Conjugate in which LYS27 side chain linked to PEG-Fc	Exendin-4 analogs	Antidiabetes	Blood samples were taken for PK measures pre-dose and at 1, 2, 4, 8, and 12 h post-dose on day 1, and once on days 2, 4, 7, 10, 14, 21, 28, 35, 42, and 49	4 μg/kg	144 (terminal elimination half life)	Hours	518400	Human serum protease	Sandwich ELISA	Human serum	In Vivo	https://pubmed.ncbi.nlm.nih.gov/32175655/	None	N.A.
4130	38288338	2024	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Efpeglenatide	39	N terminal amine group of His replaced by imidazo-acetyl	Amidation	Linear	L	Conjugate in which LYS27 side chain linked to PEG-Fc	Exendin-4 analogs	Antidiabetes	Blood samples were taken for PK measures pre-dose and at 1, 2, 4, 8, and 12 h post-dose on day 1, and once on days 2, 4, 7, 10, 14, 21, 28, 35, 42, and 49	8 μg/kg	147 (terminal elimination half life)	Hours	529200	Human serum protease	Sandwich ELISA	Human serum	In Vivo	https://pubmed.ncbi.nlm.nih.gov/32175655/	None	N.A.
4131	38288338	2024	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Efpeglenatide	39	N terminal amine group of His replaced by imidazo-acetyl	Amidation	Linear	L	Conjugate in which LYS27 side chain linked to PEG-Fc	Exendin-4 analogs	Antidiabetes	Blood samples were taken for PK measures pre-dose and at 1, 2, 4, 8, and 12 h post-dose on day 1, and once on days 2, 4, 7, 10, 14, 21, 28, 35, 42, and 49	14 μg/kg	135 (terminal elimination half life)	Hours	486000	Human serum protease	Sandwich ELISA	Human serum	In Vivo	https://pubmed.ncbi.nlm.nih.gov/32175655/	None	N.A.
4132	38288338	2024	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Efpeglenatide	39	N terminal amine group of His replaced by imidazo-acetyl	Amidation	Linear	L	Conjugate in which LYS27 side chain linked to PEG-Fc	Exendin-4 analogs	Antidiabetes	Blood samples were taken for PK measures pre-dose and at 1, 2, 4, 8, and 12 h post-dose on day 1, and once on days 2, 4, 7, 10, 14, 21, 28, 35, 42, and 49	20 μg/kg	147 (terminal elimination half life)	Hours	529200	Human serum protease	Sandwich ELISA	Human serum	In Vivo	https://pubmed.ncbi.nlm.nih.gov/32175655/	None	N.A.
4133	38288338	2024	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Efpeglenatide	39	N terminal amine group of His replaced by imidazo-acetyl	Amidation	Linear	L	Conjugate in which LYS27 side chain linked to PEG-Fc	Exendin-4 analogs	Antidiabetes	Blood samples were taken for PK measures pre-dose and at 1, 2, 4, 8, and 12 h post-dose on day 1, and once on days 2, 4, 7, 10, 14, 21, 28, 35, 42, and 49	40 μg/kg	141 (terminal elimination half life)	Hours	507600	Human serum protease	Sandwich ELISA	Human serum	In Vivo	https://pubmed.ncbi.nlm.nih.gov/32175655/	None	N.A.
4134	38288338	2024	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Efpeglenatide	39	N terminal amine group of His replaced by imidazo-acetyl	Amidation	Linear	L	Conjugate in which LYS27 side chain linked to PEG-Fc	Exendin-4 analogs	Antidiabetes	Blood samples were taken for PK measures pre-dose and at 1, 2, 4, 8, and 12 h post-dose on day 1, and once on days 2, 4, 7, 10, 14, 21, 28, 35, 42, and 49	60 μg/kg	154 (terminal elimination half life)	Hours	554400	Human serum protease	Sandwich ELISA	Human serum	In Vivo	https://pubmed.ncbi.nlm.nih.gov/32175655/	None	N.A.
4135	38288338	2024	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Efpeglenatide	39	N terminal amine group of His replaced by imidazo-acetyl	Amidation	Linear	L	Conjugate in which LYS27 side chain linked to PEG-Fc	Exendin-4 analogs	Antidiabetes	Blood samples were taken for PK measures pre-dose and at 1, 2, 4, 8, and 12 h post-dose on day 1, and once on days 2, 4, 7, 10, 14, 21, 28, 35, 42, and 49	100 μg/kg	180 (terminal elimination half life)	Hours	648000	Human serum protease	Sandwich ELISA	Human serum	In Vivo	https://pubmed.ncbi.nlm.nih.gov/32175655/	None	N.A.
4136	38288338	2024	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Efpeglenatide	39	N terminal amine group of His replaced by imidazo-acetyl	Amidation	Linear	L	Conjugate in which LYS27 side chain linked to PEG-Fc	Exendin-4 analogs	Antidiabetes	blood samples were taken for PK assessments pre-dose on the first dosing day (day 1) and 8, 24, 48, 72, 96, 120, and 144 h after the first dose. Trough samples were taken immediately before dosing on days 8, 22, 36, and 50. Samples were taken again after the last (eighth) dose at 8, 24, 48, 72, 96, 120, and 144 h after dosing and 7, 10, 14, 21, 28, and 35 days after dosing	1 mg	155.03 (terminal elimination half life)	Hours	558108	Human serum protease	Sandwich ELISA	Human serum	In Vivo	https://pubmed.ncbi.nlm.nih.gov/32175655/	None	N.A.
4137	38288338	2024	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Efpeglenatide	39	N terminal amine group of His replaced by imidazo-acetyl	Amidation	Linear	L	Conjugate in which LYS27 side chain linked to PEG-Fc	Exendin-4 analogs	Antidiabetes	blood samples were taken for PK assessments pre-dose on the first dosing day (day 1) and 8, 24, 48, 72, 96, 120, and 144 h after the first dose. Trough samples were taken immediately before dosing on days 8, 22, 36, and 50. Samples were taken again after the last (eighth) dose at 8, 24, 48, 72, 96, 120, and 144 h after dosing and 7, 10, 14, 21, 28, and 35 days after dosing	2 mg	151.53 ( terminal elimination half life)	Hours	545508	Human serum protease	Sandwich ELISA	Human serum	In Vivo	https://pubmed.ncbi.nlm.nih.gov/32175655/	None	N.A.
4138	38288338	2024	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Efpeglenatide	39	N terminal amine group of His replaced by imidazo-acetyl	Amidation	Linear	L	Conjugate in which LYS27 side chain linked to PEG-Fc	Exendin-4 analogs	Antidiabetes	blood samples were taken for PK assessments pre-dose on the first dosing day (day 1) and 8, 24, 48, 72, 96, 120, and 144 h after the first dose. Trough samples were taken immediately before dosing on days 8, 22, 36, and 50. Samples were taken again after the last (eighth) dose at 8, 24, 48, 72, 96, 120, and 144 h after dosing and 7, 10, 14, 21, 28, and 35 days after dosing	4 mg	155.85 (terminal elimination half life)	Hours	561060	Human serum protease	Sandwich ELISA	Human serum	In Vivo	https://pubmed.ncbi.nlm.nih.gov/32175655/	None	N.A.
4139	38288338	2024	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Efpeglenatide	39	N terminal amine group of His replaced by imidazo-acetyl	Amidation	Linear	L	Conjugate in which LYS27 side chain linked to PEG-Fc	Exendin-4 analogs	Antidiabetes	blood samples were taken for PK assessments pre-dose on the first dosing day (day 1) and 8, 24, 48, 72, 96, 120, and 144 h after the first dose. Samples were also taken 7, 10, 14, and 21 days after dosing. Trough samples were taken immediately before dosing on days 29 and 57. Finally, after the last (third) dose, samples were taken 8, 24, 48, 72, 96, 120, and 144 h after dosing and 7, 10, 14, 21, 28, and 35 days after dosing	8 mg	159.95 (terminal elimination half life)	Hours	575820	Human serum protease	Sandwich ELISA	Human serum	In Vivo	https://pubmed.ncbi.nlm.nih.gov/32175655/	None	N.A.
4140	38288338	2024	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Efpeglenatide	39	N terminal amine group of His replaced by imidazo-acetyl	Amidation	Linear	L	Conjugate in which LYS27 side chain linked to PEG-Fc	Exendin-4 analogs	Antidiabetes	blood samples were taken for PK assessments pre-dose on the first dosing day (day 1) and 8, 24, 48, 72, 96, 120, and 144 h after the first dose. Samples were also taken 7, 10, 14, and 21 days after dosing. Trough samples were taken immediately before dosing on days 29 and 57. Finally, after the last (third) dose, samples were taken 8, 24, 48, 72, 96, 120, and 144 h after dosing and 7, 10, 14, 21, 28, and 35 days after dosing	12 mg	170.62 (terminal elimination half life)	Hours	614232	Human serum protease	Sandwich ELISA	Human serum	In Vivo	https://pubmed.ncbi.nlm.nih.gov/32175655/	None	N.A.
4141	38288338	2024	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Efpeglenatide	39	N terminal amine group of His replaced by imidazo-acetyl	Amidation	Linear	L	Conjugate in which LYS27 side chain linked to PEG-Fc	Exendin-4 analogs	Antidiabetes	blood samples were taken for PK assessments pre-dose on the first dosing day (day 1) and 8, 24, 48, 72, 96, 120, and 144 h after the first dose. Samples were also taken 7, 10, 14, and 21 days after dosing. Trough samples were taken immediately before dosing on days 29 and 57. Finally, after the last (third) dose, samples were taken 8, 24, 48, 72, 96, 120, and 144 h after dosing and 7, 10, 14, 21, 28, and 35 days after dosing	16 mg	161.76 (terminal elimination half life)	Hours	582336	Human serum protease	Sandwich ELISA	Human serum	In Vivo	https://pubmed.ncbi.nlm.nih.gov/32175655/	None	N.A.
4142	38952487	2024	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	[3H]-semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18(3H)	GLP-1 analogs	GLP-1 receptor agonist	Blood sample were collected at predose, 8, 16, 24,32,40,48,56,64,72,96,120,144,168,240,336,504,672 and 840 hours post dose	1 mg/ml	168.3	Hours	605880	Human plasma protease	LC-MS/MS	Human plasma	In Vivo	https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/	None	N.A.
4143	38952487	2024	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Intact [3H]-semaglutide-related material	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18(3H), other metabolite may be attached	GLP-1 analogs	GLP-1 receptor agonist	Blood sample were collected at predose, 8, 16, 24,32,40,48,56,64,72,96,120,144,168,240,336,504,672 and 840 hours post dose	1 mg/ml	201.2	Hours	724320	Human plasma protease	LC-MS/MS	Human plasma	In Vivo	https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/	None	N.A.
4144	38952487	2024	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Dry [3H]-semaglutide-related material	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18(3H), other metabolite may be attached	GLP-1 analogs	GLP-1 receptor agonist	Blood sample were collected at predose, 8, 16, 24,32,40,48,56,64,72,96,120,144,168,240,336,504,672 and 840 hours post dose	1 mg/ml	180.5	Hours	649800	Human plasma protease	LC-MS/MS	Human plasma	In Vivo	https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/	None	N.A.
4145	38952487	2024	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	GLP-1 receptor agonist	Blood samples for PK assessment of semaglutide were taken at the following time points after the first dose: 0, 6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120, 144 and 168 h and at the following time points after the last dose: 0, 6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120, 144, 168, 336, 504, 672 and 840 h. Additional PK samples were taken before dosing in weeks 4, 8 and 11	0.5 mg	156	Hours	561600	Human blood sample protease	LC-MS/MS	Human blood sample with once weekly dosage (at steady state)	In Vivo	https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/	None	N.A.
4146	38952487	2024	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	GLP-1 receptor agonist	Blood samples for PK assessment of semaglutide were taken at the following time points after the first dose: 0, 6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120, 144 and 168 h and at the following time points after the last dose: 0, 6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120, 144, 168, 336, 504, 672 and 840 h. Additional PK samples were taken before dosing in weeks 4, 8 and 11	1 mg	159	Hours	572400	Human blood sample protease	LC-MS/MS	Human blood sample with once weekly dosage (at steady state)	In Vivo	https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/	None	N.A.
4147	38952487	2024	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	GLP-1 receptor agonist	blood samples were taken 15 min prior to administration of semaglutide and 2, 8, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 38, 42, 48, 54, 60, 66, 72, 96, 144, 192, 240, 360, and 480 h after administration of semaglutide	0.5 mg	183 (elimination half life)	Hours	658800	Human serum protease	LC-MS/MS	Human serum (Normal Renal Function Group)	In Vivo	https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/	None	N.A.
4148	38952487	2024	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	GLP-1 receptor agonist	blood samples were taken 15 min prior to administration of semaglutide and 2, 8, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 38, 42, 48, 54, 60, 66, 72, 96, 144, 192, 240, 360, and 480 h after administration of semaglutide	0.5 mg	169 (elimination half life)	Hours	608400	Human serum protease	LC-MS/MS	Human serum (Mild Renal Function Group)	In Vivo	https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/	None	N.A.
4149	38952487	2024	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	GLP-1 receptor agonist	blood samples were taken 15 min prior to administration of semaglutide and 2, 8, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 38, 42, 48, 54, 60, 66, 72, 96, 144, 192, 240, 360, and 480 h after administration of semaglutide	0.5 mg	201 (elimination half life)	Hours	723600	Human serum protease	LC-MS/MS	Human serum (Moderate Renal Function Group)	In Vivo	https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/	None	N.A.
4150	38952487	2024	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	GLP-1 receptor agonist	blood samples were taken 15 min prior to administration of semaglutide and 2, 8, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 38, 42, 48, 54, 60, 66, 72, 96, 144, 192, 240, 360, and 480 h after administration of semaglutide	0.5 mg	221 (elimination half life)	Hours	795600	Human serum protease	LC-MS/MS	Human serum (Severe Renal Function Group)	In Vivo	https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/	None	N.A.
4151	38952487	2024	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	GLP-1 receptor agonist	For ESRD subjects on hemodialysis, hourly blood samples were drawn during each of the first two hemodialysis sessions post-administration (each hemodialysis session lasted for ~2–4 h).	0.5 mg	243 (elimination half life)	Hours	874800	Human serum protease	LC-MS/MS	Human serum dosage 1–24 H after hemodialysis, With No Hemodialysis For 48 H Post-Dose (End Stage Renal Disease Renal Function Group)	In Vivo	https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/	None	N.A.
4152	38952487	2024	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	GLP-1 receptor agonist	Blood samples were taken to determine the plasma concentration profiles of semaglutide 15 minutes prior to dosing, at time zero, and at 6, 12, 18, 24, 30, 36, 42, 48, 54, 60, 72, 96, 120, 144, 168, 336, 504, 672 and 840 hours (up to 35 days) after administration of semaglutide	0.5 mg	150 (Terminal elimination half life)	Hours	540000	Human plasma protease	LC-MS/MS	Human plasma (Normal Hepatic Function Group)	In Vivo	https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/	None	N.A.
4153	38952487	2024	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	GLP-1 receptor agonist	Blood samples were taken to determine the plasma concentration profiles of semaglutide 15 minutes prior to dosing, at time zero, and at 6, 12, 18, 24, 30, 36, 42, 48, 54, 60, 72, 96, 120, 144, 168, 336, 504, 672 and 840 hours (up to 35 days) after administration of semaglutide	0.5 mg	155 (Terminal elimination half life)	Hours	558000	Human plasma protease	LC-MS/MS	Human plasma (Mild Hepatic Function Group)	In Vivo	https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/	None	N.A.
4154	38952487	2024	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	GLP-1 receptor agonist	Blood samples were taken to determine the plasma concentration profiles of semaglutide 15 minutes prior to dosing, at time zero, and at 6, 12, 18, 24, 30, 36, 42, 48, 54, 60, 72, 96, 120, 144, 168, 336, 504, 672 and 840 hours (up to 35 days) after administration of semaglutide	0.5 mg	151 (Terminal elimination half life)	Hours	543600	Human plasma protease	LC-MS/MS	Human plasma (Moderate Hepatic Function Group)	In Vivo	https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/	None	N.A.
4155	38952487	2024	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	GLP-1 receptor agonist	Blood samples were taken to determine the plasma concentration profiles of semaglutide 15 minutes prior to dosing, at time zero, and at 6, 12, 18, 24, 30, 36, 42, 48, 54, 60, 72, 96, 120, 144, 168, 336, 504, 672 and 840 hours (up to 35 days) after administration of semaglutide	0.5 mg	163 (Terminal elimination half life)	Hours	586800	Human plasma protease	LC-MS/MS	Human plasma (Severe Hepatic Function Group)	In Vivo	https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/	None	N.A.
4156	38952487	2024	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	GLP-1 receptor agonist	N.A.	20 mg	153	Hours	550800	Human plasma protease	Luminescence oxygen channelling immunoassay (LOCI)	Human plasma dosed at steady state (Healthy)	In Vivo	https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/	None	N.A.
4157	38952487	2024	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	GLP-1 receptor agonist	N.A.	40 mg	161	Hours	579600	Human plasma protease	Luminescence oxygen channelling immunoassay (LOCI)	Human plasma dosed at steady state (Healthy)	In Vivo	https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/	None	N.A.
4158	38952487	2024	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	GLP-1 receptor agonist	N.A.	40 mg	158	Hours	568800	Human plasma protease	Luminescence oxygen channelling immunoassay (LOCI)	Human plasma dosed at steady state (Type 2 Diabetic)	In Vivo	https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/	None	N.A.
4159	38952487	2024	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	GLP-1 receptor agonist	10 days	10 mg	160	Hours	576000	Human plasma protease	LC-MS/MS	Human plasma dosed with 10 mg Once Daily Semaglutide (Subjects In The Fasting Arm Were Fasting Overnight For At Least 10 H Before Each Dosing)	In Vivo	https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/	None	N.A.
4160	38952487	2024	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	GLP-1 receptor agonist	10 days	10 mg	152	Hours	547200	Human plasma protease	LC-MS/MS	Human plasma dosed with 10 Mg Once Daily Semaglutide (Subjects In The Reference Arm Were Fasting Overnight For At Least 6 H Before Each Dosing)	In Vivo	https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/	None	N.A.
4161	38952487	2024	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	GLP-1 receptor agonist	Blood samples for semaglutide PK assessment were drawn onday 1 (pre- and post-dose), then pre-dose on days 6 to 10	7 mg	141	Hours	507600	Human plasma protease	N.A.	Human plasma (Type 2 Diabetic Patient With Upper Gastrointestinal Disease)	In Vivo	https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/	None	N.A.
4162	38952487	2024	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	GLP-1 receptor agonist	Blood samples for semaglutide PK assessment were drawn onday 1 (pre- and post-dose), then pre-dose on days 6 to 10	7 mg	142	Hours	511200	Human plasma protease	N.A.	Human plasma (Type 2 Diabetic Patient Without Upper Gastrointestinal Disease)	In Vivo	https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/	None	N.A.
4163	38952487	2024	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	GLP-1 receptor agonist	Blood samples were drawn into K3EDTA tubes pre-dose on day 1, and at set time points on days 9 and 10	10 mg	150	Hours	540000	Human plasma protease	LC-MS/MS	Human plasma dosed with 10 mg Semaglutide Once Daily For 5 Days	In Vivo	https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/	None	N.A.
4164	38952487	2024	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	GLP-1 receptor agonist	Blood samples were drawn into K3EDTA tubes pre-dose on day 1, and at set time points on days 9 and 10	10 mg	156	Hours	561600	Human plasma protease	LC-MS/MS	Human plasma dosed with 10 mg Semaglutide Once Daily For 5 Days And With Omeprazole 40 Mg	In Vivo	https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/	None	N.A.
4165	38116563	2023	MKIILWLCVFGLFLATLFPISWQMPVESGLSSEDSASSESFASKIKRHGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSGGGGGSGGGGSGGGGS-(DARP)-GGGGSGGGGSGGGGSMDSDETGFEHSGLWVSVLAGLLLGACQAHPIPDSSPLLQFGGQVRQRYLYTDDAQQTEAHLEIREDGTVGGAADQSPESLLQLKALKPGVIQILGVKTSRFLCQRPDGALYGSLHFDPEACSFRELLLEDGYNVYQSEAHGLPLHLPGNKSPHRDPAPRGPARFLPLPGLPPALPEPPGILAPQPPDVGSSDPLSMVGPSQGRSPSYAS	Ex-DARP-FGF21	327	Exendin-4 peptide (Ex) fused to the N-terminus of the DARPin (DARP) protein via (GGGGS)3, His-tag and TEV protease site introduced at position 1	FGF21 fused to the C-terminus of the DARPin (DARP) protein via (GGGGS)3 linker	Linear	L	L98R and P171A amino acid substitutions in FBGF21	Exendin-4, DARPin, FGF21 fusion protein	Antidiabetes, Antiobesity	Approximately 40 µL of blood was collected from the orbital venous plexus at different time points (1, 3, 8, 12, 24, 36, 48, and 72 h)	10 nmol/kg	27.6 ± 3.2	Hours	99360	C57BL/6 mice plasma protease	ELISA	C57BL/6 mice plasma	In Vivo	None	None	Ex-DARP-FGF21 and Ex-DARP were efficaciously bound to HSA with half-maximal binding concentrations of 4.5 nM and 1.9 nM, respectively
4180	37874823	2023	GWGIPWCTLDPGSLQCAWLGKHGGGGSGGVVCQDWEGVELCWQGG	MDK1472	42	Acetylation	Free	Cyclic (Disulphide Bond Bw C7-C16, C32-C41)	L	IL-7Ra binding domain linked with yc binding domain with the help of linker GGS linker	Synthetic	IL-7R agonist peptide	37 °C	10 mM	60	Hours	216000	Human Plasma Protease	LC-MS/MS	Human plasma	In Vitro	None	None	IC50(nM) = 340 (IC50 values in a competition ELISA for compound binding to human IL-7Rα)
4181	37874823	2023	GWGIPWCTLDPGSLQCAWLGKHGGGGSGGVVCQDWEGVELCWQGG	MDK1472	42	Acetylation	Free	Cyclic (Disulphide Bond Bw C7-C16, C32-C41)	L	IL-7Ra binding domain linked with yc binding domain with the help of linker GGS linker	Synthetic	IL-7R agonist peptide	37 °C	10 mM	104	Hours	374400	Cynomolgus monkeys plasma protease	LC-MS/MS	Cynomolgus monkeys plasma	In Vitro	None	None	IC50(nM) = 190 (IC50 values in a competition ELISA for compound binding to Cyno IL-7Rα)
4182	37874823	2023	GSGSGSGSGSGSGSGSGSGSGWGIPWCTLDPGSLQCAWLGKHGGGGSGGVVCQDWEGVELCWQGGGWGIPWCTLDPGSLQCAWLGKHGGGGSGGVVCQDWEGVELCWQGG	MDK-703	110	Fused with IgG2 Fc chain via (Gly-Ser)10 linker, Fc-fragments consisting of the CH2 and CH3 domains of the heavy chain and hinge regions of human IgG2 Fc modified as follows: The first and second cysteines of the hinge region were replaced with serine to prevent detrimental disulfide bridge formation; the last amino acid (lysine) of the Fc region was replaced with an alanine	Free	Linear	L	None	Synthetic	IL-7R agonist peptide	Blood samples were collected at pre-Dose (day 1), 0.5, 1 h, 2 h, 4 h, 8 h, 24 h, 48 h, 72 h, 96 h, 120 h, 144 h, 168 h, 192 h, and 216 h post-dose	1 mg/kg	46 (Terminal Half Life)	Hours	165600	Cynomolgus monkeys serum protease	Sandwich ELISA	Cynomolgus monkeys serum	In Vivo	None	None	IC50(nM) = 190 (IC50 values in a competition ELISA for compound binding to Cyno IL-7Rα)
4184	37759683	2023	DCAWHLGELVWCTSLDQINVTFLDLEYEMKKLEEAIKKLEESYIDLKEL	IBP-EK1	32	Conjugation with human immunoglobulin G Fc-binding peptide (IBP) at n terminus	Free	Linear	L	None	Fusion protein	Antiviral	Serial blood samples were collected from monkeys that received IBP-EK1 or EK1 before injection and at 2, 4, 6, 24, 72, and 144 h post injection	10 mg/kg	37.67	Hours	135612	Rhesus monkeys serum protease	HPLC-MS/MS	Rhesus monkeys serum	In Vivo	None	None	IC50 = 788 nM for IBP-EK1 ( against Pseudotyped SARS-CoV-2 Variants on Caco-2 Cells)
4185	37759683	2023	DCAWHLGELVWCTSLDQINVTFLDLEYEMKKLEEAIKKLEESYIDLKEL	IBP-EK1	32	Conjugation with human immunoglobulin G Fc-binding peptide (IBP) at n terminus	Free	Linear	L	None	Fusion protein	Antiviral	Serial blood samples were collected from monkeys that received IBP-EK1 or EK1 before injection and at 2, 4, 6, 24, 72, and 144 h post injection	10 mg/kg	39.72	Hours	142992	Rhesus monkeys serum protease	HPLC-MS/MS	Rhesus monkeys serum	In Vivo	None	None	IC50 = 788 nM for IBP-EK1 ( against Pseudotyped SARS-CoV-2 Variants on Caco-2 Cells)
4244	36780899	2023	SWMEEVIKLCGRELVRAQIAICGMSTWSXGGGSGGSGGGQLYSALANKCCHVGCTKRSLARFCX	LY3540378	64	Free	Relaxin-A chain linked with albVHH domain at C terminus, A and B chain linked by linker	Linear	L	None	relaxin-2 analog	Treatment of Chronic Heart Failure	N.A.	200 nmol/kg	36.4 (Terminal Half Life)	Hours	131040	Rats plasma protease	LC-MS	Rats plasma	In Vivo	None	None	EC 50 (nM) = 109 ± 24 of LY3540378 in Rat RXFP2
4245	36780899	2023	SWMEEVIKLCGRELVRAQIAICGMSTWSXGGGSGGSGGGQLYSALANKCCHVGCTKRSLARFCX	LY3540378	64	Free	Relaxin-A chain linked with albVHH domain at C terminus, A and B chain linked by linker	Linear	L	None	relaxin-2 analog	Treatment of Chronic Heart Failure	N.A.	100 nmol/kg	124 (Terminal Half Life)	Hours	446400	Cynomolgus monkeys plasma protease	LC-MS	Cynomolgus monkeys plasma	In Vivo	None	None	EC 50 (nM) = 19.3 ± 4.0 of LY3540378 in Cynomolgus monkey RXFP2
4246	36780899	2023	SWMEEVIKLCGRELVRAQIAICGMSTWSXGGGSGGSGGGQLYSALANKCCHVGCTKRSLARFCX	LY3540378	64	Free	Relaxin-A chain linked with albVHH domain at C terminus, A and B chain linked by linker	Linear	L	None	relaxin-2 analog	Treatment of Chronic Heart Failure	N.A.	100 nmol/kg	45.7 (Terminal Half Life)	Hours	164520	Cynomolgus monkeys plasma protease	LC-MS	Cynomolgus monkeys plasma	In Vivo	None	None	EC 50 (nM) = 19.3 ± 4.0 of LY3540378 in Cynomolgus monkey RXFP2
4247	36780899	2023	SWMEEVIKLCGRELVRAQIAICGMSTWSXGGGSGGSGGGQLYSALANKCCHVGCTKRSLARFCX	LY3540378	64	Free	Relaxin-A chain linked with albVHH domain at C terminus, A and B chain linked by linker	Linear	L	None	relaxin-2 analog	Treatment of Chronic Heart Failure	N.A.	30 nmol/kg	39.7 ± 1.8 (Terminal Half Life)	Hours	142920	SD rats plasma protease	LC-MS	SD rats plasma	In Vivo	None	None	EC 50 (nM) = 109 ± 24 of LY3540378 in Rat RXFP2
4265	36630826	2023	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Ex-PEGMw(46.3KDa)	39	Free	PEGylation (Mw(46.3KDa)) and linked via DBCO	Linear	L	Fluorescently labeled	Exendin-4 analogs	Antidiabetes	Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h	1000 nmol kg−1	34.91 ± 4.5(T1/2 Elimination)	Hours	125676	Naïve mice plasma protease	Fluorescence assay	Naïve mice plasma	In Vivo	None	None	EC50 = 2.7 ± 0.5 nM
4266	36630826	2023	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Ex-POEGMAopt(54.7KDa)	39	Free	POEGMA (poly[oligo(ethylene glycol) methyl ether methacrylate]) conjugation (MW opt = 54.7KDa)	Linear	L	Fluorescently labeled	Exendin-4 analogs	Antidiabetes	Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h	1000 nmol kg−1	97.3 ± 3.2(T1/2 Elimination)	Hours	350280	Naïve mice plasma protease	Fluorescence assay	Naïve mice plasma	In Vivo	None	None	EC50 = 2.8 ± 0.7 nM
4270	36630826	2023	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Ex-POEGMAopt(54.7KDa)	39	Free	POEGMA (poly[oligo(ethylene glycol) methyl ether methacrylate]) conjugation (MW opt = 54.7KDa)	Linear	L	Fluorescently labeled	Exendin-4 analogs	Antidiabetes	Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h	1000 nmol kg−1	105.7 ± 6 (T1/2 Elimination)	Hours	380520	Immunized mice plasma protease	Fluorescence assay	Immunized mice plasma	In Vivo	None	None	EC50 = 2.8 ± 0.7 nM
4274	36410792	2023	GDGSFSDEMNTILDNLAARDFINWLIQTRITDK	HM15912	34	[(1H-imidazol-4-yl)-acetyl 1]	Conjugation of GT15912 and hIgG4 Fc was carried out through the formation of amine bonds between the bi functional PEG and Lys34 in GT15912 or the N-terminal amino acid in hIgG4 Fc	Linear	L	None	GLP-2 analogue	Small Bowel Hypertrophic Effect	Blood (0.3 ml) was then collected from the jugularvein at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 hours for teduglutide and 1, 4, 8, 24, 48, 72, 96, 230, 244, 268, 192, 216, 240, 264, 288, 312, and 336 hours for HM15912	13 nmol/kg	42.3 ± 3.4	Hours	152280	SD rats serum protease	GLP-2 ELISA	SD rats serum	In Vivo	None	None	EC50 = 0.327 ± 0.096 nM for HM15912 peptide (In vitro potency of GLP-2 analogs on human GLP-2 receptor in cell-based functional assays of dose-response cAMP)
4277	36630826	2023	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Ex-PEGMw	39	Fluorescently labelled	Exendin-DBCO was conjugated to azide-functional PEG(46.3 KDa)	Linear	L	None	Exendin-4 analogs	Antidiabetes	Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h.	1000 nmol/kg	34.91 ± 4.5 (T1/2 Elimination)	Hours	125676	Naïve mice plasma protease	fluorescence assay	Naïve mice plasma	In Vivo	None	None	EC50 (nM) = 2.7 ± 0.5
4278	36630826	2023	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Ex-POEGMAopt	39	Fluorescently labelled	Exendin-DBCO was conjugated to azide-functional POEGMA(54.7KDa)	Linear	L	None	Exendin-4 analogs	Antidiabetes	Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h.	1000 nmol/kg	97.3 ± 3.2 (T1/2 Elimination)	Hours	350280	Naïve mice plasma protease	fluorescence assay	Naïve mice plasma	In Vivo	None	None	EC50 (nM) = 2.8 ± 0.7
4281	36630826	2023	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Ex-POEGMAopt	39	Fluorescently labelled	Exendin-DBCO was conjugated to azide-functional POEGMA(54.7KDa)	Linear	L	None	Exendin-4 analogs	Antidiabetes	Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h.	1000 nmol/kg	105.7 ± 6 (T1/2 Elimination)	Hours	380520	Immunized mice plasma protease	fluorescence assay	Immunized mice plasma	In Vivo	None	None	EC50 (nM) = 2.8 ± 0.7
4302	EP 2022074607 W	2023	Y-Aib-EGTFISDLSI-Aib-KEEIHQ-Aib-EFIEWLLAQGPSSGAPPPS	SEQ ID NO 19	39	Free	Amidation	Linear	L	Aib = α-aminoisobutyric acid	Exendin-4 analogs	Antidiabetes	Blood samples were collected at 0 H and after 0.083, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, 48, 56, 72, 80, and 96 H post I.V. application	0.05 mg/kg	64.1	Hours	230760	Minipigs plasma protease	LC-MS	Minipigs plasma	In Vivo	None	EP 2022074607 W	IC50 hGIPR (nM) = 2
4307	EP 2023054305 W	2023	PSXFLSPTHSRVSSRKESKKPPAKLSPRK	SEQ ID NO 23	29	Free	Free	Linear	L	X = Octanoyl-Dpr at position 3	Human Ghrelin Analog	Ghrelin Receptor Agonist	Solutions were incubated at 37 C for 60, 120 and 180 Minutes	1 mg/ml	>58	Hours	208800	Plasma protease	LC-MS	Diluted plasma	In Vitro	None	EP 2023054305 W	EC50(nM) = 103
4308	EP 2023054305 W	2023	PSXFLSPYHSRVSSRKESKKPPAKLSPRK	SEQ ID NO 24	29	Free	Free	Linear	L	X = Octanoyl-Dpr at position 3	Human Ghrelin Analog	Ghrelin Receptor Agonist	Solutions were incubated at 37 C for 60, 120 and 180 Minutes	1 mg/ml	>58	Hours	208800	Plasma protease	LC-MS	Diluted plasma	In Vitro	None	EP 2023054305 W	EC50(nM) = 54.5
4310	EP 2023054305 W	2023	PXXFLSPTHSRVSSRKESKKPPAKLSPRK	SEQ ID NO 26	29	Free	Free	Linear	L	X = Octanoyl-Dpr at position 3, Deg = Di-ethyl glycine at position 2	Human Ghrelin Analog	Ghrelin Receptor Agonist	Solutions were incubated at 37 C for 60, 120 and 180 Minutes	1 mg/ml	>58	Hours	208800	Plasma protease	LC-MS	Diluted plasma	In Vitro	None	EP 2023054305 W	EC50(nM) = 138
4311	EP 2023054305 W	2023	PXXFLSPTHSRVSSRKESKKPPAKLSPRK	SEQ ID NO 27	29	Free	Free	Linear	L	X = Octanoyl-Dpr at position 3, Tie = L-te/t-butyl-glycine at position 2	Human Ghrelin Analog	Ghrelin Receptor Agonist	Solutions were incubated at 37 C for 60, 120 and 180 Minutes	1 mg/ml	>58	Hours	208800	Plasma protease	LC-MS	Diluted plasma	In Vitro	None	EP 2023054305 W	EC50(nM) = 61.8
4312	EP 2023054305 W	2023	PXXFLSPTHSRVSSRKESKKPPAKLSPRK	SEQ ID NO 28	29	Free	Free	Linear	L	X = Octanoyl-Dpr at position 3, Aib = 2-aminoisobutyric acid at position 2	Human Ghrelin Analog	Ghrelin Receptor Agonist	Solutions were incubated at 37 C for 60, 120 and 180 Minutes	1 mg/ml	>58	Hours	208800	Plasma protease	LC-MS	Diluted plasma	In Vitro	None	EP 2023054305 W	EC50(nM) = 72.4
4313	EP 2023054305 W	2023	PVXFLSPTHSRVSSRKESKKPPAKLSPRK	SEQ ID NO 29	29	Free	Free	Linear	L	X = Octanoyl-Dpr at position 3	Human Ghrelin Analog	Ghrelin Receptor Agonist	Solutions were incubated at 37 C for 60, 120 and 180 Minutes	1 mg/ml	>58	Hours	208800	Plasma protease	LC-MS	Diluted plasma	In Vitro	None	EP 2023054305 W	EC50(nM) = 36.6
4314	EP 2023054305 W	2023	PTXFLSPTHSRVSSRKESKKPPAKLSPRK	SEQ ID NO 30	29	Free	Free	Linear	L	X = Octanoyl-Dpr at position 3	Human Ghrelin Analog	Ghrelin Receptor Agonist	Solutions were incubated at 37 C for 60, 120 and 180 Minutes	1 mg/ml	>58	Hours	208800	Plasma protease	LC-MS	Diluted plasma	In Vitro	None	EP 2023054305 W	EC50(nM) = 56.5
4316	EP 2023054305 W	2023	SXFLSPTHSRVSSRKESKKPPAKLSPRK	SEQ ID NO 32	28	Free	Free	Linear	L	X = Octanoyl-Dpr at position 2	Human Ghrelin Analog	Ghrelin Receptor Agonist	Solutions were incubated at 37 C for 60, 120 and 180 Minutes	1 mg/ml	>58	Hours	208800	Plasma protease	LC-MS	Diluted plasma	In Vitro	None	EP 2023054305 W	EC50(nM) = 142
4317	EP 2023054305 W	2023	PSXXLSPYHSRVSSRKESKKPPAKLSPRK	SEQ ID NO 33	29	Free	Free	Linear	L	X = Octanoyl-Dpr at position 3, 1Nal = 3-(l-naphthyl)-L-alanine at position 4	Human Ghrelin Analog	Ghrelin Receptor Agonist	Solutions were incubated at 37 C for 60, 120 and 180 Minutes	1 mg/ml	>58	Hours	208800	Plasma protease	LC-MS	Diluted plasma	In Vitro	None	EP 2023054305 W	EC50(nM) = 61
4318	EP 2023054305 W	2023	PXXXLSPYHSRVSSRKESKKPPAKLSPRK	SEQ ID NO 34	29	Free	Free	Linear	L	NMeS = N- methyl-L-serineat position 2,X = Octanoyl-Dpr at position 3, Nal = 3-(l-naphthyl)-L-alanine at position 4	Human Ghrelin Analog	Ghrelin Receptor Agonist	Solutions were incubated at 37 C for 60, 120 and 180 Minutes	1 mg/ml	25	Hours	90000	Plasma protease	LC-MS	Diluted plasma	In Vitro	None	EP 2023054305 W	EC50(nM) = 27.2
4319	EP 2023054305 W	2023	PSXFLSPTHQRVSSRKESKKPPAKLSPRK	SEQ ID NO 35	29	Free	Free	Linear	L	X = Octanoyl-Dpr at position 3	Human Ghrelin Analog	Ghrelin Receptor Agonist	Solutions were incubated at 37 C for 60, 120 and 180 Minutes	1 mg/ml	63	Hours	226800	Plasma protease	LC-MS	Diluted plasma	In Vitro	None	EP 2023054305 W	EC50(nM) = 76.7
4320	EP 2023054305 W	2023	PSXFLSPTHSRVQSRKESKKPPAKLSPRK	SEQ ID NO 36	29	Free	Free	Linear	L	X = Octanoyl-Dpr at position 3	Human Ghrelin Analog	Ghrelin Receptor Agonist	Solutions were incubated at 37 C for 60, 120 and 180 Minutes	1 mg/ml	>58	Hours	208800	Plasma protease	LC-MS	Diluted plasma	In Vitro	None	EP 2023054305 W	EC50(nM) = 44.5
4321	EP 2023054305 W	2023	PSXFLSPTHSRVSQRKESKKPPAKLSPRK	SEQ ID NO 37	29	Free	Free	Linear	L	X = Octanoyl-Dpr at position 3	Human Ghrelin Analog	Ghrelin Receptor Agonist	Solutions were incubated at 37 C for 60, 120 and 180 Minutes	1 mg/ml	>58	Hours	208800	Plasma protease	LC-MS	Diluted plasma	In Vitro	None	EP 2023054305 W	EC50(nM) = 27.5
4322	EP 2023054305 W	2023	PSXFLSPTHSRVSSRKESKKPPAKLQPRK	SEQ ID NO 38	29	Free	Free	Linear	L	X = Octanoyl-Dpr at position 3	Human Ghrelin Analog	Ghrelin Receptor Agonist	Solutions were incubated at 37 C for 60, 120 and 180 Minutes	1 mg/ml	>58	Hours	208800	Plasma protease	LC-MS	Diluted plasma	In Vitro	None	EP 2023054305 W	EC50(nM) = 56.1
4323	EP 2023051315 W	2023	Y-Aib-EGTFTSDYSILLEEQAAREFIEWLLAGGPSKGAPPPS	Parent compound 1	39	Free	Free	Linear	L	Aib at position 2, Chem. 8 [2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	3 mg	104 (Terminal Half Life)	Hours	374400	Beagle dogs plasma protease	LC-MS	Beagle dogs plasma	In Vivo	None	EP 2023051315 W	hGLP-1R, CRE Luc 0% HSA EC50(pM) = 2.1
4324	EP 2023051315 W	2023	Y-Aib-EGTFTSDYSILLEEQAAREFIEWLLAGGPSKGAPPPS	Parent compound 3	39	Free	Free	Linear	L	Aib at position 2, Chem. 7 [(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(17-carboxyheptadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys33	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	2.9 mg	131 (Terminal Half Life)	Hours	471600	Beagle dogs plasma protease	LC-MS	Beagle dogs plasma	In Vivo	None	EP 2023051315 W	hGLP-1R, CRE Luc 0% HSA EC50(pM) = 4
4325	EP 2023051315 W	2023	Y-Aib-EGTFTSDYSILLEKQAAREFIEWLLAGGPSSGAPPPS	Parent compound 4	39	Free	Free	Linear	L	Aib at position 2, Chem. 7 [(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(17- carboxyheptadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys16	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	2.9 mg	56 (Terminal Half Life)	Hours	201600	Beagle dogs plasma protease	LC-MS	Beagle dogs plasma	In Vivo	None	EP 2023051315 W	hGLP-1R, CRE Luc 0% HSA EC50(pM) = 4.2
4326	EP 2023051315 W	2023	Y-Aib-EGTFTSDYSI-Aib-LDKIAQKAFVQWLIAGGPSSGAPPPS	Parent compound 5	39	Free	Amidation	Linear	L	Aib at position 2 and 13, Chem.16[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(19- carboxynonadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	3 mg	134 (Terminal Half Life)	Hours	482400	Beagle dogs plasma protease	LC-MS	Beagle dogs plasma	In Vivo	None	EP 2023051315 W	hGLP-1R, CRE Luc 0% HSA EC50(pM) = 9.7
4327	EP 2023051315 W	2023	KVY-Aib-EGTFTSDYSILLEEQAAREFIEWLLAGGPSKGAPPPS	Non-converting compound 1	41	Lys side chain conatins Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1	Free	Linear	L	Aib at position 4, Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	2.8 mg	137 (Terminal Half Life)	Hours	493200	Beagle dogs plasma protease	LC-MS	Beagle dogs plasma	In Vivo	None	EP 2023051315 W	N.A.
4328	EP 2023051315 W	2023	KVY-Aib-EGTFTSDYSILLEEQAAREFIEWLLAGGPSKGAPPPS	Non-converting compound 2	41	Lys side chain conatins Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1	Free	Linear	L	Aib at position 4,Chem. 10[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4- carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys33	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	3.5 mg	130 (Terminal Half Life)	Hours	468000	Beagle dogs plasma protease	LC-MS	Beagle dogs plasma	In Vivo	None	EP 2023051315 W	N.A.
4329	EP 2023051315 W	2023	KVY-Aib-EGTFTSDYSILLEKQAAREFIEWLLAGGPSSGAPPPS	Non-converting compound 3	41	Lys side chain conatins Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1 ,	Free	Linear	L	Aib at position 4,Chem. 7[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(17-carboxyheptadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys 16	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	3 mg	115 (Terminal Half Life)	Hours	414000	Beagle dogs plasma protease	LC-MS	Beagle dogs plasma	In Vivo	None	EP 2023051315 W	N.A.
4330	EP 2023051315 W	2023	KVY-Aib-EGTFTSDYSI-Aib-LDKIAQKAFVQWLIAGGPSSGAPPPS	Non-converting compound 4	41	Lys side chain conatins Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl attached to Lys1	Amidation	Linear	L	Aib at position 4,Chem. 11[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(19-carboxynonadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys20	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	3 mg	136 (Terminal Half Life)	Hours	489600	Beagle dogs plasma protease	LC-MS	Beagle dogs plasma	In Vivo	None	EP 2023051315 W	N.A.
4331	EP 2023051315 W	2023	k-Sar-Y-Aib-EGTFTSDYSILLEEQAAREFIEWLLAGGPSKGAPPPS	Compound 1	41	D-Lys conjugated with [(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl]	Free	Linear	Mix	Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33 , Sar2, Aib modifications	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	3.1 mg	146 (Terminal Half Life)	Hours	525600	Beagle dogs plasma protease	LC-MS	Beagle dogs plasma	In Vivo	None	EP 2023051315 W	N.A.
4332	EP 2023051315 W	2023	G-Aeg-Y-Aib-EGTFTSDYSILLEEQAAREFIEWLLAGGPSKGAPPPS	Compound 2	41	Free	Free	Linear	L	Aeg = N-(2-aminoethyl)glycine, Chem.16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Aeg2, Chem.8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl] attached to Lys33	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	2.9 mg	142 (Terminal Half Life)	Hours	511200	Beagle dogs plasma protease	LC-MS	Beagle dogs plasma	In Vivo	None	EP 2023051315 W	N.A.
4333	EP 2023051315 W	2023	K-Sar-Y-Aib-EGTFTSDYSILLEEQAAREFIEWLLAGGPSKGAPPPS	Compound 3	41	Chem. 16 [(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1	Free	Linear	L	Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33, Sar2 modification	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	3 mg	139 (Terminal Half Life)	Hours	500400	Beagle dogs plasma protease	LC-MS	Beagle dogs plasma	In Vivo	None	EP 2023051315 W	N.A.
4334	EP 2023051315 W	2023	L-Aeg-Y-Aib-EGTFTSDYSILLEEQAAREFIEWLLAGGPSKGAPPPS	Compound 5	41	Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to L-Aeg	Free	Linear	L	Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	2.8 mg	106 (Terminal Half Life)	Hours	381600	Beagle dogs plasma protease	LC-MS	Beagle dogs plasma	In Vivo	None	EP 2023051315 W	N.A.
4335	EP 2023051315 W	2023	K-Sar-Y-Aib-EGTFTSDYSILLEEQAAREFIEWLLAGGPSKGAPPPS	Compound 12	41	Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1	Free	Linear	L	Chem. 10[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4- carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys33, Sar2 modfications	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	2.7 mg	143 (Terminal Half Life)	Hours	514800	Beagle dogs plasma protease	LC-MS	Beagle dogs plasma	In Vivo	None	EP 2023051315 W	N.A.
4336	EP 2023051315 W	2023	K-Sar-Y-Aib-EGTFTSDYSILLEEQAAREFIEWLLAGGPSKGAPPPS	Compound 13	41	Chem. 17[(4S)-4-carboxy-4-(17-carboxyheptadecanoylamino)butanoyl] attached to Lys1	Free	Linear	L	Chem. 10[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4- carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys33, Sar2 modifications	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	2.8 mg	121 (Terminal Half Life)	Hours	435600	Beagle dogs plasma protease	LC-MS	Beagle dogs plasma	In Vivo	None	EP 2023051315 W	N.A.
4337	EP 2023051315 W	2023	K-Sar-Y-Aib-EGTFTSDYSILLEEQAAREFIEWLLAGGPSKGAPPPS	Compound 14	41	Chem. 22[(2S)-2,6-bis[[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]hexanoyl] attached to Lys1	Free	Linear	L	Chem. 10[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys33, Sar2 modifications	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	3.2 mg	119 (Terminal Half Life)	Hours	428400	Beagle dogs plasma protease	LC-MS	Beagle dogs plasma	In Vivo	None	EP 2023051315 W	N.A.
4338	EP 2023051315 W	2023	K-Sar-Y-Aib-EGTFTSDYSILLEEQAAREFIEWLLAGGPSKGAPPPS	Compound 15	41	Chem. 17[(4S)-4-carboxy-4-(17-carboxyheptadecanoylamino)butanoyl] attached to Lys1	Free	Linear	L	Chem. 7[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4- carboxy-4-(17-carboxyheptadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys33, Sar2 modifications	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	2 mg	124 (Terminal Half Life)	Hours	446400	Beagle dogs plasma protease	LC-MS	Beagle dogs plasma	In Vivo	None	EP 2023051315 W	N.A.
4339	EP 2023051315 W	2023	K-Sar-Y-Aib-EGTFTSDYSILLEKQAAREFIEWLLAGGPSSGAPPPS	Compound 16	41	Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1	Free	Linear	L	Chem. 7[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(17- carboxyheptadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys 16, Sar2 modifications	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	2.9 mg	96 (Terminal Half Life)	Hours	345600	Beagle dogs plasma protease	LC-MS	Beagle dogs plasma	In Vivo	None	EP 2023051315 W	N.A.
4340	EP 2023051315 W	2023	G-Aeg-Y-Aib-EGTFTSDYSILLEKQAAREFIEWLLAGGPSSGAPPPS	Compound 17	41	Chem. 16 [(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to G-Aeg	Free	Linear	L	Chem.7[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(17- carboxyheptadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys16, Aib modifications	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	3.2 mg	105 (Terminal Half Life)	Hours	378000	Beagle dogs plasma protease	LC-MS	Beagle dogs plasma	In Vivo	None	EP 2023051315 W	N.A.
4341	EP 2023051315 W	2023	K-Sar-Y-Aib-EGTFTSDYSI-Aib-LDKIAQKAFVQWLIAGGPSSGAPPPS	Compound 18	41	Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1	Amidation	Linear	L	Chem.11 [2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(19- carboxynonadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys20, Sar2 modification	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	2.9 mg	88 (Terminal Half Life)	Hours	316800	Beagle dogs plasma protease	LC-MS	Beagle dogs plasma	In Vivo	None	EP 2023051315 W	N.A.
4342	EP 2023051315 W	2023	Y-Aib-EGTFTSDYSILLEEQAAREFIEWLLAGGPSKGAPPPS	Parent compound 1	39	Free	Free	Linear	L	Aib at position 2, Chem. 8 [2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	2 nmol/kg	121 (Terminal Half Life)	Hours	435600	Minipigs plasma protease	ELISA or similar antibody based assay or LC-MS	Minipigs plasma	In Vivo	None	EP 2023051315 W	hGLP-1R, CRE Luc 0% HSA EC50(pM) = 2.1
4343	EP 2023051315 W	2023	Y-Aib-EGTFTSDYSILLEEQAAREFIEWLLAGGPSKGAPPPS	Parent compound 2	39	Free	Free	Linear	L	Aib at position 2, Chem. 10[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl attached to Lys33	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	1 nmol/kg	104 (Terminal Half Life)	Hours	374400	Minipigs plasma protease	ELISA or similar antibody based assay or LC-MS	Minipigs plasma	In Vivo	None	EP 2023051315 W	hGLP-1R, CRE Luc 0% HSA EC50(pM) = 1.5
4344	EP 2023051315 W	2023	Y-Aib-EGTFTSDYSILLEKQAAREFIEWLLAGGPSSGAPPPS	Parent compound 4	39	Free	Free	Linear	L	Aib at position 2, Chem. 7 [(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(17- carboxyheptadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys16	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	1 nmol/kg	106 (Terminal Half Life)	Hours	381600	Minipigs plasma protease	ELISA or similar antibody based assay or LC-MS	Minipigs plasma	In Vivo	None	EP 2023051315 W	hGLP-1R, CRE Luc 0% HSA EC50(pM) = 4.2
4345	EP 2023051315 W	2023	KVY-Aib-EGTFTSDYSILLEEQAAREFIEWLLAGGPSKGAPPPS	Non-converting compound 1	41	Lys side chain conatins Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1	Free	Linear	L	Aib at position 4, Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	2 nmol/kg	170 (Terminal Half Life)	Hours	612000	Minipigs plasma protease	ELISA or similar antibody based assay or LC-MS	Minipigs plasma	In Vivo	None	EP 2023051315 W	N.A.
4346	EP 2023051315 W	2023	k-Sar-Y-Aib-EGTFTSDYSILLEEQAAREFIEWLLAGGPSKGAPPPS	Compound 1	41	D-Lys conjugated with [(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl]	Free	Linear	Mix	Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33 , Sar2 modification	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	20 nmol/kg	118 (Terminal Half Life)	Hours	424800	Minipigs plasma protease	ELISA or similar antibody based assay or LC-MS	Minipigs plasma	In Vivo	None	EP 2023051315 W	N.A.
4347	EP 2023051315 W	2023	K-Sar-Y-Aib-EGTFTSDYSILLEEQAAREFIEWLLAGGPSKGAPPPS	Compound 3	41	Chem. 16 [(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1	Free	Linear	L	Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33, Sar2 modifications	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	2 nmol/kg	119 (Terminal Half Life)	Hours	428400	Minipigs plasma protease	ELISA or similar antibody based assay or LC-MS	Minipigs plasma	In Vivo	None	EP 2023051315 W	N.A.
4348	EP 2023051315 W	2023	K-Sar-Y-Aib-EGTFTSDYSILLEEQAAREFIEWLLAGGPSKGAPPPS	Compound 9	41	Chem. 19[2-[[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]acetyl] attached to Lys1	Free	Linear	L	Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33, Sar2 modifications	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	20 nmol/kg	102 (Terminal Half Life)	Hours	367200	Minipigs plasma protease	ELISA or similar antibody based assay or LC-MS	Minipigs plasma	In Vivo	None	EP 2023051315 W	N.A.
4349	EP 2023051315 W	2023	k-Sar-Y-Aib-EGTFTSDYSILLEEQAAREFIEWLLAGGPSKGAPPPS	Compound 10	41	Chem. 21[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to D-Lys1	Free	Linear	Mix	Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4- carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33	Synthetic	GLP-1/GIP receptor co-agonist	N.A.	20 nmol/kg	118 (Terminal Half Life)	Hours	424800	Minipigs plasma protease	ELISA or similar antibody based assay or LC-MS	Minipigs plasma	In Vivo	None	EP 2023051315 W	N.A.
4350	EP 2023066180 W	2023	EVQLLESGGGLVQPGGSLRLSCAASGFTFRSFGMSWVRQAPGKGPEWVSSISGSGSDTLYADSVKGRFTISRDNSKNTLYLQMNSLRPEDTAVYYCTIGGSLSRSSQGTLVTVSSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLYITREPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALKFHYTQKSLSLSPG	TA-Alb23-Fc-ABDEG	341	Alb23 fused at the N-termini of both Fc domains of efgartigimod	Free	Linear	L	None	Synthetic	FcRN Antagonist	Blood sample were collected for Pk Measurement Ar : Test Day 1 (Td1)(Pre-Dosing), Td1(Prior To Dosing), Td1(5 Min), Td2(24 Hrs Post Dosing), Td3, Td4, Td6, Td8, Td11, Td15, Td18, Td22, Td29, Td36 And Td43	20 mg/kg	27	Days	2332800	Cynomolgus monkeys serum protease	Sandwich ELISA	Cynomolgus monkeys serum	In Vivo	None	EP 2023066180 W	N.A.
4351	EP 2023066180 W	2023	EVQLLESGGGLVQPGGSLRLSCAASGFTFRSFGMSWVRQAPGKGPEWVSSISGSGSDTLYADSVKGRFTISRDNSKNTLYLQMNSLRPEDTAVYYCTIGGSLSRSSQGTLVTVSSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLYITREPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALKFHYTQKSLSLSPG	TA-Alb23-Fc-ABDEG	341	Alb23 fused at the N-termini of both Fc domains of efgartigimod	Free	Linear	L	None	Synthetic	FcRN Antagonist	Blood sample were collected for PK measurement Ar : Test Day 1 (Td1)(Pre-Dosing), Td1(Prior To Dosing), Td1(5 Min), Td2(24 Hrs Post Dosing), Td3, Td4, Td6, Td8, Td11, Td15, Td18, Td22, Td29, Td36 And Td43	5 mg/kg	28 ± 23	Days	2419200	Cynomolgus monkeys serum protease	Sandwich ELISA	Cynomolgus monkeys serum	In Vivo	None	EP 2023066180 W	N.A.
4352	EP 2023066180 W	2023	EVQLLESGGGLVQPGGSLRLSCAASGFTFRSFGMSWVRQAPGKGPEWVSSISGSGSDTLYADSVKGRFTISRDNSKNTLYLQMNSLRPEDTAVYYCTIGGSLSRSSQGTLVTVSSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLYITREPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALKFHYTQKSLSLSPG	TA-Alb23-Fc-ABDEG	341	Alb23 fused at the N-termini of both Fc domains of efgartigimod	Free	Linear	L	None	Synthetic	FcRN Antagonist	Blood sample were collected for PK measurement Ar : Test Day 1 (Td1)(Pre-Dosing), Td1(Prior To Dosing), Td1(5 Min), Td2(24 Hrs Post Dosing), Td3, Td4, Td6, Td8, Td11, Td15, Td18, Td22, Td29, Td36 And Td43	20 mg/kg	26.5	Days	2289600	C2 Cynomolgus monkeys serum protease	Sandwich ELISA	C2 Cynomolgus monkeys serum	In Vivo	None	EP 2023066180 W	N.A.
4353	EP 2023066180 W	2023	EVQLLESGGGLVQPGGSLRLSCAASGFTFRSFGMSWVRQAPGKGPEWVSSISGSGSDTLYADSVKGRFTISRDNSKNTLYLQMNSLRPEDTAVYYCTIGGSLSRSSQGTLVTVSSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLYITREPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALKFHYTQKSLSLSPG	TA-Alb23-Fc-ABDEG	341	Alb23 fused at the N-termini of both Fc domains of efgartigimod	Free	Linear	L	None	Synthetic	FcRN Antagonist	Blood sample were collected for PK Measurement Ar : Test Day 1 (Td1)(Pre-Dosing), Td1(Prior To Dosing), Td1(5 Min), Td2(24 Hrs Post Dosing), Td3, Td4, Td6, Td8, Td11, Td15, Td18, Td22, Td29, Td36 And Td43	5 mg/kg	13.4	Days	1157760	C4 Cynomolgus monkeys serum protease	Sandwich ELISA	C4 Cynomolgus monkeys serum	In Vivo	None	EP 2023066180 W	N.A.
4354	EP 2023066180 W	2023	EVQLLESGGGLVQPGGSLRLSCAASGFTFRSFGMSWVRQAPGKGPEWVSSISGSGSDTLYADSVKGRFTISRDNSKNTLYLQMNSLRPEDTAVYYCTIGGSLSRSSQGTLVTVSSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLYITREPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALKFHYTQKSLSLSPG	TA-Alb23-Fc-ABDEG	341	Alb23 fused at the N-termini of both Fc domains of efgartigimod	Free	Linear	L	None	Synthetic	FcRN Antagonist	Blood sample were collected for PK measurement Ar : Test Day 1 (Td1)(Pre-Dosing), Td1(Prior To Dosing), Td1(5 Min), Td2(24 Hrs Post Dosing), Td3, Td4, Td6, Td8, Td11, Td15, Td18, Td22, Td29, Td36 And Td43	5 mg/kg	54.4	Days	4700160	C5 Cynomolgus monkeys serum protease	Sandwich ELISA	C5 Cynomolgus monkeys serum	In Vivo	None	EP 2023066180 W	N.A.
4355	EP 2023066180 W	2023	EVQLLESGGGLVQPGGSLRLSCAASGFTFRSFGMSWVRQAPGKGPEWVSSISGSGSDTLYADSVKGRFTISRDNSKNTLYLQMNSLRPEDTAVYYCTIGGSLSRSSQGTLVTVSSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLYITREPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALKFHYTQKSLSLSPG	TA-Alb23-Fc-ABDEG	341	Alb23 fused at the N-termini of both Fc domains of efgartigimod	Free	Linear	L	None	Synthetic	FcRN Antagonist	Blood sample were collected for PK Measurement Ar : Test Day 1 (Td1)(Pre-Dosing), Td1(Prior To Dosing), Td1(5 Min), Td2(24 Hrs Post Dosing), Td3, Td4, Td6, Td8, Td11, Td15, Td18, Td22, Td29, Td36 And Td43	5 mg/kg	16.9	Days	1460160	C6 Cynomolgus monkeys serum protease	Sandwich ELISA	C6 Cynomolgus monkeys serum	In Vivo	None	EP 2023066180 W	N.A.
4356	EP 2023066180 W	2023	DKTHTCPPCPAPELLGGPSVFLFPPKPKDTLYITREPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALKFHYTQKSLSLSPGGGGGSGGGGSGGGGSGGGGSEVQLLESGGGLVQPGGSLRLSCAASGFTFRSFGMSWVRQAPGKGPEWVSSISGSGSDTLYADSVKGRFTISRDNSKNTLYLQMNSLRPEDTAVYYCTIGGSLSRSSQGTLVTVSS	TA-Fc-ABDEG-Alb23	361	Free	Alb23 fused at the C-termini of both Fc domains of ABDEG via a 20GS linker	Linear	L	None	Synthetic	FcRN Antagonist	N.A.	30 mg/kg	15	Days	1296000	G1-1 Cynomolgus monkeys serum protease	Sandwich ELISA	G1-1 Cynomolgus monkeys serum	In Vivo	None	EP 2023066180 W	N.A.
4357	EP 2023066180 W	2023	DKTHTCPPCPAPELLGGPSVFLFPPKPKDTLYITREPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALKFHYTQKSLSLSPGGGGGSGGGGSGGGGSGGGGSEVQLLESGGGLVQPGGSLRLSCAASGFTFRSFGMSWVRQAPGKGPEWVSSISGSGSDTLYADSVKGRFTISRDNSKNTLYLQMNSLRPEDTAVYYCTIGGSLSRSSQGTLVTVSS	TA-Fc-ABDEG-Alb23	361	Free	Alb23 fused at the C-termini of both Fc domains of ABDEG via a 20GS linker	Linear	L	None	Synthetic	FcRN Antagonist	N.A.	30 mg/kg	9.3	Days	803520	G1-2 Cynomolgus monkeys serum protease	Sandwich ELISA	G1-2 Cynomolgus monkeys serum	In Vivo	None	EP 2023066180 W	N.A.
4358	EP 2023066180 W	2023	DKTHTCPPCPAPELLGGPSVFLFPPKPKDTLYITREPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALKFHYTQKSLSLSPGGGGGSGGGGSGGGGSGGGGSEVQLLESGGGLVQPGGSLRLSCAASGFTFRSFGMSWVRQAPGKGPEWVSSISGSGSDTLYADSVKGRFTISRDNSKNTLYLQMNSLRPEDTAVYYCTIGGSLSRSSQGTLVTVSS	TA-Fc-ABDEG-Alb23	361	Free	Alb23 fused at the C-termini of both Fc domains of ABDEG via a 20GS linker	Linear	L	None	Synthetic	FcRN Antagonist	N.A.	30 mg/kg	4.5	Days	388800	G1-3 Cynomolgus monkeys serum protease	Sandwich ELISA	G1-3 Cynomolgus monkeys serum	In Vivo	None	EP 2023066180 W	N.A.
4359	EP 2023066180 W	2023	DKTHTCPPCPAPELLGGPSVFLFPPKPKDTLYITREPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALKFHYTQKSLSLSPGGGGGSGGGGSGGGGSGGGGSEVQLLESGGGLVQPGGSLRLSCAASGFTFRSFGMSWVRQAPGKGPEWVSSISGSGSDTLYADSVKGRFTISRDNSKNTLYLQMNSLRPEDTAVYYCTIGGSLSRSSQGTLVTVSS	TA-Fc-ABDEG-Alb23	361	Free	Alb23 fused at the C-termini of both Fc domains of ABDEG via a 20GS linker	Linear	L	None	Synthetic	FcRN Antagonist	N.A.	75 mg/kg	13	Days	1123200	G2-1 Cynomolgus monkeys serum protease	Sandwich ELISA	G2-1 Cynomolgus monkeys serum	In Vivo	None	EP 2023066180 W	N.A.
4360	EP 2023066180 W	2023	DKTHTCPPCPAPELLGGPSVFLFPPKPKDTLYITREPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALKFHYTQKSLSLSPGGGGGSGGGGSGGGGSGGGGSEVQLLESGGGLVQPGGSLRLSCAASGFTFRSFGMSWVRQAPGKGPEWVSSISGSGSDTLYADSVKGRFTISRDNSKNTLYLQMNSLRPEDTAVYYCTIGGSLSRSSQGTLVTVSS	TA-Fc-ABDEG-Alb23	361	Free	Alb23 fused at the C-termini of both Fc domains of ABDEG via a 20GS linker	Linear	L	None	Synthetic	Fcrn Antagonist	N.A.	75 mg/kg	6.1	Days	527040	G2-2 Cynomolgus monkeys serum protease	Sandwich ELISA	G2-2 Cynomolgus monkeys serum	In Vivo	None	EP 2023066180 W	N.A.
4361	EP 2023066180 W	2023	DKTHTCPPCPAPELLGGPSVFLFPPKPKDTLYITREPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALKFHYTQKSLSLSPGGGGGSGGGGSGGGGSGGGGSEVQLLESGGGLVQPGGSLRLSCAASGFTFRSFGMSWVRQAPGKGPEWVSSISGSGSDTLYADSVKGRFTISRDNSKNTLYLQMNSLRPEDTAVYYCTIGGSLSRSSQGTLVTVSS	TA-Fc-ABDEG-Alb23	361	Free	Alb23 fused at the C-termini of both Fc domains of ABDEG via a 20GS linker	Linear	L	None	Synthetic	Fcrn Antagonist	N.A.	75 mg/kg	12	Days	1036800	G2-3 Cynomolgus monkeys serum protease	Sandwich ELISA	G2-3 Cynomolgus monkeys serum	In Vivo	None	EP 2023066180 W	N.A.
4362	EP 2023053030 W	2023	AEAKYAKEAVEALVEIWTLPNLTREQWQAFIYKLRDDPSQSSELLSEAKKLNDSQAPKASGSLAEAKEAANAELDSYGVSDFYKRLIDKAKTVEGVEALKDAILAALP	ZTPA001	108	Free	ABD (albumin Binding Domain)	Linear	L	None	Tslp Binding Z Variants	Antiinflammatory	Blood samples (0.5 mL) were collected at the following time points: Predose, At 10 And 30 Min And 1 , 6, 10, 26, 50, 72, And 96 H Postdose And At Days 6, 7, 8, 11 , 13, 15, 18, And 22	1.33 mg/kg	3-4 (Terminal Half Life)	Days	259200	Cynomolgus monkeys serum protease	Sandwich PK-ELISA	Cynomolgus monkeys serum	In Vivo	None	EP 2023053030 W	IC50(nM) = 0.5
4363	EP 2023053030 W	2023	GSLAEAKEAANAELDSYGVSDFYKRLIDKAKTVEGVEALKDAILAALPGGGGSAEAKYAKEAVEALVEIWTLPNLTREQWQAFIYKLRDDPSQSSELLSEAKKLNDSQAPK	ZTPA104	111	ABD (albumin Binding Domain)	Free	Linear	L	None	Tslp Binding Z Variants	Antiinflammatory	Blood sampling time points were divided into two cohorts as follows: Cohort A (N=3 Per Test Item) Were Bled Predose, At 5 Min And 1 , 8, 72, 168, 264, 408 And 504 H Postdose; And Cohort B (N=3 Per Test Item) Were Bled Predose, At 30 Min And 3, 24, 120, 216, 336 And 456 H Postdose	1.2 mg/kg	36 (Terminal Half Life)	Hours	129600	SD rats serum protease	ELISA	SD rats serum	In Vivo	None	EP 2023053030 W	IC50(nM) = 0.03
4364	EP 2023053030 W	2023	AEAKYAKEAVEALVEIWTLPNLTREQWQAFIYKLRDDPSQSSELLSEAKKLNDSQAPKASGSLAEAKEAANAELDSYGVSDFYKRLIDKAKTVEGVEALKDAILAALP	ZTPA001	108	Free	ABD (albumin Binding Domain)	Linear	L	None	Tslp Binding Z Variants	Antiinflammatory	Blood sampling time points were divided into two cohorts as follows: Cohort A (N=3 Per Test Item) Were Bled Predose, At 5 Min And 1 , 8, 72, 168, 264, 408 And 504 H Postdose; And Cohort B (N=3 Per Test Item) Were Bled Predose, At 30 Min And 3, 24, 120, 216, 336 And 456 H Postdose	1.2 mg/kg	29 (Terminal Half Life)	Hours	104400	SD rats serum protease	ELISA	SD rats serum	In Vivo	None	EP 2023053030 W	IC50(nM) = 0.5
4378	36997003	2023	Y-Aib-QGTFTSDYSKYLDERRAKEFVQWLMNTC	HM15136	30	IgG Fc linked at N terminus through MAL-PEG-ALD linker	Free	Cyclic (lactam bridge between E16-K20)	L	Aib2 modification	Synthetic	Treatment of Hyperinsulinemic Hypoglycemia	Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration	260 μg/kg	54.5	Hours	196200	Mouse serum protease	Modified ELISA	Mouse serum	In Vivo	https://www.nature.com/articles/s41598-022-21251-y	None	EC50 of HM15136 was 0.024 ± 0.006 nM while that of native glucagon was 0.003 ± 0.001 nM for hGCGR
4379	36997003	2023	Y-Aib-QGTFTSDYSKYLDERRAKEFVQWLMNTC	HM15136	30	IgG Fc linked at N terminus through MAL-PEG-ALD linker	Free	Cyclic (lactam bridge between E16-K20)	L	Aib2 modification	Synthetic	Treatment of Hyperinsulinemic Hypoglycemia	Blood (0.3 mL) was collected from the retro-orbital plexus at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration	260 μg/kg	32.3	Hours	116280	Mouse serum protease	Modified ELISA	Mouse serum	In Vivo	https://www.nature.com/articles/s41598-022-21251-y	None	EC50 of HM15136 was 0.024 ± 0.006 nM while that of native glucagon was 0.003 ± 0.001 nM for hGCGR
4380	36997003	2023	Y-Aib-QGTFTSDYSKYLDERRAKEFVQWLMNTC	HM15136	30	IgG Fc linked at N terminus through MAL-PEG-ALD linker	Free	Cyclic (lactam bridge between E16-K20)	L	Aib2 modification	Synthetic	Treatment of Hyperinsulinemic Hypoglycemia	Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration	260 μg/kg	66.4 ± 33.0	Hours	239040	Rats serum protease	Modified ELISA	Rats serum	In Vivo	https://www.nature.com/articles/s41598-022-21251-y	None	EC50 of HM15136 was 0.024 ± 0.006 nM while that of native glucagon was 0.003 ± 0.001 nM for hGCGR
4381	36997003	2023	Y-Aib-QGTFTSDYSKYLDERRAKEFVQWLMNTC	HM15136	30	IgG Fc linked at N terminus through MAL-PEG-ALD linker	Free	Cyclic (lactam bridge between E16-K20)	L	Aib2 modification	Synthetic	Treatment of Hyperinsulinemic Hypoglycemia	Blood (0.3 mL) was collected from the retro-orbital plexus at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration	260 μg/kg	40.9 ± 17.7	Hours	147240	Rats serum protease	Modified ELISA	Rats serum	In Vivo	https://www.nature.com/articles/s41598-022-21251-y	None	EC50 of HM15136 was 0.024 ± 0.006 nM while that of native glucagon was 0.003 ± 0.001 nM for hGCGR
4382	36997003	2023	Y-Aib-QGTFTSDYSKYLDERRAKEFVQWLMNTC	HM15136	30	IgG Fc linked at N terminus through MAL-PEG-ALD linker	Free	Cyclic (lactam bridge between E16-K20)	L	Aib2 modification	Synthetic	Treatment of Hyperinsulinemic Hypoglycemia	Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration	52 μg/kg	24.9 ± 2.2	Hours	89640	Dogs serum protease	Modified ELISA	Dogs serum	In Vivo	https://www.nature.com/articles/s41598-022-21251-y	None	EC50 of HM15136 was 0.024 ± 0.006 nM while that of native glucagon was 0.003 ± 0.001 nM for hGCGR
4383	36997003	2023	Y-Aib-QGTFTSDYSKYLDERRAKEFVQWLMNTC	HM15136	30	IgG Fc linked at N terminus through MAL-PEG-ALD linker	Free	Cyclic (lactam bridge between E16-K20)	L	Aib2 modification	Synthetic	Treatment of Hyperinsulinemic Hypoglycemia	Blood (0.3 mL) was collected from the retro-orbital plexus at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration	52 μg/kg	26.6 ± 1.5	Hours	95760	Dogs serum protease	Modified ELISA	Dogs serum	In Vivo	https://www.nature.com/articles/s41598-022-21251-y	None	EC50 of HM15136 was 0.024 ± 0.006 nM while that of native glucagon was 0.003 ± 0.001 nM for hGCGR
4389	36997003	2023	Y-Aib-QGTFTSDYSKYLDERRAKEFVQWLMNTCLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTFPPSQEEMTKNQVSLRCLVKGFYPSDIAVEWESNGQPENNYKTTKPVLDSDGSFRLESRLTVDKSRWQEGNVFSCSVMHEALHNHYTQKSLSLS	HM15136	240	Free	HMC001	Cyclic (E36-K40 lactam bridge in GCG analog)	L	Aib, GC15136 and HMC001 are linked via a 10-kDa, bifunctional maleimide-polyethylene glycol-aldehyde (MAL-PEG-ALD) linker	Glucagon analog	Treatment of Congenital Hyperinsulinism	Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration and at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration of HM15136	260 μg/kg	54.5	Hours	196200	Mouse serum protease	ELISA	Mouse serum	In Vivo	PDB id: 5HVW, https://pubmed.ncbi.nlm.nih.gov/36202918/	None	KD (HM15136) = No binding for FcγRIA, FcγRIIA, FcγRIIB/C, FcγRIIIA, FcγRIIIB, C1q
4390	36997003	2023	Y-Aib-QGTFTSDYSKYLDERRAKEFVQWLMNTCLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTFPPSQEEMTKNQVSLRCLVKGFYPSDIAVEWESNGQPENNYKTTKPVLDSDGSFRLESRLTVDKSRWQEGNVFSCSVMHEALHNHYTQKSLSLS	HM15136	240	Free	HMC001	Cyclic (E36-K40 lactam bridge in GCG analog)	L	Aib, GC15136 and HMC001 are linked via a 10-kDa, bifunctional maleimide-polyethylene glycol-aldehyde (MAL-PEG-ALD) linker	Glucagon analog	Treatment of Congenital Hyperinsulinism	Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration and at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration of HM15136	260 μg/kg	32.3	Hours	116280	Mouse serum protease	ELISA	Mouse serum	In Vivo	PDB id: 5HVW, https://pubmed.ncbi.nlm.nih.gov/36202918/	None	KD (HM15136) = No binding for FcγRIA, FcγRIIA, FcγRIIB/C, FcγRIIIA, FcγRIIIB, C1q
4391	36997003	2023	Y-Aib-QGTFTSDYSKYLDERRAKEFVQWLMNTCLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTFPPSQEEMTKNQVSLRCLVKGFYPSDIAVEWESNGQPENNYKTTKPVLDSDGSFRLESRLTVDKSRWQEGNVFSCSVMHEALHNHYTQKSLSLS	HM15136	240	Free	HMC001	Cyclic (E36-K40 lactam bridge in GCG analog)	L	Aib, GC15136 and HMC001 are linked via a 10-kDa, bifunctional maleimide-polyethylene glycol-aldehyde (MAL-PEG-ALD) linker	Glucagon analog	Treatment of Congenital Hyperinsulinism	Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration and at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration of HM15136	260 μg/kg	66.4 ± 33.0	Hours	239040	Rats serum protease	ELISA	Rats serum	In Vivo	PDB id: 5HVW, https://pubmed.ncbi.nlm.nih.gov/36202918/	None	KD (HM15136) = No binding for FcγRIA, FcγRIIA, FcγRIIB/C, FcγRIIIA, FcγRIIIB, C1q
4392	36997003	2023	Y-Aib-QGTFTSDYSKYLDERRAKEFVQWLMNTCLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTFPPSQEEMTKNQVSLRCLVKGFYPSDIAVEWESNGQPENNYKTTKPVLDSDGSFRLESRLTVDKSRWQEGNVFSCSVMHEALHNHYTQKSLSLS	HM15136	240	Free	HMC001	Cyclic (E36-K40 lactam bridge in GCG analog)	L	Aib, GC15136 and HMC001 are linked via a 10-kDa, bifunctional maleimide-polyethylene glycol-aldehyde (MAL-PEG-ALD) linker	Glucagon analog	Treatment of Congenital Hyperinsulinism	Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration and at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration of HM15136	260 μg/kg	40.9 ± 17.7	Hours	147240	Rats serum protease	ELISA	Rats serum	In Vivo	PDB id: 5HVW, https://pubmed.ncbi.nlm.nih.gov/36202918/	None	KD (HM15136) = No binding for FcγRIA, FcγRIIA, FcγRIIB/C, FcγRIIIA, FcγRIIIB, C1q
4393	36997003	2023	Y-Aib-QGTFTSDYSKYLDERRAKEFVQWLMNTCLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTFPPSQEEMTKNQVSLRCLVKGFYPSDIAVEWESNGQPENNYKTTKPVLDSDGSFRLESRLTVDKSRWQEGNVFSCSVMHEALHNHYTQKSLSLS	HM15136	240	Free	HMC001	Cyclic (E36-K40 lactam bridge in GCG analog)	L	Aib, GC15136 and HMC001 are linked via a 10-kDa, bifunctional maleimide-polyethylene glycol-aldehyde (MAL-PEG-ALD) linker	Glucagon analog	Treatment of Congenital Hyperinsulinism	Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration and at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration of HM15136	52 μg/kg	24.9 ± 2.2	Hours	89640	Dogs serum protease	ELISA	Dogs serum	In Vivo	PDB id: 5HVW, https://pubmed.ncbi.nlm.nih.gov/36202918/	None	KD (HM15136) = No binding for FcγRIA, FcγRIIA, FcγRIIB/C, FcγRIIIA, FcγRIIIB, C1q
4394	36997003	2023	Y-Aib-QGTFTSDYSKYLDERRAKEFVQWLMNTCLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTFPPSQEEMTKNQVSLRCLVKGFYPSDIAVEWESNGQPENNYKTTKPVLDSDGSFRLESRLTVDKSRWQEGNVFSCSVMHEALHNHYTQKSLSLS	HM15136	240	Free	HMC001	Cyclic (E36-K40 lactam bridge in GCG analog)	L	Aib, GC15136 and HMC001 are linked via a 10-kDa, bifunctional maleimide-polyethylene glycol-aldehyde (MAL-PEG-ALD) linker	Glucagon analog	Treatment of Congenital Hyperinsulinism	Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration and at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration of HM15136	52 μg/kg	26.6 ± 1.5	Hours	95760	Dogs serum protease	ELISA	Dogs serum	In Vivo	PDB id: 5HVW, https://pubmed.ncbi.nlm.nih.gov/36202918/	None	KD (HM15136) = No binding for FcγRIA, FcγRIIA, FcγRIIB/C, FcγRIIIA, FcγRIIIB, C1q
4405	36588717	2022	GEPPPPGKPADDAGLV	[3H]BPC157	15	Free	Free	Linear	L	all Proline radiolabelled with [3H]	Isolated from human gastric juice	Treatment of various wounds in rats and dogs	Whole blood and plasma samples of six JVC rats were collected at 0.05, 0.167, 0.5, 1, 2, 4, 8, 24, 48, and 72 h after administration (three males and three females at each time point) for the examination of radio pharmacokinetics of total plasma	100 µg/300 μCi/kg	102 ± 32	Hours	367200	JVC rats plasma protease	Liquid scintillation counter	JVC Rats plasma	In Vivo	None	None	N.A.
4477	36323988	2022	HADGSFSDEMNTILDNLAARDFINWLIQTKITD	Glepaglutide	33	Free	Free	Linear	L	None	GLP-2 analogue	Treatment of Short Bowel Syndrome	blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose)	5 mg	228	Hours	820800	Human plasma protease	LC-MS	Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses	In Vivo	None	None	EC50 = 0.12 nM In vitro potency
4480	36323988	2022	HGEGTFSSELATILDALAARDFIAWLIATKITDK	Glepaglutide M2	34	Free	1 lysines has been added at C terminal	Linear	L	None	GLP-2 analogue	Treatment of Short Bowel Syndrome	blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose)	5 mg	231	Hours	831600	Human plasma protease	LC-MS	Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses	In Vivo	None	None	EC50 = 0.044 nM In vitro potency
4481	36323988	2022	HADGSFSDEMNTILDNLAARDFINWLIQTKITD	Glepaglutide	33	Free	Free	Linear	L	None	GLP-2 analogue	Treatment of Short Bowel Syndrome	blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose)	10 mg	254	Hours	914400	Human plasma protease	LC-MS	Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses	In Vivo	None	None	EC50 = 0.12 nM In vitro potency
4483	36323988	2022	HGEGTFSSELATILDALAARDFIAWLIATKITDKK	Glepaglutide M1	35	Free	Two lysines has been added at C terminal	Linear	L	None	GLP-2 analogue	Treatment of Short Bowel Syndrome	blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose)	10 mg	37.7	Hours	135720	Human plasma protease	LC-MS	Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses	In Vivo	None	None	EC50 = 0.068 nM In vitro potency
4484	36323988	2022	HGEGTFSSELATILDALAARDFIAWLIATKITDK	Glepaglutide M2	34	Free	1 lysines has been added at C terminal	Linear	L	None	GLP-2 analogue	Treatment of Short Bowel Syndrome	blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose)	10 mg	255	Hours	918000	Human plasma protease	LC-MS	Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses	In Vivo	None	None	EC50 = 0.044 nM In vitro potency
4485	36323988	2022	HADGSFSDEMNTILDNLAARDFINWLIQTKITD	Glepaglutide	33	Free	Free	Linear	L	None	GLP-2 analogue	Treatment of Short Bowel Syndrome	blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose)	10 mg	88.3	Hours	317880	Human plasma protease	LC-MS	Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses	In Vivo	None	None	EC50 = 0.044 nM In vitro potency
4493	36142749	2022	Dmt-kFFKKPFTL	PK20	10	Replacing tyrosine (Tyr) with 2,6-dimethyltyrosine (Dmt) at position 1	Free	Linear	Mix	D-amino acid residue (D-Lys) inserted at position 2	opioid–neurotensin hybrid peptide	Analgesic	37°C for 24 h	50 μg/mL	204.4	Hours	735840	N.A.	LC-MS	1M HCl	In Vitro	None	None	Emax = 149.17% ± 2.9 for PK20 (intrinsic activity of the receptor)
4495	36142749	2022	Dmt-kFFKKPFIL	[Ile9]PK20	10	Replacing tyrosine (Tyr) with 2,6-dimethyltyrosine (Dmt) at position 1	Free	Linear	Mix	D-amino acid residue (D-Lys) inserted at position 2	PK20 derivative	Analgesic	37°C for 24 h	50 μg/mL	117.7	Hours	423720	N.A.	LC-MS	1M HCl	In Vitro	None	None	Emax = 151.2% ± 74.5 for [Ile9]PK20 (intrinsic activity of the receptor)
4498	36135098	2022	QDTDTWA	GNRs-AAP1-Cy5	7	Free	Free	Linear	L	Cy5 conjugation	AAP1/AAP1-1/AAP1-2 modified GNRs	Antiadhesive property	At 0, 0.08, 0.16, 0.33, 0.5, 1, 2, 6, 12, 24, 48, 72 h, adding 40 μL termination solution	1 mg/ml	37.81 (T1/2 b )	Hours	136116	Mouse serum protease	HPLC	1 mL mouse serum	In Vitro	None	None	N.A.
4506	36112771	2022	CP-1Nal-dCM-HArg-DWSTP-HyP-WC	BT8009	16	Acetylation	Conjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10	Bicyclic	Mix	cyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modification	BT8009 and MMAE cytotoxin hybrid	Anticancer	24 hours	2 µM	>57.8	Hours	208080	Human plasma protease	LC-MS/MS	Human plasma	In Vitro	None	None	KD(nM) = 2.5±1.3 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in human)
4507	36112771	2022	CP-1Nal-dCM-HArg-DWSTP-HyP-WC	BT8009	16	Acetylation	Conjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10	Bicyclic	Mix	cyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modification	BT8009 and MMAE cytotoxin hybrid	Anticancer	24 hours	2 µM	>57.8	Hours	208080	NHP plasma protease	LC-MS/MS	NHP plasma	In Vitro	None	None	KD(nM) = 6.3±1.3 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in NHP)
4508	36112771	2022	CP-1Nal-dCM-HArg-DWSTP-HyP-WC	BT8009	16	Acetylation	Conjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10	Bicyclic	Mix	cyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modification	BT8009 and MMAE cytotoxin hybrid	Anticancer	24 hours	2 µM	60.7	Hours	218520	Rats plasma protease	LC-MS/MS	Rats plasma	In Vitro	None	None	KD(nM) = 6.0±1.2 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in Rat)
4510	36112771	2022	CP-1Nal-dCM-HArg-DWSTP-HyP-WC	BT8009	16	Acetylation	Conjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10	Bicyclic	Mix	cyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modification	BT8009 and MMAE cytotoxin hybrid	Anticancer	24 hours	2 µM	26.1	Hours	93960	Human blood Protease	LC-MS/MS	Human blood sample	In Vitro	None	None	KD(nM) = 2.5±1.3 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in human)
4511	36112771	2022	CP-1Nal-dCM-HArg-DWSTP-HyP-WC	BT8009	16	Acetylation	Conjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10	Bicyclic	Mix	cyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modification	BT8009 and MMAE cytotoxin hybrid	Anticancer	24 hours	2 µM	28.3	Hours	101880	NHP blood protease	LC-MS/MS	NHP blood sample	In Vitro	None	None	KD(nM) = 6.3±1.3 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in NHP)
4514	36101452	2022	NNFQGLRSFGCRFGTCTVQKLAHQIYQFTDKDKDNVAPRSKISPQGY	IgG1 S-AM (6-52)	47	IgG1 Fc linked with hAM using linker (GGGGS)3	Amidation	Cyclic (C16-C21 Disulfide Bond In Ham)	L	None	hAM-IgG Fc fusion protein	AntiiInflammatory	Blood was collected before injection (day 0), and then 1, 2, 4, 6, 8, 10, 12, and 14 days after administration	30 nmol/kg	2.11	Days	182304	Wistar rats plasma protease	ELISA (measure mAM)	Wistar rats plasma	In Vivo	None	None	After treatment with IgG4-AM (6-52), SBP (Systolic Blood Pressure) decreased significantly over time, showing reductions of 24.3 ± 4.8 mmHg on day 3, 32.2 ± 6.9 mmHg on day 6, 40.7 ± 3.1 mmHg on day 9, and 56.6 ± 4.5 mmHg on day 12, compared to the control group
4515	36101452	2022	NNFQGLRSFGCRFGTCTVQKLAHQIYQFTDKDKDNVAPRSKISPQGY	IgG4 S-AM (6-52)	47	IgG4 Fc linked with hAM using linker (GGGGS)3	Amidation	Linear	L	None	hAM-IgG Fc fusion protein	AntiiInflammatory	Blood was collected before injection (day 0), and then 1, 2, 4, 6, 8, 10, 12, and 14 days after administration	30 nmol/kg	2.37	Days	204768	Wistar rats plasma protease	ELISA (measure mAM )	Wistar rats plasma	In Vivo	None	None	After treatment with IgG4-AM (6-52), SBP (Systolic Blood Pressure) decreased significantly over time, showing reductions of 24.3 ± 4.8 mmHg on day 3, 32.2 ± 6.9 mmHg on day 6, 40.7 ± 3.1 mmHg on day 9, and 56.6 ± 4.5 mmHg on day 12, compared to the control group
4516	36101452	2022	NNFQGLRSFGCRFGTCTVQKLAHQIYQFTDKDKDNVAPRSKISPQGY	IgG1 S-AM (6-52)	47	IgG1 Fc linked with hAM using linker (GGGGS)3	Amidation	Cyclic (C16-C21 Disulfide Bond In Ham)	L	None	hAM-IgG Fc fusion protein	AntiiInflammatory	Blood was collected before injection (day 0), and then 1, 2, 4, 6, 8, 10, 12, and 14 days after administration	30 nmol/kg	2.885	Days	249264	Wistar rats plasma protease	ELISA (measure tAM )	Wistar rats plasma	In Vivo	None	None	After treatment with IgG4-AM (6-52), SBP (Systolic Blood Pressure) decreased significantly over time, showing reductions of 24.3 ± 4.8 mmHg on day 3, 32.2 ± 6.9 mmHg on day 6, 40.7 ± 3.1 mmHg on day 9, and 56.6 ± 4.5 mmHg on day 12, compared to the control group
4517	36101452	2022	NNFQGLRSFGCRFGTCTVQKLAHQIYQFTDKDKDNVAPRSKISPQGY	IgG4 S-AM (6-52)	47	IgG4 Fc linked with hAM using linker (GGGGS)3	Amidation	Linear	L	None	hAM-IgG Fc fusion protein	AntiiInflammatory	Blood was collected before injection (day 0), and then 1, 2, 4, 6, 8, 10, 12, and 14 days after administration	30 nmol/kg	3.23	Days	279072	Wistar rats plasma protease	ELISA (measure tAM )	Wistar rats plasma	In Vivo	None	None	After treatment with IgG4-AM (6-52), SBP (Systolic Blood Pressure) decreased significantly over time, showing reductions of 24.3 ± 4.8 mmHg on day 3, 32.2 ± 6.9 mmHg on day 6, 40.7 ± 3.1 mmHg on day 9, and 56.6 ± 4.5 mmHg on day 12, compared to the control group
4521	36075899	2022	None	S-20-1	None	N.A.	N.A.	Cyclic	L	Modified by adding negative charge	Synthetic	Antiviral (Against Infection By Sars-Cov-2 )	Blood samples were collected at 10 min, 20 min, 30 min, 1 h, 2 h, 4 h, 8 h, 24 h and 48 h	50 mg/kg	24.29 (Terminal Elimination Half Life)	Hours	87444	C57Bl/6 mice plasma protease	LC-MS/MS	C57BL/6 mice plasma	In Vivo	None	None	IC50 (μM) = 0.8 in HUH 7 cells
4526	35999612	2022	RGD	cRGD-Exo/TP	3	DSPE-PEG	Free	Cyclic (RGD)	L	DiR labeled	Synthetic	Targeted delivery of triptolide against malignant melanoma	Scanned at interval times (1, 2, 4, 6, 12, and 24 h)	N.A.	27.14 ± 2.55	Hours	97704	Mice plasma protease	IVIS at 750/780 nm	BALB/c nude mice plasma	In Vivo	None	None	Tumor inhibition rate of 65.73 ± 3.29% in the cRGD-Exo/TP
4539	35971165	2022	YLCSSNNNRERDKFRRGGSGGTSFEQFWAWLWP	Au‐AR pep‐PROTAC	33	Free	Free	Linear	L	None	Synthetic	Anticancer (Prostate Cancer Therapy)	N.A.	N.A.	26.3	Hours	94680	Mouse serum protease	ICP‐MS	mouse serum	In Vivo	None	None	N.A.
4540	35971165	2022	YLCSSNNNRERDKFRRGGSGGTSFEQFWAWLWP	Au‐AR pep‐PROTAC	33	Free	Free	Linear	L	None	Synthetic	Anticancer (Prostate Cancer Therapy)	N.A.	N.A.	25.1	Hours	90360	PBS containing 10% serum protease	HPLC	PBS containing 10% serum	In Vitro	None	None	IC50 of Au‐AR pep‐PROTAC on AML 12 cells is 2.41 µM
4542	35892256	2022	GIVEQCCTSICSLYQLENYCN/FVNQHLCGSHLVEALYLVCGERGFFYTPKT	RA15127343	51	Free	Free	Linear	L	Albumin binding fatty-acid side chain is coupled to lysine (B29)	Insulin analogue	Antidiabetes	Blood samples were collected before RA15127343 administration (baseline) and 1–4 times per day until study end.	10 nmol/kg	47	Hours	169200	Göttingen minipigs plasma protease	LC-MS/MS	Göttingen minipigs plasma	In Vivo	https://sci-hub.st/10.1016/j.jpba.2018.07.009	None	(Activity values of RA15127343) IC50 for IR-A: 19.9 μM, IC50 for IR-B: 6.31 μM, EC50 for IR-A: 2.054 μM, EC50 for IR-B: 669.6 nM
4543	35892256	2022	GIVEQCCTSICSLYQLENYCN/FVNQHLCGSHLVEALYLVCGERGFFYTPKT	RA15127343	51	Free	Free	Linear	L	Albumin binding fatty-acid side chain is coupled to lysine (B29)	Insulin analogue	Antidiabetes	Blood samples were collected before RA15127343 administration (baseline) and 1–4 times per day until study end.	10,30,45,60 nmol/kg	48 - 59	Hours	212400	Göttingen minipigs plasma protease	LC-MS/MS	Göttingen minipigs plasma	In Vivo	https://sci-hub.st/10.1016/j.jpba.2018.07.009	None	(Activity values of RA15127343) IC50 for IR-A: 19.9 μM, IC50 for IR-B: 6.31 μM, EC50 for IR-A: 2.054 μM, EC50 for IR-B: 669.6 nM
4554	35858423	2022	LQEHPQARKYKGAQKKGLSKGCFGLKLDRIGSMSGLGC	4A	38	3A coupled to bicyclononyne-modified MSs (MS-N-hydroxysuccinymidocarbonates)	Free	Linear	L	Gln 6,14 modification, Mod = (CH3)2CHSO2-, N3-linker N-hydroxysuccinymidocarbonates containing isopropyl sulfone (1A) and N,N-dimethyl-sulfonamide (1B) modulators	MS-[Gln6,14]CNP-38 conjugate	Treatment of Achondroplasia	Blood samples (~100 μL) were drawn from the tail vein at 8, 24, 48, 72, 120, 168, 240, 336, 432, 504, 600 and 672 h on a staggered schedule from 12 mice to give 4 replicates at each time-point	20 nmol	40 (T1/2,a -Elimination Half Life)	Hours	144000	CD1 mice plasma protease	ELISA, LC-MS/MS	CD1 mice plasma	In Vivo	None	None	QWk 50 nmol of 4A caused significantly increased growth, with mice becoming about 25% longer than the vehicle control over the study period
4555	35858423	2022	LQEHPQARKYKGAQKKGLSKGCFGLKLDRIGSMSGLGC	4B	38	3B coupled to bicyclononyne-modified MSs (MS-N-hydroxysuccinymidocarbonates)	Free	Linear	L	Gln 6,14 modification, Mod = (CH3)2CHSO2-, N3-linker N-hydroxysuccinymidocarbonates containing N,N-dimethyl-sulfonamide (1B) modulators	MS-[Gln6,14]CNP-38 conjugate	Treatment of Achondroplasia	Blood samples (~100 μL) were drawn from the tail vein at 8, 24, 24, 96, 168, 240, 336, 408, 504, 576, 672, 840, 1008, 1176, 1344, and 1512 h from 8 mice on a staggered schedule to give 4 replicates at each time-point	700 nmol	60 ( T1/2,a - Elimination Half Life)	Hours	216000	CD1 mice plasma protease	ELISA, LC-MS/MS	CD1 mice plasma	In Vivo	None	None	Single dose of 85 nmol of 4B showed similar growth stimulation as QD administration of [Gln6,14]CNP-38 for 3 weeks, but growth plateaued afterward
4556	35858423	2022	LQEHPQARKYKGAQKKGLSKGCFGLKLDRIGSMSGLGC	4A	38	3A coupled to bicyclononyne-modified MSs (MS-N-hydroxysuccinymidocarbonates)	Free	Linear	L	Gln 6,14 modification, Mod = (CH3)2CHSO2-	MS-[Gln6,14]CNP-38 conjugate	Treatment of Achondroplasia	Blood samples (~100 μL) were drawn from the tail vein at 8, 24, 48, 72, 120, 168, 240, 336, 432, 504, 600 and 672 h on a staggered schedule from 12 mice to give 4 replicates at each time-point	20 nmol	212 (T1/2,b-Elimination Half Life)	Hours	763200	CD1 mice plasma protease	ELISA, LC-MS/MS	CD1 mice plasma	In Vivo	None	None	QWk 50 nmol of 4A caused significantly increased growth, with mice becoming about 25% longer than the vehicle control over the study period
4557	35858423	2022	LQEHPQARKYKGAQKKGLSKGCFGLKLDRIGSMSGLGC	4B	38	3B coupled to bicyclononyne-modified MSs (MS-N-hydroxysuccinymidocarbonates)	Free	Linear	L	Gln 6,14 modification, Mod = (CH3)2NSO2-	MS-[Gln6,14]CNP-38 conjugate	Treatment of Achondroplasia	Blood samples (~100 μL) were drawn from the tail vein at 8, 24, 24, 96, 168, 240, 336, 408, 504, 576, 672, 840, 1008, 1176, 1344, and 1512 h from 8 mice on a staggered schedule to give 4 replicates at each time-point	700 nmol	610 ( T1/2,b-Elimination Half Life)	Hours	2196000	CD1 mice plasma protease	ELISA, LC-MS/MS	CD1 mice plasma	In Vivo	None	None	Single dose of 85 nmol of 4B showed similar growth stimulation as QD administration of [Gln6,14]CNP-38 for 3 weeks, but growth plateaued afterward
4562	35840338	2022	FVNQHLCGSHLVEALELVCGERGFHYGGGGGGSGGGGGIVEQCCTSTCSLDQLENYCGGGGGQGGGGQGGGGQGGGGGECPPCPAPPVAGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTFRVVSVLTVVHQDWLNGKEYKCKVSNKGLPAPIEKTISKTKGQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPMLDSDGSFFLYSVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	BIF	296	Single-chain variant of insulin has modifications:TyrB16Glu,PheB25His,ThrB27Gly,ProB28Gly,LysB29Gly,ThrB30Gly,IleA10Thr,TyrA14Asp,AsnA21Gly, single-chain variant of insulin with B-chain linked to A-chain by a short linker (Linker 1)	Interdomain linker (Linker 2) connecting the A-chain of insulin to the Fc and the Fc domain from IgG2	Linear	L	None	Fc-fusion protein	Antidiabetes	Blood samples for glucose measurements were collected by tail bleed conducted under brief restraint. Blood glucose was measured preinjection, 1, 2, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120,144, 168, 240, and 336 hours postdose	3 nmol/kg	128 ± 10	Hours	460800	Streptozotocin STZ-treated diabetic SD rats blood protease	Insulin receptor ELISA	Streptozotocin STZ-treated diabetic SD rats blood sample	In Vivo	None	None	Receptor Phosphorylation EC50, nM = 4241 (Functional activity of BIF as determined by phosphorylation of hIR-A expressed in 293 cells)
4563	35840338	2022	FVNQHLCGSHLVEALELVCGERGFHYGGGGGGSGGGGGIVEQCCTSTCSLDQLENYCGGGGGQGGGGQGGGGQGGGGGECPPCPAPPVAGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTFRVVSVLTVVHQDWLNGKEYKCKVSNKGLPAPIEKTISKTKGQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPMLDSDGSFFLYSVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	BIF	296	Single-chain variant of insulin has modifications:TyrB16Glu,PheB25His,ThrB27Gly,ProB28Gly,LysB29Gly,ThrB30Gly,IleA10Thr,TyrA14Asp,AsnA21Gly, single-chain variant of insulin with B-chain linked to A-chain by a short linker (Linker 1)	Interdomain linker (Linker 2) connecting the A-chain of insulin to the Fc and the Fc domain from IgG2	Linear	L	None	Fc-fusion protein	Antidiabetes	Blood samples for glucose measurements were collected by tail bleed conducted under brief restraint. Blood glucose was measured preinjection, 1, 2, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120,144, 168, 240, and 336 hours postdose	10 nmol/kg	104 ± 4	Hours	374400	Streptozotocin STZ-treated diabetic SD rats blood protease	Insulin receptor ELISA	Streptozotocin STZ-treated diabetic SD rats blood sample	In Vivo	None	None	Receptor Phosphorylation EC50, nM = 391 (Functional activity of BIF as determined by phosphorylation of hIR-B expressed in 293 cells)
4564	35840338	2022	FVNQHLCGSHLVEALELVCGERGFHYGGGGGGSGGGGGIVEQCCTSTCSLDQLENYCGGGGGQGGGGQGGGGQGGGGGECPPCPAPPVAGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTFRVVSVLTVVHQDWLNGKEYKCKVSNKGLPAPIEKTISKTKGQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPMLDSDGSFFLYSVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	BIF	296	single-chain variant of insulin has modifications:TyrB16Glu,PheB25His,ThrB27Gly,ProB28Gly,LysB29Gly,ThrB30Gly,IleA10Thr,TyrA14Asp,AsnA21Gly, single-chain variant of insulin with B-chain linked to A-chain by a short linker (Linker 1)	interdomain linker (Linker 2) connecting the A-chain of insulin to the Fc and the Fc domain from IgG2	Linear	L	None	Fc-fusion protein	Antidiabetes	Blood samples for glucose measurements were collected by tail bleed conducted under brief restraint. Blood glucose was measured preinjection, 1, 2, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120,144, 168, 240, and 336 hours postdose	30 nmol/kg	120 ± 21	Hours	432000	Streptozotocin STZ-treated diabetic SD rats blood protease	Insulin receptor ELISA	Streptozotocin STZ-treated diabetic SD rats blood sample	In Vivo	None	None	Receptor Phosphorylation EC50, nM > 10,000 (Functional activity of BIF as determined by phosphorylation of hIGF-1R expressed in 293 cells)
4565	35840338	2022	FVNQHLCGSHLVEALELVCGERGFHYGGGGGGSGGGGGIVEQCCTSTCSLDQLENYCGGGGGQGGGGQGGGGQGGGGGECPPCPAPPVAGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTFRVVSVLTVVHQDWLNGKEYKCKVSNKGLPAPIEKTISKTKGQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPMLDSDGSFFLYSVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	BIF	296	single-chain variant of insulin has modifications:TyrB16Glu,PheB25His,ThrB27Gly,ProB28Gly,LysB29Gly,ThrB30Gly,IleA10Thr,TyrA14Asp,AsnA21Gly, single-chain variant of insulin with B-chain linked to A-chain by a short linker (Linker 1)	interdomain linker (Linker 2) connecting the A-chain of insulin to the Fc and the Fc domain from IgG2	Linear	L	None	Fc-fusion protein	Antidiabetes	Blood samples for glucose measurements were collected by tail bleed conducted under brief restraint. Blood glucose was measured preinjection, 1, 2, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120,144, 168, 240, and 336 hours postdose	30 nmol/kg	120 ± 21	Hours	432000	Streptozotocin STZ-treated diabetic SD rats blood protease	Insulin receptor ELISA	Streptozotocin STZ-treated diabetic SD rats blood sample	In Vivo	None	None	Lipogenesis in 3T3-L1 Adipocytes, EC50 nM = 19 (Functional activity of BIF as assessed by lipogenesis and cellular proliferation)
4566	35840338	2022	FVNQHLCGSHLVEALELVCGERGFHYGGGGGGSGGGGGIVEQCCTSTCSLDQLENYCGGGGGQGGGGQGGGGQGGGGGECPPCPAPPVAGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTFRVVSVLTVVHQDWLNGKEYKCKVSNKGLPAPIEKTISKTKGQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPMLDSDGSFFLYSVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	BIF	296	single-chain variant of insulin has modifications:TyrB16Glu,PheB25His,ThrB27Gly,ProB28Gly,LysB29Gly,ThrB30Gly,IleA10Thr,TyrA14Asp,AsnA21Gly, single-chain variant of insulin with B-chain linked to A-chain by a short linker (Linker 1)	interdomain linker (Linker 2) connecting the A-chain of insulin to the Fc and the Fc domain from IgG2	Linear	L	None	Fc-fusion protein	Antidiabetes	Blood samples for glucose measurements were collected by tail bleed conducted under brief restraint. Blood glucose was measured preinjection, 1, 2, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120,144, 168, 240, and 336 hours postdose	30 nmol/kg	120 ± 21	Hours	432000	Streptozotocin STZ-treated diabetic SD rats blood protease	Insulin receptor ELISA	Streptozotocin STZ-treated diabetic SD rats blood sample	In Vivo	None	None	Proliferation in Saos-2 Cells,EC50 nM = 134 (Functional activity of BIF as assessed by cellular proliferation)
4567	35840338	2022	FVNQHLCGSHLVEALELVCGERGFHYGGGGGGSGGGGGIVEQCCTSTCSLDQLENYCGGGGGQGGGGQGGGGQGGGGGECPPCPAPPVAGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTFRVVSVLTVVHQDWLNGKEYKCKVSNKGLPAPIEKTISKTKGQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPMLDSDGSFFLYSVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	BIF	296	single-chain variant of insulin has modifications:TyrB16Glu,PheB25His,ThrB27Gly,ProB28Gly,LysB29Gly,ThrB30Gly,IleA10Thr,TyrA14Asp,AsnA21Gly, single-chain variant of insulin with B-chain linked to A-chain by a short linker (Linker 1)	interdomain linker (Linker 2) connecting the A-chain of insulin to the Fc and the Fc domain from IgG2	Linear	L	None	Fc-fusion protein	Antidiabetes	Blood samples for glucose measurements were collected by tail bleed conducted under brief restraint. Blood glucose was measured preinjection, 1, 2, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120,144, 168, 240, and 336 hours postdose	30 nmol/kg	120 ± 21	Hours	432000	Streptozotocin STZ-treated diabetic SD rats blood protease	Insulin receptor ELISA	Streptozotocin STZ-treated diabetic SD rats blood sample	In Vivo	None	None	Proliferation in H4IIE Cells,EC50 nM = 20 (Functional activity of BIF as assessed by cellular proliferation)
4598	35674880	2022	Y-Aib-EGTFTSDYSI-Aib-LDKIAQKAFVQWLIAGGPSSGAPPPS	Tirzepatide	39	Free	Free	Linear	L	C20 fatty diacid conjugation at the side chain of the Lys20, Aib = alpha-amino isobutyric acid at position 2,13	GLP-1 analogs	Antidiabetes	Plasma concentrations of tirzepatide measured pre-dose, and at 8, 12, 24, 48, 72, 96, 168, and 336 hours post-dose	5 mg	124	Hours	446400	Human Plasma Protease	LC-MS	Human plasma with Normal hepatic function	In Vivo	None	None	N.A.
4599	35674880	2022	Y-Aib-EGTFTSDYSI-Aib-LDKIAQKAFVQWLIAGGPSSGAPPPS	Tirzepatide	39	Free	Free	Linear	L	C20 fatty diacid conjugation at the side chain of the Lys20, Aib = alpha-amino isobutyric acid at position 2,13	GLP-1 analogs	Antidiabetes	Plasma concentrations of tirzepatide measured pre-dose, and at 8, 12, 24, 48, 72, 96, 168, and 336 hours post-dose	5 mg	131	Hours	471600	Human Plasma Protease	LC-MS	Human plasma with Mild hepatic impairment	In Vivo	None	None	N.A.
4600	35674880	2022	Y-Aib-EGTFTSDYSI-Aib-LDKIAQKAFVQWLIAGGPSSGAPPPS	Tirzepatide	39	Free	Free	Linear	L	C20 fatty diacid conjugation at the side chain of the Lys20, Aib = alpha-amino isobutyric acid at position 2,13	GLP-1 analogs	Antidiabetes	Plasma concentrations of tirzepatide measured pre-dose, and at 8, 12, 24, 48, 72, 96, 168, and 336 hours post-dose	5 mg	116	Hours	417600	Human Plasma Protease	LC-MS	Human plasma with Moderate hepatic impairment	In Vivo	None	None	N.A.
4601	35674880	2022	Y-Aib-EGTFTSDYSI-Aib-LDKIAQKAFVQWLIAGGPSSGAPPPS	Tirzepatide	39	Free	Free	Linear	L	C20 fatty diacid conjugation at the side chain of the Lys20, Aib = alpha-amino isobutyric acid at position 2,13	GLP-1 analogs	Antidiabetes	Plasma concentrations of tirzepatide measured pre-dose, and at 8, 12, 24, 48, 72, 96, 168, and 336 hours post-dose	5 mg	122	Hours	439200	Human Plasma Protease	LC-MS	Human plasma with Severe hepatic impairment	In Vivo	None	None	N.A.
4615	35458385	2022	RDLEVVAATPTSLLISWDAPAVTVRYYRITYGETGGNSPVQEFTVPGSKSTATISGLKPGVDYTITVYAVTGRGDSPASSKPISINYRTEIGGGGSGGGGSGGGGSGGGGSGGGGSGGGGSGGGGSSLDQINVTFLDLEYEMKKLEEAIKKLEESYIDLKEL	FL-EK1	162	Flexible 35-mer linker (L35) connects the FN3 domain to the EK1 peptide at N terminus	Free	Linear	L	None	EK1 and 10th FN3 unit conjugate	Pan-cov fusion inhibitor	Serum samples were collected before (0 h) and after injection of EK1 (0.5 h, 1 h, 3 h, 7 h, and 12 h) or FL-EK1 (0.5 h, 1 h, 3 h, 7 h, 24 h, 48 h, 72 h, and 96 h)	40 mg/kg	30.0 ± 12.8	Hours	108000	Mice serum protease	Sandwich ELISA	Mice serum	In Vivo	None	None	IC50(nM) = 114.5 ± 33.4 against B.1.1.7 (Alpha), IC50(nM) = 201.2 ± 16.8 against B.1.351 (Beta), IC50(nM) = 373.1 ± 16.9 against P.1 (Gamma), IC50(nM) = 133.0 ± 16.5 against B.1.617.2 (Delta), IC50(nM) = 179.2 ± 38.3 against B.1.525 (Eta), IC50(nM) = 230.9 ± 49.3 against B.1.617.1 (Kappa), IC50(nM) = 88.5 ± 58.2 against C.37 (Lambda), IC50(nM) = 297.5 ± 188.2 against B.1.1.529 (Omicron)
4617	35455421	2022	RDLEVVAATPTSLLISWDAPAVTVRYYRITYGETGGNSPVQEFTVPGSKSTATISGLKPGVDYTITVYAVTGRGDSPASSKPISINYRTEIGGGGSGGGGSGGGGSGGGGSGGGGSGGGGSGGGGSTTWEAWDRAIAEYAARIEALLRALQEQQEKNEAALRE	FLT	163	FN3 domain	Free	Linear	L	None	FN3 ,T1144 fusion protein	Antiviral (HIV fusion inhibitor)	Blood samples were collected from the orbital sinus at 0, 0.5, 1.5, 3, 6, 9, 12, 24, 48, 72, 96 and 120 h after injection of the inhibitors tested	5.94 mg/kg	27.09 ± 6.9	Hours	97524	Rats serum protease	Sandwich ELISA	Rats serum	In Vivo	None	None	IC50(nM)= 65.3 ± 2.6 against HIV-1 96USSN20 (X4/R5, A), IC50(nM) = 9.8 ± 0.9 against HIV-1 96USNG17 (X4, A), IC50(nM) = 6.5 ± 0.2 against HIV-1 90US_873 (R5, B), IC50(nM) = 8.8 ± 0.3 against HIV-1 BZ167 (X4, B), IC50(nM) = 12.5 ± 0.5 against HIV-1 SE364 (R5, C), IC50(nM) = 9.3 ± 0.5 against HIV-1 PBL288 (R5, C), IC50(nM) = 11.7 ± 0.8 against HIV-1 92UG001 (X4/R5, D), IC50(nM) = 6.4 ± 0.3 against HIV-1 J32228M4 (R5, D), IC50(nM) = 7.5 ± 0.3 against HIV-1 DJ263 (R5, CRF02_AG), IC50(nM) = 10.2 ± 0.6 against HIV-1 CAM1475MV (R5, CRF02_AG) (Infection on MT-4 cells)
4667	35046019	2022	MSKGPG-(VPGGGVPGAGVPG(pAzF)G)10-PGGGG–SKGEELFTGVVPILVELDGDVNGHKFSVRGEGEGDATNGKLTLKFICTTGKLPVPWPTLVTTLTYGVQCFSRYPDHMKRHDFFKSAMPEGYVQERTISFKDDGTYKTRAEVKFEGDTLVNRIELKGIDFKEDGNILGHKLEYNFNSHNVYITADKQKNGIKANFKIRHNVEDGSVQLADHYQQNTPIGDGPVLLPDNHYLSTQSVLSKDPNEKRDHMVLLEFVTAAGITHGMDELYKGS	ELP(10FA)GFP	400	Free	GFP	Linear	L	10 Fatty acid conjugation through pAzF (para-azidophenylalanine)	ELP-GFP conjugate	Increases Half Life	1 week	10 μM	33.3	Hours	119880	C57Bl/6J mice blood plasma protease	GFP-specific ELISA	C57BL/6J mice blood plasma	In Vivo	None	None	KD MSA (μM) =2.76 ± 0.19, KD HSA - Human serum albumin (μM) = n.d
4669	35046019	2022	MSKGPG-(VPGGGVPGAGVPG(pAzF-FA)GVPGGGVPGAGVPGYG)5-PGGGG-SKGEELFTGVVPILVELDGDVNGHKFSVRGEGEGDATNGKLTLKFICTTGKLPVPWPTLVTTLTYGVQCFSRYPDHMKRHDFFKSAMPEGYVQERTISFKDDGTYKTRAEVKFEGDTLVNRIELKGIDFKEDGNILGHKLEYNFNSHNVYITADKQKNGIKANFKIRHNVEDGSVQLADHYQQNTPIGDGPVLLPDNHYLSTQSVLSKDPNEKRDHMVLLEFVTAAGITHGMDELYKGS	ELP(5FA)GFP	400	Free	GFP	Linear	L	5 Fatty acid conjugation through pAzF (para-azidophenylalanine)	ELP-GFP conjugate	Increases Half Life	1 week	10 μM	31.7	Hours	114120	C57Bl/6J mice blood plasma protease	GFP-specific ELISA	C57BL/6J mice blood plasma	In Vivo	None	None	KD MSA (μM) =4.0 ± 1.6, KD HSA - Human serum albumin (μM) = 3.16 ± 0.60
4670	35046019	2022	MSKGPG-(VPGGGVPGAGVPG(pAzF)G)10-PGGGG–SKGEELFTGVVPILVELDGDVNGHKFSVRGEGEGDATNGKLTLKFICTTGKLPVPWPTLVTTLTYGVQCFSRYPDHMKRHDFFKSAMPEGYVQERTISFKDDGTYKTRAEVKFEGDTLVNRIELKGIDFKEDGNILGHKLEYNFNSHNVYITADKQKNGIKANFKIRHNVEDGSVQLADHYQQNTPIGDGPVLLPDNHYLSTQSVLSKDPNEKRDHMVLLEFVTAAGITHGMDELYKGS	ELP(10FA)GFP	400	Free	GFP	Linear	L	10 Fatty acid conjugation through pAzF (para-azidophenylalanine)	ELP-GFP conjugate	Increases Half Life	1 week	10 μM	27.9	Hours	100440	C57Bl/6J mice blood plasma protease	GFP-specific ELISA	C57BL/6J mice blood plasma	In Vivo	None	None	KD MSA (μM) = 2.22 ± 0.03, KD HSA - Human serum albumin (μM) = 1.64 ± 0.17
4718	EP 2021080747 W	2022	k-Sar-H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Chem.37 (reference compound)	33	k=D-Lysine,Sar=N-terminal glycine, N£-octadecanoyl	Free	Linear	Mix	Aib substituitions at position 2 of semaglutide	Semaglutide Derivative	Antidiabetes	Blood samples (0.8 Ml) were taken via the second catheter at predetermined time points (0-3 weeks)	10 nmol/kg	78 (Terminal Half Life)	Hours	280800	Minipigs plasma protease	LC-MS	Minipigs plasma	In Vivo	None	EP 2021080747 W	N.A.
4719	EP 2021080747 W	2022	None	Test 1	None	N.A.	N.A.	N.A.	N.A.	N.A.	GLP-1 analogs	Antidiabetes	Blood samples (0.8 Ml) were taken via the second catheter at predetermined time points (0-3 weeks)	10 nmol/kg	100 (Terminal Half Life)	Hours	360000	Minipigs plasma protease	LC-MS	Minipigs plasma	In Vivo	None	EP 2021080747 W	N.A.
4720	EP 2021080747 W	2022	None	Test 2	None	N.A.	N.A.	N.A.	N.A.	N.A.	GLP-1 analogs	Antidiabetes	Blood samples (0.8 Ml) were taken via the second catheter at predetermined time points (0-3 weeks)	10 nmol/kg	101 (Terminal Half Life)	Hours	363600	Minipigs plasma protease	LC-MS	Minipigs plasma	In Vivo	None	EP 2021080747 W	N.A.
4721	EP 2021080747 W	2022	None	Test 3	None	N.A.	N.A.	N.A.	N.A.	N.A.	GLP-1 analogs	Antidiabetes	Blood samples (0.8 Ml) were taken via the second catheter at predetermined time points (0-3 weeks)	10 nmol/kg	105 (Terminal Half Life)	Hours	378000	Minipigs plasma protease	LC-MS	Minipigs plasma	In Vivo	None	EP 2021080747 W	N.A.
4722	EP 2021080747 W	2022	None	Test 4	None	N.A.	N.A.	N.A.	N.A.	N.A.	GLP-1 analogs	Antidiabetes	Blood samples (0.8 Ml) were taken via the second catheter at predetermined time points (0-3 weeks)	10 nmol/kg	109 (Terminal Half Life)	Hours	392400	Minipigs plasma protease	LC-MS	Minipigs plasma	In Vivo	None	EP 2021080747 W	N.A.
4723	EP 2021080747 W	2022	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	GLP-1 receptor agonist	Blood samples (0.8 Ml) were taken via the second catheter at predetermined time points (0-3 weeks)	10 nmol/kg	69 (Terminal Half Life)	Hours	248400	Minipigs plasma protease	LC-MS	Minipigs plasma	In Vivo	None	EP 2021080747 W	N.A.
4725	US 2021/0062261 W	2022	EVQLVESGGGLVQPGGSLRLSCAASGSTFYTAVMGWVRQAPGKGLEWVAAIRWTALTTSYADSVKGRFTISRDGAKTTLYLQMNSLRPEDTAVYYCAARGTLGLFTTADSYDYWGQGTLVTVSSGGGGSGGGSGGVYCGPEFDESVGCMGGGGSGGGLSGRSDAGSPLGLAGSGGGSEVQLVESGGGLVQPGGSLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTVVTQEPSLTVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVLGGGGSQVQLQQSGSELKKPGASVKVSCKASGYTFTNYGMNWVKQAPGQGLKWMGWINTYTGEPTYTDDFKGRFAFSLDTSVSTAYLQISSLKADDTAVYFCARGGFGSSYWYFDVWGQGSLVTVSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSC-GGVDFCKIYSWPVCHQGGGGSGGLSGRSDAGSPLGLAGSGGSDIQLTQSPSSLSASVGDRVSITCKASQDVSIAVAWYQQKPGKAPKLLIYSASYRYTGVPDRFSGSGSGTDFTLTISSLQPEDFAVYYCQQHYITPLTFGAGTKVEIKRTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC	TROP2 TRACTr PC complex (PC5)	911	Free	Fab heavy chain linked to C terminus of ScFv light chain	Linear	L	None	Synthetic	Mediates tumor cytotoxicity and T cell activation	N.A.	100 ug/kg	90.16	Hours	324576	Cynomolgus monkeys plasma protease	ELISA	Cynomolgus monkeys plasma	In Vivo	None	US 2021/0062261 W	EC50(nM) = 60.25 (TROP binding)
4726	US 2021/0062261 W	2022	EVQLVESGGGLVQPGGSLRLSCAASGSTFYTAVMGWVRQAPGKGLEWVAAIRWTALTTSYADSVKGRFTISRDGAKTTLYLQMNSLRPEDTAVYYCAARGTLGLFTTADSYDYWGQGTLVTVSSGGGGSGGGSGGVYCGPEFDESVGCMGSSGGSAAGLLAPPGGLSGRSDAGGGGSEVQLVESGGGLVQPGGSLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTVVTQEPSLTVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVLGGGGSQVQLQQSGSELKKPGASVKVSCKASGYTFTNYGMNWVKQAPGQGLKWMGWINTYTGEPTYTDDFKGRFAFSLDTSVSTAYLQISSLKADDTAVYFCARGGFGSSYWYFDVWGQGSLVTVSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSC-GGIDFCMLYNWPICAGGGGGSSGGSAAGLLAPPGGLSGRSDAGGGGSDIQLTQSPSSLSASVGDRVSITCKASQDVSIAVAWYQQKPGKAPKLLIYSASYRYTGVPDRFSGSGSGTDFTLTISSLQPEDFAVYYCQQHYITPLTFGAGTKVEIKRTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC	TROP2 TRACTr PC complex (PC18)	916	Free	Fab heavy chain linked to C terminus of ScFv light chain	Linear	L	None	Synthetic	Mediates tumor cytotoxicity and T cell activation	N.A.	100 μg/kg	97.31	Hours	350316	Cynomolgus monkeys plasma protease	ELISA	Cynomolgus monkeys plasma	In Vivo	None	US 2021/0062261 W	IC50(pM) = 3,253
4727	US 2021/0062261 W	2022	EVQLVESGGGLVQPGGSLRLSCAASGSTFYTAVMGWVRQAPGKGLEWVAAIRWTALTTSYADSVKGRFTISRDGAKTTLYLQMNSLRPEDTAVYYCAARGTLGLFTTADSYDYWGQGTLVTVSSGGGGSGGGSGGVYCGPEFDESVGCMGSSGGSAAGLLAPPGGLSGRSDAGGGGSEVQLVESGGGLVQPGGSLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTVVTQEPSLTVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVLGGGGSQVQLQQSGSELKKPGASVKVSCKASGYTFTNYGMNWVKQAPGQGLKWMGWINTYTGEPTYTDDFKGRFAFSLDTSVSTAYLQISSLKADDTAVYFCARGGFGSSYWYFDVWGQGSLVTVSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSC-GGVDFCKIYSWPVCHQGGGGSSGGSAAGLLAPPGGLSGRSDAGGGGSDIQLTQSPSSLSASVGDRVSITCKASQDVSIAVAWYQQKPGKAPKLLIYSASYRYTGVPDRFSGSGSGTDFTLTISSLQPEDFAVYYCQQHYITPLTFGAGTKVEIKRTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGECGGIDFCMLYNWPICAGGGGGSSGGSAAGLLAPPGGLSGRSDAGGGGSDIQLTQSPSSLSASVGDRVSITCKASQDVSIAVAWYQQKPGKAPKLLIYSASYRYTGVPDRFSGSGSGTDFTLTISSLQPEDFAVYYCQQHYITPLTFGAGTKVEIKRTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC	TROP2 TRACTr PC complex (PC21)	1177	Free	Fab heavy chain linked to C terminus of ScFv light chain	Linear	L	None	Synthetic	Mediates tumor cytotoxicity and T cell activation	N.A.	100 μg/kg	100.73	Hours	362628	Cynomolgus monkeys plasma protease	ELISA	Cynomolgus monkeys plasma	In Vivo	None	US 2021/0062261 W	N.A.
4728	US 2021/0062261 W	2022	EVQLVESGGGLVQPGGSLRLSCAASGSTFYTAVMGWVRQAPGKGLEWVAAIRWTALTTSYADSVKGRFTISRDGAKTTLYLQMNSLRPEDTAVYYCAARGTLGLFTTADSYDYWGQGTLVTVSSGGGGSGGGSGGVYCGPEFDESVGCMGGGGSGGGLSGRSDAGSPLGLAGSGGGSEVQLVESGGGLVQPGGSLKLSCAASGFTFNKYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMNNLKTEDTAVYYCVRHGNFGNSYISYWAYWGQGTLVTVSSGGGGSGGGGSGGGGSQTVVTQEPSLTVSPGGTVTLTCGSSTGAVTSGNYPNWVQQKPGQAPRGLIGGTKFLAPGTPARFSGSLLGGKAALTLSGVQPEDEAEYYCVLWYSNRWVFGGGTKLTVLGGGGSQVQLQQSGSELKKPGASVKVSCKASGYTFTNYGMNWVKQAPGQGLKWMGWINTYTGEPTYTDDFKGRFAFSLDTSVSTAYLQISSLKADDTAVYFCARGGFGSSYWYFDVWGQGSLVTVSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSC-GGIDFCMLYNWPICAGGGGGSGGLSGRSDAGSPLGLAGSGGSDIQLTQSPSSLSASVGDRVSITCKASQDVSIAVAWYQQKPGKAPKLLIYSASYRYTGVPDRFSGSGSGTDFTLTISSLQPEDFAVYYCQQHYITPLTFGAGTKVEIKRTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC	PC-22 complex	911	Free	Fab heavy chain linked to C terminus of ScFv light chain	Linear	L	None	Synthetic	Mediates tumor cytotoxicity and T cell activation	N.A.	100 μg/kg	68.97	Hours	248292	Cynomolgus monkeys plasma protease	ELISA	Cynomolgus monkeys plasma	In Vivo	None	US 2021/0062261 W	N.A.
4815	35259149	2022	HGEGTFTSDVSSYLEGQAAKEFIAWLVKGRC	Conjugate 2	31	Free	Ethylene Diamine-modified chondroitin90 (CH) linked with C terminus of GLP-1C using linker C12 , (N-[λ-maleimidododecanoyloxy]-sulfosuccinimide ester (sulfo-LMDS, C12 derived from LMDS)	Linear	L	None	CH-Conjugated Glp-1C Peptide	Antidiabetes	Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration	300 nmol/kg	25.3 (T1/2 Elimination Half Life)	Hours	91080	ICR mice plasma protease	ELISA	ICR mice plasma	In Vivo	https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/	None	EC50 = 9.9 nM
4816	35259149	2022	HGEGTFTSDVSSYLEGQAAKEFIAWLVKGRC	Conjugate 2	31	Free	Ethylene Diamine-modified chondroitin90 (CH) linked with C terminus of GLP-1C using linker C12 , (N-[λ-maleimidododecanoyloxy]-sulfosuccinimide ester (sulfo-LMDS, C12 derived from LMDS)	Linear	L	None	CH-Conjugated Glp-1C Peptide	Antidiabetes	Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration	100 nmol/kg	30.3 (T1/2 Elimination Half Life)	Hours	109080	ICR mice plasma protease	ELISA	ICR mice plasma	In Vivo	https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/	None	EC50 = 9.9 nM
4817	35259149	2022	HGEGTFTSDVSSYLEGQAAKEFIAWLVKGRC	Conjugate 3	31	Free	Ethylene Diamine-modified heparosan (HPN) linked with C terminus of GLP-1C using linker C12 , (N-[λ-maleimidododecanoyloxy]-sulfosuccinimide ester (sulfo-LMDS, C12 derived from LMDS)	Linear	L	None	Hpn-Conjugated Glp-1C Peptide	Antidiabetes	Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration	300 nmol/kg	33.6 (T1/2 Elimination Half Life)	Hours	120960	ICR mice plasma protease	ELISA	ICR mice plasma	In Vivo	https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/	None	EC50 = 7.0 nM
4818	35259149	2022	HGEGTFTSDVSSYLEGQAAKEFIAWLVKGRC	Conjugate 3	31	Free	Ethylene Diamine-modified heparosan (HPN) linked with C terminus of GLP-1C using linker C12 , (N-[λ-maleimidododecanoyloxy]-sulfosuccinimide ester (sulfo-LMDS, C12 derived from LMDS)	Linear	L	None	Hpn-Conjugated Glp-1C Peptide	Antidiabetes	Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration	100 nmol/kg	25.8 (T1/2 Elimination Half Life)	Hours	92880	ICR mice plasma protease	ELISA	ICR mice plasma	In Vivo	https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/	None	EC50 = 7.0 nM
4822	35651477	2022	Y-Aib-EGTFTSDYSI-Aib-LDKIAQKAFVQWLIAGGPSSGAPPPS	LY3298176	39	Free	Amidation	Linear	L	Conjugated to a C20 fatty diacid moiety via a linker connected to the lysine residue at position 20 (C20 diacid-yGlu-(AEEA)2), two non-coded amino acid residues at positions 2 and 13 (Aib, α-amino isobutyric acid)	Fatty Acid Modified Peptide	Antidiabetes	Blood samples for PK assessment of LY3298176 in the SAD part were collected at predose, 8, 24, 48, 72, 96, 120, 168, and 336 hours postdose	0.25 mg	116	Hours	417600	Human plasma protease	HRAM LC/MS	Human plasma	In Vivo	https://pubmed.ncbi.nlm.nih.gov/30473097/	None	GIPR, EC50 nM (cAMP potency) = 0.0224
4823	35651477	2022	Y-Aib-EGTFTSDYSI-Aib-LDKIAQKAFVQWLIAGGPSSGAPPPS	LY3298176	39	Free	Amidation	Linear	L	Conjugated to a C20 fatty diacid moiety via a linker connected to the lysine residue at position 20 (C20 diacid-yGlu-(AEEA)2), two non-coded amino acid residues at positions 2 and 13 (Aib, α-amino isobutyric acid)	Fatty Acid Modified Peptide	Antidiabetes	Blood samples for PK assessment of LY3298176 in the SAD part were collected at predose, 8, 24, 48, 72, 96, 120, 168, and 336 hours postdose	0.5 mg	124	Hours	446400	Human plasma protease	HRAM LC/MS	Human plasma	In Vivo	https://pubmed.ncbi.nlm.nih.gov/30473097/	None	GIPR, EC50 nM (cAMP potency) = 0.0224
4824	35651477	2022	Y-Aib-EGTFTSDYSI-Aib-LDKIAQKAFVQWLIAGGPSSGAPPPS	LY3298176	39	Free	Amidation	Linear	L	Conjugated to a C20 fatty diacid moiety via a linker connected to the lysine residue at position 20 (C20 diacid-yGlu-(AEEA)2), two non-coded amino acid residues at positions 2 and 13 (Aib, α-amino isobutyric acid)	Fatty Acid Modified Peptide	Antidiabetes	Blood samples for PK assessment of LY3298176 in the SAD part were collected at predose, 8, 24, 48, 72, 96, 120, 168, and 336 hours postdose	1 mg	106	Hours	381600	Human plasma protease	HRAM LC/MS	Human plasma	In Vivo	https://pubmed.ncbi.nlm.nih.gov/30473097/	None	GIPR, EC50 nM (cAMP potency) = 0.0224
4825	35651477	2022	Y-Aib-EGTFTSDYSI-Aib-LDKIAQKAFVQWLIAGGPSSGAPPPS	LY3298176	39	Free	Amidation	Linear	L	Conjugated to a C20 fatty diacid moiety via a linker connected to the lysine residue at position 20 (C20 diacid-yGlu-(AEEA)2), two non-coded amino acid residues at positions 2 and 13 (Aib, α-amino isobutyric acid)	Fatty Acid Modified Peptide	Antidiabetes	Blood samples for PK assessment of LY3298176 in the SAD part were collected at predose, 8, 24, 48, 72, 96, 120, 168, and 336 hours postdose	2.5 mg	120	Hours	432000	Human plasma protease	HRAM LC/MS	Human plasma	In Vivo	https://pubmed.ncbi.nlm.nih.gov/30473097/	None	GIPR, EC50 nM (cAMP potency) = 0.0224
4826	35651477	2022	Y-Aib-EGTFTSDYSI-Aib-LDKIAQKAFVQWLIAGGPSSGAPPPS	LY3298176	39	Free	Amidation	Linear	L	Conjugated to a C20 fatty diacid moiety via a linker connected to the lysine residue at position 20 (C20 diacid-yGlu-(AEEA)2), two non-coded amino acid residues at positions 2 and 13 (Aib, α-amino isobutyric acid)	Fatty Acid Modified Peptide	Antidiabetes	Blood samples for PK assessment of LY3298176 in the SAD part were collected at predose, 8, 24, 48, 72, 96, 120, 168, and 336 hours postdose	5 mg	123	Hours	442800	Human plasma protease	HRAM LC/MS	Human plasma	In Vivo	https://pubmed.ncbi.nlm.nih.gov/30473097/	None	GIPR, EC50 nM (cAMP potency) = 0.0224
4827	35651477	2022	Y-Aib-EGTFTSDYSI-Aib-LDKIAQKAFVQWLIAGGPSSGAPPPS	LY3298176	39	Free	Amidation	Linear	L	Conjugated to a C20 fatty diacid moiety via a linker connected to the lysine residue at position 20 (C20 diacid-yGlu-(AEEA)2), two non-coded amino acid residues at positions 2 and 13 (Aib, α-amino isobutyric acid)	Fatty Acid Modified Peptide	Antidiabetes	Blood samples for PK assessment of LY3298176 in the SAD part were collected at predose, 8, 24, 48, 72, 96, 120, 168, and 336 hours postdose	8 mg	111	Hours	399600	Human plasma protease	HRAM LC/MS	Human plasma	In Vivo	https://pubmed.ncbi.nlm.nih.gov/30473097/	None	GIPR, EC50 nM (cAMP potency) = 0.0224
4828	35807558	2022	Y-Aib-EGTFTSDYSI-Aib-LDKIAQKAFVQWLIAGGPSSGAPPPS	Tirzepatide	39	Free	Amidation	Linear	L	C20 fatty diacid moiety at Lys20	Synthetic	Insulinotrophic	N.A.	5 mg	127	Hours	457200	Human plasma protease	N.A.	Human plasma With Multiple Dose (Participants Received 5‐Mg Tirzepatide Weeks 1‐8)(Japanese Participant With Type 2 Diabetes)	In Vivo	https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/	None	N.A.
4829	35807558	2022	Y-Aib-EGTFTSDYSI-Aib-LDKIAQKAFVQWLIAGGPSSGAPPPS	Tirzepatide	39	Free	Amidation	Linear	L	C20 fatty diacid moiety at Lys20	Synthetic	Insulinotrophic	N.A.	10 mg	135	Hours	486000	Human plasma protease	N.A.	Human plasma With Multiple Dose (Participants Received 2.5‐Mg Tirzepatide, Weeks 1‐2; 5 Mg, Weeks 3‐4; 10 Mg, Weeks 5‐8) (Japanese Participant With Type 2 Diabetes)	In Vivo	https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/	None	N.A.
4830	35807558	2022	Y-Aib-EGTFTSDYSI-Aib-LDKIAQKAFVQWLIAGGPSSGAPPPS	Tirzepatide	39	Free	Amidation	Linear	L	C20 fatty diacid moiety at Lys20	Synthetic	Insulinotrophic	N.A.	15 mg	121	Hours	435600	Human plasma protease	N.A.	Human plasma With Multiple Dose(Participants Received 5‐Mg Tirzepatide, Weeks 1‐2; 10 Mg, Weeks 3‐6; 15 Mg, Weeks 7‐8) (Japanese Participant With Type 2 Diabetes)	In Vivo	https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/	None	N.A.
4864	34707178	2021	IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY	PYY3-36 analogues 20	34	Free	Amidation	Linear	L	Fatty acid conjugation at position 22	Derived from PYY	Antiobesity	N.A.	15 nmol/kg	36	Hours	129600	Male göttingen minipigs plasma protease	LC-MS	Male göttingen minipigs plasma	In Vivo	None	None	EC50(nM) = 4 for Y2 receptor
4866	34707178	2021	IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY	PYY3-36 analogues 27	34	Free	Amidation	Linear	L	Fatty acid conjugation at position 29	Derived from PYY	Antiobesity	N.A.	15 nmol/kg	39	Hours	140400	Male göttingen minipigs plasma protease	LC-MS	Male göttingen minipigs plasma	In Vivo	None	None	EC50(nM) = 32 for Y2 receptor
4867	34707178	2021	IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY	PYY3-36 analogues 28	34	Free	Amidation	Linear	L	Fatty acid conjugation at position 30	Derived from PYY	Antiobesity	N.A.	15 nmol/kg	76	Hours	273600	Male göttingen minipigs plasma protease	LC-MS	Male göttingen minipigs plasma	In Vivo	None	None	EC50(nM) = 500 for Y2 receptor
4868	34707178	2021	IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY	PYY3-36 analogues 31	34	Free	Amidation	Linear	L	Fatty acid conjugation at position 33	Derived from PYY	Antiobesity	N.A.	15 nmol/kg	56	Hours	201600	Male göttingen minipigs plasma protease	LC-MS	Male göttingen minipigs plasma	In Vivo	None	None	EC50(nM) = 50 for Y2 receptor
4869	34707178	2021	IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY	PYY3-36 analogues 33	34	Free	Amidation	Linear	L	Fatty acid conjugation at position 35	Derived from PYY	Antiobesity	N.A.	15 nmol/kg	67	Hours	241200	Male göttingen minipigs plasma protease	LC-MS	Male göttingen minipigs plasma	In Vivo	None	None	N.A.
4871	34707178	2021	IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY	PYY3-36 analogues 35	34	Free	Amidation	Linear	L	Fatty acid conjugation at position 30	Derived from PYY	Antiobesity	N.A.	15 nmol/kg	28	Hours	100800	Male göttingen minipigs plasma protease	LC-MS	Male göttingen minipigs plasma	In Vivo	None	None	N.A.
4872	34707178	2021	IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY	PYY3-36 analogues 36	34	Free	Amidation	Linear	L	Fatty acid conjugation at position 30	Derived from PYY	Antiobesity	N.A.	15 nmol/kg	99	Hours	356400	Male göttingen minipigs plasma protease	LC-MS	Male göttingen minipigs plasma	In Vivo	None	None	N.A.
4877	34707178	2021	IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY	PYY3-36 analogues 41	34	Free	Amidation	Linear	L	Fatty acid conjugation at position 30	Derived from PYY	Antiobesity	N.A.	15 nmol/kg	97	Hours	349200	Male göttingen minipigs plasma protease	LC-MS	Male göttingen minipigs plasma	In Vivo	None	None	N.A.
4878	34707178	2021	IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY	PYY3-36 analogues 42	34	Free	Amidation	Linear	L	Fatty acid conjugation at position 30	Derived from PYY	Antiobesity	N.A.	15 nmol/kg	75	Hours	270000	Male göttingen minipigs plasma protease	LC-MS	Male göttingen minipigs plasma	In Vivo	None	None	N.A.
4879	34707178	2021	IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY	PYY3-36 analogues 43	34	Free	Amidation	Linear	L	Fatty acid conjugation at position 30	Derived from PYY	Antiobesity	N.A.	15 nmol/kg	78	Hours	280800	Male göttingen minipigs plasma protease	LC-MS	Male göttingen minipigs plasma	In Vivo	None	None	N.A.
4881	34707178	2021	I-MeArg-PEAPGEDASPEELNRYYASLRHYLNLVTRQRY	PYY3-36 analogues 45	34	Free	Amidation	Linear	L	Fatty acid conjugation at position 4, MeArg4	Derived from PYY	Antiobesity	N.A.	15 nmol/kg	83	Hours	298800	Male göttingen minipigs plasma protease	LC-MS	Male göttingen minipigs plasma	In Vivo	None	None	N.A.
4882	34707178	2021	IKPEAPGEDASPEELNRYYASLRHYLNAKVTRQRY	PYY3-36 analogues 46	35	Free	Amidation	Linear	L	Fatty acid conjugation at position 30	Derived from PYY	Antiobesity	N.A.	15 nmol/kg	84	Hours	302400	Male göttingen minipigs plasma protease	LC-MS	Male göttingen minipigs plasma	In Vivo	None	None	N.A.
4883	34707178	2021	IKPEAPGEDASPEELNRYYASLRHYLNAKVTRQRY	PYY3-36 analogues 47	35	Free	Amidation	Linear	L	Fatty acid conjugation at position 30	Derived from PYY	Antiobesity	N.A.	15 nmol/kg	62	Hours	223200	Male göttingen minipigs plasma protease	LC-MS	Male göttingen minipigs plasma	In Vivo	None	None	N.A.
4884	34707178	2021	IKPEAPGEDASPEELNRYYASLRHYLNNKVTRQRY	PYY3-36 analogues 48	35	Free	Amidation	Linear	L	Fatty acid conjugation at position 30	Derived from PYY	Antiobesity	N.A.	15 nmol/kg	104	Hours	374400	Male göttingen minipigs plasma protease	LC-MS	Male göttingen minipigs plasma	In Vivo	None	None	N.A.
4885	34707178	2021	IKPEAPGEDASPEELNRYYASLRHYLNAKVTRQRY	PYY3-36 analogues 49	35	Free	Amidation	Linear	L	Fatty acid conjugation at position 30, Acetylation at Asn28	Derived from PYY	Antiobesity	N.A.	15 nmol/kg	113	Hours	406800	Male göttingen minipigs plasma protease	LC-MS	Male göttingen minipigs plasma	In Vivo	None	None	N.A.
4887	34707178	2021	IKPEAPGEDASPEELNRYYASLRHYLNANKVTRQRY	PYY3-36 analogues 51	36	Free	Amidation	Linear	L	Fatty acid conjugation at position 30, Acetylation at Asn28	Derived from PYY	Antiobesity	N.A.	15 nmol/kg	114	Hours	410400	Male göttingen minipigs plasma protease	LC-MS	Male göttingen minipigs plasma	In Vivo	None	None	N.A.
4888	34707178	2021	IKPEAPGEDASPEELNRYYASLRHYLNRQKVTRQRY	PYY3-36 analogues 52	36	Free	Amidation	Linear	L	Fatty acid conjugation at position 30, Acetylation at Asn28	Derived from PYY	Antiobesity	N.A.	15 nmol/kg	79	Hours	284400	Male göttingen minipigs plasma protease	LC-MS	Male göttingen minipigs plasma	In Vivo	None	None	EC50(nM) = 30 for Y2 receptor
4901	34450223	2021	HGEGTFTSNVSSYLEGQAAKEFIAWLVKGRG	GLP-2DARPin	31	Genetic fusion of modified GLP-1 to the N-terminal of DARPins through a flexible linke (GGGGS)3 further DARPin linked with another DARPin using PT-linker	Free	Linear	L	FITC labeled	GLP-1 analogs	Antidiabetes	At 0.5, 2, 4, 7, 10, 24, 36, 48 and 72 h after injection, 20 μL of blood was collected	2 mg/mL	52.3 ± 4.6	Hours	188280	Mice plasma protease	Fluorescence assay	Mice plasma	In Vivo	None	None	Glucose-lowering effect of GLP-DARPin was more potent than that of GLP-2DARPin, EC50 of GLP-2DARPin was 0.51 ± 0.04 nM
4911	34254101	2021	GG	Glycylglycine model dipeptide	2	Free	Free	Linear	L	None	Synthetic	N.A.	60 °C and pD 7.4	Equimolar amounts of Hf-NU-1000 and GG	231	Hours	831600	N.A.	1H-NMR	Equimolar amounts of Hf-NU-1000 (Metal-organic Framework)(Hf6O8-based NU-1000) and GG	In Vitro	None	None	A glycylglycine model dipeptide was hydrolysed with a rate constant of kobs = 8.33 × 10−7 s−1
4913	34206631	2021	YGGFL	KK 103	6	N terminal of Tyr linked with NH bond with R1 = Structure given in paper	Free	Linear	L	None	Synthetic	Analgesic	Aliquot (95 µL) was taken at 0, 5, 15, 60, and 300 min	315 µmol/L	37	Hours	133200	Mice plasma protease	UPLC	Mice dipotassium ethylenediaminetetraacetic acid containing pooled plasma	In Vitro	None	None	N.A.
4924	34064291	2021	RGDfK	111In-DOTA-EB-cRGDfK	5	Radiolabelled with 111ln, DOTA, EvansBlue dye	Free	Cyclic	L	None	Synthetic	For Spect imaging and potential theranostic	Blood samples (10 μL) were collected by heart puncture under 2% isoflurane anesthesia at 0.083, 0.5, 2, 4, 24, 48, 72, 96, and 168 h	1.85 MBq	77.3 (Terminal Half Life)	Hours	278280	U-87 mg tumor bearing mice plasma protease	Radioactivity assay	U-87 mg tumor-bearing mice plasma	In Vivo	None	None	IC50(nM) =71.7
4930	33969456	2021	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	Antidiabetes	Blood samples for PK assessment were obtained during the first 9 days of dosing (7–45 samples per subject) and following the last dose on day 10 (16–38 samples per subject)	N.A.	158	Hours	568800	Human plasma protease	LC-MS	Human plasma (Healthy subjects)	In Vivo	https://pmc.ncbi.nlm.nih.gov/articles/PMC8736331/	None	N.A.
4931	33969456	2021	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	Antidiabetes	Blood samples for PK assessment were obtained during the first 9 days of dosing (7–45 samples per subject) and following the last dose on day 10 (16–38 samples per subject)	N.A.	146	Hours	525600	Human plasma protease	LC-MS	Human plasma (Subjects with T2D)	In Vivo	https://pmc.ncbi.nlm.nih.gov/articles/PMC8736331/	None	N.A.
4939	33894838	2021	KCNTATCATQRLAEFLRHSSNNFGPIlpptnvgsntp	Cagrilintide	37	Free	Amidation	Cyclic (Cys-Cys Disulfide Bond)	Mix	LPPTNVGSNTP all D-amino acids, Lipidation on Lys1	amylin analogue	Antiobesity	Blood samples for pharmacokinetic testing were collected before dosing at baseline (week 0) and at weekly visits, and after the last dose (week 19) at 4, 8, 12, 24, 48, 72, 96, 168, 336, 504, 672, 840, and 1008 h after dosing	0·16 − 4·5 mg	159 – 195	Hours	572400	Human plasma protease	N.A.	Human plasma	In Vivo	pubchem CID: 171397054	None	N.A.
4940	33894838	2021	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	Antidiabetes	Blood samples for pharmacokinetic testing were collected before dosing at baseline (week 0) and at weekly visits, and after the last dose (week 19) at 4, 8, 12, 24, 48, 72, 96, 168, 336, 504, 672, 840, and 1008 h after dosing	2·4 mg	145 – 165	Hours	522000	Human plasma protease	N.A.	Human plasma	In Vivo	None	None	N.A.
4945	33822591	2021	KX	PEG−DNP-Lys conjugates 6C	1	DNP	PEG20 KDa, MeO	Linear	L	GDM linker with a two-carbon spacer between the β-carbon and the triazole, Mod = NC−, X = Structure given in paper (n=0)	Synthetic	Increases Half Life	pH 7.4	N.A.	87 (b-Elimination Half-Life)	Hours	313200	N.A.	N.A.	N.A.	In Vitro	None	None	N.A.
4946	33822591	2021	KX	PEG−DNP-Lys conjugates 6C	1	DNP	PEG20 KDa, MeO	Linear	L	GDM linker with a two-carbon spacer between the β-carbon and the triazole, Mod = NC−, X = Structure given in paper (n=0)	Synthetic	Increases Half Life	pH 7.4	N.A.	87 (b-Elimination Half-Life)	Hours	1044000	N.A.	N.A.	N.A.	In Vitro	None	None	N.A.
4947	33822591	2021	KX	PEG−DNP-Lys conjugates 6C	1	DNP	PEG20 KDa, MeO	Linear	L	GDM linker with a two-carbon spacer between the β-carbon and the triazole, Mod = NC−, X = Structure given in paper (n=0)	Synthetic	Increases Half Life	pH 7.4	N.A.	1030 (b-Elimination Half-Life)	Hours	3708000	N.A.	N.A.	N.A.	In Vitro	None	None	N.A.
4948	33822591	2021	KX	PEG−DNP-Lys conjugates 7	1	DNP	PEG20 KDa, MeO	Linear	L	GDM linker with a three-carbon spacer between the β-carbon and the triazole, Mod = PhSO2−, X = Structure given in paper (n=1)	Synthetic	Increases Half Life	pH 7.4	N.A.	256 (b-Elimination Half-Life)	Hours	921600	N.A.	N.A.	N.A.	In Vitro	None	None	N.A.
4949	33822591	2021	KX	PEG−DNP-Lys conjugates 7	1	DNP	PEG20 KDa, MeO	Linear	L	GDM linker with a three-carbon spacer between the β-carbon and the triazole, Mod = PhSO2−, X = Structure given in paper (n=1)	Synthetic	Increases Half Life	pH 7.4	N.A.	724 (b-Elimination Half-Life)	Hours	2606400	N.A.	N.A.	N.A.	In Vitro	None	None	N.A.
4950	33822591	2021	KX	PEG−DNP-Lys conjugates 7	1	DNP	PEG20 KDa, MeO	Linear	L	GDM linker with a three-carbon spacer between the β-carbon and the triazole, Mod = PhSO2−, X = Structure given in paper (n=1)	Synthetic	Increases Half Life	pH 7.4	N.A.	2490 (b-Elimination Half-Life)	Hours	8964000	N.A.	N.A.	N.A.	In Vitro	None	None	N.A.
4951	33822591	2021	KX	PEG−DNP-Lys conjugates 8	1	DNP	PEG20 KDa, MeO	Linear	L	GDM linker with a four-carbon spacer between the β-carbon and the triazole, Mod = MeSO2−, X = Structure given in paper (n=2)	Synthetic	Increases Half Life	pH 7.4	N.A.	1570 (b-Elimination Half-Life)	Hours	5652000	N.A.	N.A.	N.A.	In Vitro	None	None	N.A.
4952	33822591	2021	KX	PEG−DNP-Lys conjugates 8	1	DNP	PEG20 KDa, MeO	Linear	L	GDM linker with a four-carbon spacer between the β-carbon and the triazole, Mod = MeSO2−, X = Structure given in paper (n=2)	Synthetic	Increases Half Life	pH 7.4	N.A.	5310 (b-Elimination Half-Life)	Hours	19116000	N.A.	N.A.	N.A.	In Vitro	None	None	N.A.
4958	33706686	2021	HMSMQEGAVTGEGQAAKEFIAWLVKGRVRADLVGDAFDV	TB01-3	39	Free	Free	Linear	L	None	Synthetic	Antidiabetes	250 ul blood samples were collected via jugular vein cannula at these time points: pre-dose, 0.0833, 0.25, 0.5, 1, 2, 4, 8, 24, 48, 72, 96, 168, 240 and 336 hours post dose.	10 mg/kg	~1	Week	604800	Rats plasma protease	ELISA	Rats plasma	In Vivo	None	None	TB59-2 binds specifically to the GLP-1 R with an EC50 of 15.5 nM, TB-59-2 is a potent agonist in the cAMP assay with a similar EC50 as the GLP-1 7–36 peptide, TB59-2 can also induce the β-arrestin recruitment in GLP-1 R expression cells
4959	33706686	2021	HAEGTFTSNVSSYLEGQAAKEFIAWLVKGR	TB59-2	30	GLP-1 7–36 peptide is linked to the light chain N-terminal of the TB01-2 antibody via a (G4S)x3 linker	Free	Linear	L	None	Synthetic	Antidiabetes	250 ul blood samples were collected via jugular vein cannula at these time points: pre-dose, 0.0833, 0.25, 0.5, 1, 2, 4, 8, 24, 48, 72, 96, 168, 240 and 336 hours post dose.	10 mg/kg	>2	Days	172800	Rats plasma protease	ELISA	Rats plasma	In Vivo	None	None	TB59-2 binds specifically to the GLP-1 R with an EC50 of 15.5 nM, TB-59-2 is a potent agonist in the cAMP assay with a similar EC50 as the GLP-1 7–36 peptide, TB59-2 can also induce the β-arrestin recruitment in GLP-1 R expression cells
4960	33674401	2021	pCl-F-cyclo(c-Y-(D-4-amino-Phe)(Cbm))-KTC)y	177Lu-DOTA-LM3	9	DOTA	Amidation	Cyclic(C-C NC terminal bond)	Mix	DOTA-LM3 conjugation, Cbm = Carbamoyl, 177Lu labeling, pCl-Phe = P-Chloro Phenyalanine	SST analog	Treating Metastatic Neuroendocrine Neoplasms (Nens)	N.A.	7 ± 1 GBq	76	Hours	273600	Whole body	Dosimetry	whole body	In Vivo	None	None	Partial Remission: 17 patients (36.2%), Stable Disease: 23 patients (48.9%), Progressive Disease: 7 patients (14.9%) (The efficacy of the peptide 177Lu-DOTA-LM3 for peptide receptor radionuclide therapy (PRRT) in patients with metastatic neuroendocrine neoplasms )
4961	33674401	2021	pCl-Phe-cyclo(c-Y-(D-4-amino-Phe)(Cbm))-KTC)y	177Lu-DOTA-LM3	9	DOTA	Amidation	Cyclic	Mix	DOTA-LM3 conjugation, Cbm = Carbamoyl, 177Lu labeling, pCl-Phe = P-Chloro Phenyalanine	SST analog	Treating Metastatic Neuroendocrine Neoplasms (Nens)	N.A.	7 ± 1 GBq	92	Hours	331200	Human kidney homogenate protease	Dosimetry	Human kidney homogenate	In Vivo	None	None	Partial Remission: 17 patients (36.2%), Stable Disease: 23 patients (48.9%), Progressive Disease: 7 patients (14.9%) (The efficacy of the peptide 177Lu-DOTA-LM3 for peptide receptor radionuclide therapy (PRRT) in patients with metastatic neuroendocrine neoplasms )
4962	33674401	2021	pCl-Phe-cyclo(c-Y-(D-4-amino-Phe)(Cbm))-KTC)y	177Lu-DOTA-LM3	9	DOTA	Amidation	Cyclic	Mix	DOTA-LM3 conjugation, Cbm = Carbamoyl, 177Lu labeling, pCl-Phe = P-Chloro Phenyalanine	SST analog	Treating Metastatic Neuroendocrine Neoplasms (Nens)	N.A.	7 ± 1 GBq	97	Hours	349200	Human spleen	Dosimetry	Human spleen	In Vivo	None	None	Partial Remission: 17 patients (36.2%), Stable Disease: 23 patients (48.9%), Progressive Disease: 7 patients (14.9%) (The efficacy of the peptide 177Lu-DOTA-LM3 for peptide receptor radionuclide therapy (PRRT) in patients with metastatic neuroendocrine neoplasms )
4963	33674401	2021	pCl-Phe-cyclo(c-Y-(D-4-amino-Phe)(Cbm))-KTC)y	177Lu-DOTA-LM3	9	DOTA	Amidation	Cyclic	Mix	DOTA-LM3 conjugation, Cbm = Carbamoyl, 177Lu labeling, pCl-Phe = P-Chloro Phenyalanine	SST analog	Treating Metastatic Neuroendocrine Neoplasms (Nens)	N.A.	7 ± 1 GBq	111	Hours	399600	Human metastases	Dosimetry	Human metastases	In Vivo	None	None	Partial Remission: 17 patients (36.2%), Stable Disease: 23 patients (48.9%), Progressive Disease: 7 patients (14.9%) (The efficacy of the peptide 177Lu-DOTA-LM3 for peptide receptor radionuclide therapy (PRRT) in patients with metastatic neuroendocrine neoplasms )
4979	33650155	2021	DYKDDDDKDYKDDDDKDYKDDDDKMDTARIAVVGAGVVGLSTAVCISKLVPRCSVTIISDKFTPDTTSDVAAGMLIPHTYPDTPIHTQKQWFRETFNHLFAIANSAEAGDAGVHLVSGWQIFQSTPTEEVPFWADVVLGFRKMTEAELKKFPQYVFGQAFTTLKCECPAYLPWLEKRIKGSGGWTLTRRIEDLWELHPSFDIVVNCSGLGSRQLAGDSKIFPVRGQVLQVQAPWVEHFIRDGSGLTYIYPGTSHVTLGGTRQKGDWNLSPDAENSREILSRCCALEPSLHGACNIREKVGLRPYRPGVRLQTELLARDGQRLPVVHHYGHGSGGISVHWGTALEAARLVSECVHALRTPIPKSNL	3XFLAG-hDASPO_341	365	3XFLAG labelling	Free	Linear	L	None	Found in the hippocampus of female patients affected by Alzheimer's disease	Degradation Of D-Aspartate ( D-Asp)	10 hours	2 μg	≈ 100	Hours	360000	U87 cells lysate protease	Western blotting	U87 cells lysate with cycloheximide (CHX)	In Vivo	None	None	N.A.
4980	33650155	2021	DYKDDDDKDYKDDDDKDYKDDDDKMRPARHWETRFGARDFGGFQDCFFRDRLMDTARIAVVGAGVVGLSTAVCISKLVPRCSVTIISDKFTPDTTSDVAAGMLIPHTYPDTPIHTQKQWFRETFNHLFAIANSAEAGDAGVHLVSGWQIFQSTPTEEVPFWADVVLGFRKMTEAELKKFPQYVFGQAFTTLKCECPAYLPWLEKRIKGSGGWTLTRRIEDLWELHPSFDIVVNCSGLGSRQLAGDSKIFPVRGQVLQVQAPWVEHFIRDGSGLTYIYPGTSHVTLGGTRQKGDWNLSPDAENSREILSRCCALEPSLHGACNIREKVGLRPYRPGVRLQTELLARDGQRLPVVHHYGHGSGGISVHWGTALEAARLVSECVHALRTPIPKSNL	3XFLAG-hDASPO_369	393	3XFLAG labelling	Free	Linear	L	None	Found in the hippocampus of female patients affected by Alzheimer's disease	Degradation Of D-Aspartate ( D-Asp)	10 hours	2 μg	≈ 100	Hours	360000	U87 cells lysate protease	Western blotting	U87 cells lysate with cycloheximide (CHX)	In Vivo	None	None	N.A.
5018	33049303	2021	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRGGSGGGGSGGGGSGGGGSLAEAKVLANRELDKYGVSDYYKNLINNAKTVEGVKALIDEILAALP	GLP-GA3-GS-L3	94	Free	Free	Linear	L	GLP-1 linked with GA3 through L3 linker, FITC labeled	Synthetic	Antidiabetes	8 h at 4 ◦C	50 μg	36.3 ± 7.8	Hours	130680	Mice plasma protease	Fluorescence assay	Mice plasma	In Vivo	None	None	Based on the ELISA method, we also found that the fusion proteins containing GA3, ABD035 and ABDCon showed no significant difference in apparent affinity for HSA (P > 0.50)
5019	33049303	2021	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRGGSGGGGSGGGGSGGGGSLAEAKVLANRELDKYGVSDFYKRLINKAKVEGVEALKLHILAALP	GLPABD035-GS-L3	93	Free	Free	Linear	L	GLP-1 linked with ABD035 through L3 linker, amino acid subsituitions with F,R,K,E,K,L,H, FITC labeled	Synthetic	Antidiabetes	8 h at 4 ◦C	50 μg	31.3 ± 1.0	Hours	112680	Mice plasma protease	Fluorescence assay	Mice plasma	In Vivo	None	None	Based on the ELISA method, we also found that the fusion proteins containing GA3, ABD035 and ABDCon showed no significant difference in apparent affinity for HSA (P > 0.50)
5020	33049303	2021	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRGGSGGGGSGGGGSGGGGSLKEAKEKAIEELKKAGITSDYYFDLINKAKTVEGVNALKDEILKA	GLP-ABDCon-GS-L3	93	Free	Free	Linear	L	GLP-1 linked with ABDCon through L3 linker, amino acid subsituitions with K,E,K,I,E,K,I,T,F,D,K,N,K,K, FITC labeled	Synthetic	Antidiabetes	8 h at 4 ◦C	50 μg	38.3 ± 2.7	Hours	137880	Mice plasma protease	Fluorescence assay	Mice plasma	In Vivo	None	None	Based on the ELISA method, we also found that the fusion proteins containing GA3, ABD035 and ABDCon showed no significant difference in apparent affinity for HSA (P > 0.50)
5027	32078672	2020	MQIELSTCFFLCLLRFCFSATRRYYLGAVELSWDYMQSDLGELPVDARFPPRVPKSFPFNTSVVYKKTLFVEFTDHLFNIAKPRPPWMGLLGPTIQAEVYDTVVITLKNMASHPVSLHAVGVSYWKASEGAEYDDQTSQREKEDDKVFPGGSHTYVWQVLKENGPMASDPLCLTYSYLSHVDLVKDLNSGLIGALLVCREGSLAKEKTQTLHKFILLFAVFDEGKSWHSETKNSLMQDRDAASARAWPKMHTVNGYVNRSLPGLIGCHRKSVYWHVIGMGTTPEVHSIFLEGHTFLVRNHRQASLEISPITFLTAQTLLMDLGQFLLFCHISSHQHDGMEAYVKVDSCPEEPQLRMKNNEEAEDYDDDLTDSEMDVVRFDDDNSPSFIQIRSVAKKHPKTWVHYIAAEEEDWDYAPLVLAPDDRSYKSQYLNNGPQRIGRKYKKVRFMAYTDETFKTREAIQHESGILGPLLYGEVGDTLLIIFKNQASRPYNIYPHGITDVRPLYSRRLPKGVKHLKDFPILPGEIFKYKWTVTVEDGPTKSDPRCLTRYYSSFVNMERDLASGLIGPLLICYKESVDQRGNQIMSDKRNVILFSVFDENRSWYLTENIQRFLPNPAGVQLEDPEFQASNIMHSINGYVFDSLQLSVCLHEVAYWYILSIGAQTDFLSVFFSGYTFKHKMVYEDTLTLFPFSGETVFMSMENPGLWILGCHNSDFRNRGMTALLKVSSCDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSQNGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGTSTEPSEGSAPGTSESATPESGPGTSESATPESGPGTSESATPESGPGSEPATSGSETPGSEPATSGSETPGSPAGSPTSTEEGTSTEPSEGSAPGTSTEPSEGSAPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPASSEITRTTLQSDQEEIDYDDTISVEMKKEDFDIYDEDENQSPRSFQKKTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG/MIPARFAGVLLALALILPGTLCAEGTRGRSSTARCSLFGSDFVNTFDGSMYSFAGYCSYLLAGGCQKRSFSIIGDFQNGKRVSLSVYLGEFFDIHLFVNGTVTQGDQRVSMPYASKGLYLETEAGYYKLSGEAYGFVARIDGSGNFQVLLSDRYFNKTCGLCGNFNIFAEDDFMTQEGTLTSDPYDFANSWALSSGEQWCERASPPSSSCNISSGEMQKGLWEQCQLLKSTSVFARCHPLVDPEPFVALCEKTLCECAGGLECACPALLEYARTCAQEGMVLYGWTDHSACSPVCPAGMEYRQCVSPCARTCQSLHINEMCQERCVDGCSCPEGQLLDEGLCVESTECPCVHSGKRYPPGTSLSRDCNTCICRNSQWICSNEECPGECLVTGQSHFKSFDNRYFTFSGICQYLLARDCQDHSFSIVIETVQCADDRDAVCTRSVTVRLPGLHNSLVKLKHGAGVAMDGQDIQLPLLKGDLRIQHTVTASVRLSYGEDLQMDWDGRGRLLVKLSPVYAGKTCGLCGNYNGNQGDDFLTPSGLAEPRVEDFGNAWKLHGDCQDLQKQHSDPCALNPRMTRFSEEACAVLTSPTFEACHRAVSPLPYLRNCRYDVCSCSDGRECLCGALASYAAACAGRGVRVAWREPGRCELNCPKGQVYLQCGTPCNLTCRSLSYPDEECNEACLEGCFCPPGLYMDERGDCVPKAQCPCYYDGEIFQPEDIFSDHHTMCYCEDGFMHCTMSGVPGSLLPDAVLSSPLSHRSKRSLSCRPPMVKLVCPADNLRAEGLECTKTCQNYDLECMSMGCVSGCLCPPGMVRHENRCVALERCPCFHQGKEYAPGETVKIGCNTCVCRDRKWNCTDHVCDATCSTIGMAHYLTFDGLKYLFPGECQYVLVQDYCGSNPGTFRILVGNKGCSHPSVKCKKRVTILVEGGEIELFDGEVNVKRPMKDETHFEVVESGRYIILLLGKALSVVWDRHLSISVVLKQTYQEKVCGLCGNFDGIQNNDLTSSNLQVEEDPVDFGNSWKVSSQCADTRKVPLDSSPATCHNNIMKQTMVDSSCRILTSDVFQDCNKLVDPEPYLDVCIYDTCSCESIGDCAAFCDTIAAYAHVCAQHGKVVTWRTATLCPQSCEERNLRENGYEAEWRYNSCAPACQVTCQHPEPLACPVQCVEGCHAHCPPGKILDELLQTCVDPEDCPVCEVAGRRFASGKKVTLNPSDPEHCQICHCDVVNLTCEACQEPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGASSDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	rFVIIIFc-VWF-XTEN (construct 4) (BIVV001)	3,611	Free	Free	Linear	L	Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site	Synthetic	Role in clotting	N.A.	25 IU/kg	31	Hours	111600	HemA mice plasma protease	Chromogenic activity assays	HemA mice plasma	In Vivo	PDB id : 5K8D	None	ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar
5028	32078672	2020	MQIELSTCFFLCLLRFCFSATRRYYLGAVELSWDYMQSDLGELPVDARFPPRVPKSFPFNTSVVYKKTLFVEFTDHLFNIAKPRPPWMGLLGPTIQAEVYDTVVITLKNMASHPVSLHAVGVSYWKASEGAEYDDQTSQREKEDDKVFPGGSHTYVWQVLKENGPMASDPLCLTYSYLSHVDLVKDLNSGLIGALLVCREGSLAKEKTQTLHKFILLFAVFDEGKSWHSETKNSLMQDRDAASARAWPKMHTVNGYVNRSLPGLIGCHRKSVYWHVIGMGTTPEVHSIFLEGHTFLVRNHRQASLEISPITFLTAQTLLMDLGQFLLFCHISSHQHDGMEAYVKVDSCPEEPQLRMKNNEEAEDYDDDLTDSEMDVVRFDDDNSPSFIQIRSVAKKHPKTWVHYIAAEEEDWDYAPLVLAPDDRSYKSQYLNNGPQRIGRKYKKVRFMAYTDETFKTREAIQHESGILGPLLYGEVGDTLLIIFKNQASRPYNIYPHGITDVRPLYSRRLPKGVKHLKDFPILPGEIFKYKWTVTVEDGPTKSDPRCLTRYYSSFVNMERDLASGLIGPLLICYKESVDQRGNQIMSDKRNVILFSVFDENRSWYLTENIQRFLPNPAGVQLEDPEFQASNIMHSINGYVFDSLQLSVCLHEVAYWYILSIGAQTDFLSVFFSGYTFKHKMVYEDTLTLFPFSGETVFMSMENPGLWILGCHNSDFRNRGMTALLKVSSCDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSQNGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGTSTEPSEGSAPGTSESATPESGPGTSESATPESGPGTSESATPESGPGSEPATSGSETPGSEPATSGSETPGSPAGSPTSTEEGTSTEPSEGSAPGTSTEPSEGSAPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPASSEITRTTLQSDQEEIDYDDTISVEMKKEDFDIYDEDENQSPRSFQKKTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG/MIPARFAGVLLALALILPGTLCAEGTRGRSSTARCSLFGSDFVNTFDGSMYSFAGYCSYLLAGGCQKRSFSIIGDFQNGKRVSLSVYLGEFFDIHLFVNGTVTQGDQRVSMPYASKGLYLETEAGYYKLSGEAYGFVARIDGSGNFQVLLSDRYFNKTCGLCGNFNIFAEDDFMTQEGTLTSDPYDFANSWALSSGEQWCERASPPSSSCNISSGEMQKGLWEQCQLLKSTSVFARCHPLVDPEPFVALCEKTLCECAGGLECACPALLEYARTCAQEGMVLYGWTDHSACSPVCPAGMEYRQCVSPCARTCQSLHINEMCQERCVDGCSCPEGQLLDEGLCVESTECPCVHSGKRYPPGTSLSRDCNTCICRNSQWICSNEECPGECLVTGQSHFKSFDNRYFTFSGICQYLLARDCQDHSFSIVIETVQCADDRDAVCTRSVTVRLPGLHNSLVKLKHGAGVAMDGQDIQLPLLKGDLRIQHTVTASVRLSYGEDLQMDWDGRGRLLVKLSPVYAGKTCGLCGNYNGNQGDDFLTPSGLAEPRVEDFGNAWKLHGDCQDLQKQHSDPCALNPRMTRFSEEACAVLTSPTFEACHRAVSPLPYLRNCRYDVCSCSDGRECLCGALASYAAACAGRGVRVAWREPGRCELNCPKGQVYLQCGTPCNLTCRSLSYPDEECNEACLEGCFCPPGLYMDERGDCVPKAQCPCYYDGEIFQPEDIFSDHHTMCYCEDGFMHCTMSGVPGSLLPDAVLSSPLSHRSKRSLSCRPPMVKLVCPADNLRAEGLECTKTCQNYDLECMSMGCVSGCLCPPGMVRHENRCVALERCPCFHQGKEYAPGETVKIGCNTCVCRDRKWNCTDHVCDATCSTIGMAHYLTFDGLKYLFPGECQYVLVQDYCGSNPGTFRILVGNKGCSHPSVKCKKRVTILVEGGEIELFDGEVNVKRPMKDETHFEVVESGRYIILLLGKALSVVWDRHLSISVVLKQTYQEKVCGLCGNFDGIQNNDLTSSNLQVEEDPVDFGNSWKVSSQCADTRKVPLDSSPATCHNNIMKQTMVDSSCRILTSDVFQDCNKLVDPEPYLDVCIYDTCSCESIGDCAAFCDTIAAYAHVCAQHGKVVTWRTATLCPQSCEERNLRENGYEAEWRYNSCAPACQVTCQHPEPLACPVQCVEGCHAHCPPGKILDELLQTCVDPEDCPVCEVAGRRFASGKKVTLNPSDPEHCQICHCDVVNLTCEACQEPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGASSDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	rFVIIIFc-VWF-XTEN (construct 4) (BIVV001)	3,611	Free	Free	Linear	L	Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site	Synthetic	Role in clotting	N.A.	50 IU/kg	30	Hours	108000	HemA mice plasma protease	Chromogenic activity assays	HemA mice plasma	In Vivo	PDB id : 5K8D	None	ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar
5029	32078672	2020	MQIELSTCFFLCLLRFCFSATRRYYLGAVELSWDYMQSDLGELPVDARFPPRVPKSFPFNTSVVYKKTLFVEFTDHLFNIAKPRPPWMGLLGPTIQAEVYDTVVITLKNMASHPVSLHAVGVSYWKASEGAEYDDQTSQREKEDDKVFPGGSHTYVWQVLKENGPMASDPLCLTYSYLSHVDLVKDLNSGLIGALLVCREGSLAKEKTQTLHKFILLFAVFDEGKSWHSETKNSLMQDRDAASARAWPKMHTVNGYVNRSLPGLIGCHRKSVYWHVIGMGTTPEVHSIFLEGHTFLVRNHRQASLEISPITFLTAQTLLMDLGQFLLFCHISSHQHDGMEAYVKVDSCPEEPQLRMKNNEEAEDYDDDLTDSEMDVVRFDDDNSPSFIQIRSVAKKHPKTWVHYIAAEEEDWDYAPLVLAPDDRSYKSQYLNNGPQRIGRKYKKVRFMAYTDETFKTREAIQHESGILGPLLYGEVGDTLLIIFKNQASRPYNIYPHGITDVRPLYSRRLPKGVKHLKDFPILPGEIFKYKWTVTVEDGPTKSDPRCLTRYYSSFVNMERDLASGLIGPLLICYKESVDQRGNQIMSDKRNVILFSVFDENRSWYLTENIQRFLPNPAGVQLEDPEFQASNIMHSINGYVFDSLQLSVCLHEVAYWYILSIGAQTDFLSVFFSGYTFKHKMVYEDTLTLFPFSGETVFMSMENPGLWILGCHNSDFRNRGMTALLKVSSCDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSQNGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGTSTEPSEGSAPGTSESATPESGPGTSESATPESGPGTSESATPESGPGSEPATSGSETPGSEPATSGSETPGSPAGSPTSTEEGTSTEPSEGSAPGTSTEPSEGSAPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPASSEITRTTLQSDQEEIDYDDTISVEMKKEDFDIYDEDENQSPRSFQKKTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG/MIPARFAGVLLALALILPGTLCAEGTRGRSSTARCSLFGSDFVNTFDGSMYSFAGYCSYLLAGGCQKRSFSIIGDFQNGKRVSLSVYLGEFFDIHLFVNGTVTQGDQRVSMPYASKGLYLETEAGYYKLSGEAYGFVARIDGSGNFQVLLSDRYFNKTCGLCGNFNIFAEDDFMTQEGTLTSDPYDFANSWALSSGEQWCERASPPSSSCNISSGEMQKGLWEQCQLLKSTSVFARCHPLVDPEPFVALCEKTLCECAGGLECACPALLEYARTCAQEGMVLYGWTDHSACSPVCPAGMEYRQCVSPCARTCQSLHINEMCQERCVDGCSCPEGQLLDEGLCVESTECPCVHSGKRYPPGTSLSRDCNTCICRNSQWICSNEECPGECLVTGQSHFKSFDNRYFTFSGICQYLLARDCQDHSFSIVIETVQCADDRDAVCTRSVTVRLPGLHNSLVKLKHGAGVAMDGQDIQLPLLKGDLRIQHTVTASVRLSYGEDLQMDWDGRGRLLVKLSPVYAGKTCGLCGNYNGNQGDDFLTPSGLAEPRVEDFGNAWKLHGDCQDLQKQHSDPCALNPRMTRFSEEACAVLTSPTFEACHRAVSPLPYLRNCRYDVCSCSDGRECLCGALASYAAACAGRGVRVAWREPGRCELNCPKGQVYLQCGTPCNLTCRSLSYPDEECNEACLEGCFCPPGLYMDERGDCVPKAQCPCYYDGEIFQPEDIFSDHHTMCYCEDGFMHCTMSGVPGSLLPDAVLSSPLSHRSKRSLSCRPPMVKLVCPADNLRAEGLECTKTCQNYDLECMSMGCVSGCLCPPGMVRHENRCVALERCPCFHQGKEYAPGETVKIGCNTCVCRDRKWNCTDHVCDATCSTIGMAHYLTFDGLKYLFPGECQYVLVQDYCGSNPGTFRILVGNKGCSHPSVKCKKRVTILVEGGEIELFDGEVNVKRPMKDETHFEVVESGRYIILLLGKALSVVWDRHLSISVVLKQTYQEKVCGLCGNFDGIQNNDLTSSNLQVEEDPVDFGNSWKVSSQCADTRKVPLDSSPATCHNNIMKQTMVDSSCRILTSDVFQDCNKLVDPEPYLDVCIYDTCSCESIGDCAAFCDTIAAYAHVCAQHGKVVTWRTATLCPQSCEERNLRENGYEAEWRYNSCAPACQVTCQHPEPLACPVQCVEGCHAHCPPGKILDELLQTCVDPEDCPVCEVAGRRFASGKKVTLNPSDPEHCQICHCDVVNLTCEACQEPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGASSDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	rFVIIIFc-VWF-XTEN (construct 4) (BIVV001)	3,611	Free	Free	Linear	L	Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site	Synthetic	Role in clotting	N.A.	100 IU/kg	25	Hours	90000	HemA mice plasma protease	Chromogenic activity assays	HemA mice plasma	In Vivo	PDB id : 5K8D	None	ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar
5030	32078672	2020	MQIELSTCFFLCLLRFCFSATRRYYLGAVELSWDYMQSDLGELPVDARFPPRVPKSFPFNTSVVYKKTLFVEFTDHLFNIAKPRPPWMGLLGPTIQAEVYDTVVITLKNMASHPVSLHAVGVSYWKASEGAEYDDQTSQREKEDDKVFPGGSHTYVWQVLKENGPMASDPLCLTYSYLSHVDLVKDLNSGLIGALLVCREGSLAKEKTQTLHKFILLFAVFDEGKSWHSETKNSLMQDRDAASARAWPKMHTVNGYVNRSLPGLIGCHRKSVYWHVIGMGTTPEVHSIFLEGHTFLVRNHRQASLEISPITFLTAQTLLMDLGQFLLFCHISSHQHDGMEAYVKVDSCPEEPQLRMKNNEEAEDYDDDLTDSEMDVVRFDDDNSPSFIQIRSVAKKHPKTWVHYIAAEEEDWDYAPLVLAPDDRSYKSQYLNNGPQRIGRKYKKVRFMAYTDETFKTREAIQHESGILGPLLYGEVGDTLLIIFKNQASRPYNIYPHGITDVRPLYSRRLPKGVKHLKDFPILPGEIFKYKWTVTVEDGPTKSDPRCLTRYYSSFVNMERDLASGLIGPLLICYKESVDQRGNQIMSDKRNVILFSVFDENRSWYLTENIQRFLPNPAGVQLEDPEFQASNIMHSINGYVFDSLQLSVCLHEVAYWYILSIGAQTDFLSVFFSGYTFKHKMVYEDTLTLFPFSGETVFMSMENPGLWILGCHNSDFRNRGMTALLKVSSCDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSQNGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGTSTEPSEGSAPGTSESATPESGPGTSESATPESGPGTSESATPESGPGSEPATSGSETPGSEPATSGSETPGSPAGSPTSTEEGTSTEPSEGSAPGTSTEPSEGSAPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPASSEITRTTLQSDQEEIDYDDTISVEMKKEDFDIYDEDENQSPRSFQKKTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG/MIPARFAGVLLALALILPGTLCAEGTRGRSSTARCSLFGSDFVNTFDGSMYSFAGYCSYLLAGGCQKRSFSIIGDFQNGKRVSLSVYLGEFFDIHLFVNGTVTQGDQRVSMPYASKGLYLETEAGYYKLSGEAYGFVARIDGSGNFQVLLSDRYFNKTCGLCGNFNIFAEDDFMTQEGTLTSDPYDFANSWALSSGEQWCERASPPSSSCNISSGEMQKGLWEQCQLLKSTSVFARCHPLVDPEPFVALCEKTLCECAGGLECACPALLEYARTCAQEGMVLYGWTDHSACSPVCPAGMEYRQCVSPCARTCQSLHINEMCQERCVDGCSCPEGQLLDEGLCVESTECPCVHSGKRYPPGTSLSRDCNTCICRNSQWICSNEECPGECLVTGQSHFKSFDNRYFTFSGICQYLLARDCQDHSFSIVIETVQCADDRDAVCTRSVTVRLPGLHNSLVKLKHGAGVAMDGQDIQLPLLKGDLRIQHTVTASVRLSYGEDLQMDWDGRGRLLVKLSPVYAGKTCGLCGNYNGNQGDDFLTPSGLAEPRVEDFGNAWKLHGDCQDLQKQHSDPCALNPRMTRFSEEACAVLTSPTFEACHRAVSPLPYLRNCRYDVCSCSDGRECLCGALASYAAACAGRGVRVAWREPGRCELNCPKGQVYLQCGTPCNLTCRSLSYPDEECNEACLEGCFCPPGLYMDERGDCVPKAQCPCYYDGEIFQPEDIFSDHHTMCYCEDGFMHCTMSGVPGSLLPDAVLSSPLSHRSKRSLSCRPPMVKLVCPADNLRAEGLECTKTCQNYDLECMSMGCVSGCLCPPGMVRHENRCVALERCPCFHQGKEYAPGETVKIGCNTCVCRDRKWNCTDHVCDATCSTIGMAHYLTFDGLKYLFPGECQYVLVQDYCGSNPGTFRILVGNKGCSHPSVKCKKRVTILVEGGEIELFDGEVNVKRPMKDETHFEVVESGRYIILLLGKALSVVWDRHLSISVVLKQTYQEKVCGLCGNFDGIQNNDLTSSNLQVEEDPVDFGNSWKVSSQCADTRKVPLDSSPATCHNNIMKQTMVDSSCRILTSDVFQDCNKLVDPEPYLDVCIYDTCSCESIGDCAAFCDTIAAYAHVCAQHGKVVTWRTATLCPQSCEERNLRENGYEAEWRYNSCAPACQVTCQHPEPLACPVQCVEGCHAHCPPGKILDELLQTCVDPEDCPVCEVAGRRFASGKKVTLNPSDPEHCQICHCDVVNLTCEACQEPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGASSDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	rFVIIIFc-VWF-XTEN (construct 4) (BIVV001)	3,611	Free	Free	Linear	L	Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site	Synthetic	Role in clotting	N.A.	100 IU/kg	32.7	Hours	117720	Cynomolgus monkeys plasma protease	Chromogenic activity assays	Cynomolgus monkeys plasma	In Vivo	PDB id : 5K8D	None	ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar
5031	32078672	2020	MQIELSTCFFLCLLRFCFSATRRYYLGAVELSWDYMQSDLGELPVDARFPPRVPKSFPFNTSVVYKKTLFVEFTDHLFNIAKPRPPWMGLLGPTIQAEVYDTVVITLKNMASHPVSLHAVGVSYWKASEGAEYDDQTSQREKEDDKVFPGGSHTYVWQVLKENGPMASDPLCLTYSYLSHVDLVKDLNSGLIGALLVCREGSLAKEKTQTLHKFILLFAVFDEGKSWHSETKNSLMQDRDAASARAWPKMHTVNGYVNRSLPGLIGCHRKSVYWHVIGMGTTPEVHSIFLEGHTFLVRNHRQASLEISPITFLTAQTLLMDLGQFLLFCHISSHQHDGMEAYVKVDSCPEEPQLRMKNNEEAEDYDDDLTDSEMDVVRFDDDNSPSFIQIRSVAKKHPKTWVHYIAAEEEDWDYAPLVLAPDDRSYKSQYLNNGPQRIGRKYKKVRFMAYTDETFKTREAIQHESGILGPLLYGEVGDTLLIIFKNQASRPYNIYPHGITDVRPLYSRRLPKGVKHLKDFPILPGEIFKYKWTVTVEDGPTKSDPRCLTRYYSSFVNMERDLASGLIGPLLICYKESVDQRGNQIMSDKRNVILFSVFDENRSWYLTENIQRFLPNPAGVQLEDPEFQASNIMHSINGYVFDSLQLSVCLHEVAYWYILSIGAQTDFLSVFFSGYTFKHKMVYEDTLTLFPFSGETVFMSMENPGLWILGCHNSDFRNRGMTALLKVSSCDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSQNGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGTSTEPSEGSAPGTSESATPESGPGTSESATPESGPGTSESATPESGPGSEPATSGSETPGSEPATSGSETPGSPAGSPTSTEEGTSTEPSEGSAPGTSTEPSEGSAPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPASSEITRTTLQSDQEEIDYDDTISVEMKKEDFDIYDEDENQSPRSFQKKTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG/MIPARFAGVLLALALILPGTLCAEGTRGRSSTARCSLFGSDFVNTFDGSMYSFAGYCSYLLAGGCQKRSFSIIGDFQNGKRVSLSVYLGEFFDIHLFVNGTVTQGDQRVSMPYASKGLYLETEAGYYKLSGEAYGFVARIDGSGNFQVLLSDRYFNKTCGLCGNFNIFAEDDFMTQEGTLTSDPYDFANSWALSSGEQWCERASPPSSSCNISSGEMQKGLWEQCQLLKSTSVFARCHPLVDPEPFVALCEKTLCECAGGLECACPALLEYARTCAQEGMVLYGWTDHSACSPVCPAGMEYRQCVSPCARTCQSLHINEMCQERCVDGCSCPEGQLLDEGLCVESTECPCVHSGKRYPPGTSLSRDCNTCICRNSQWICSNEECPGECLVTGQSHFKSFDNRYFTFSGICQYLLARDCQDHSFSIVIETVQCADDRDAVCTRSVTVRLPGLHNSLVKLKHGAGVAMDGQDIQLPLLKGDLRIQHTVTASVRLSYGEDLQMDWDGRGRLLVKLSPVYAGKTCGLCGNYNGNQGDDFLTPSGLAEPRVEDFGNAWKLHGDCQDLQKQHSDPCALNPRMTRFSEEACAVLTSPTFEACHRAVSPLPYLRNCRYDVCSCSDGRECLCGALASYAAACAGRGVRVAWREPGRCELNCPKGQVYLQCGTPCNLTCRSLSYPDEECNEACLEGCFCPPGLYMDERGDCVPKAQCPCYYDGEIFQPEDIFSDHHTMCYCEDGFMHCTMSGVPGSLLPDAVLSSPLSHRSKRSLSCRPPMVKLVCPADNLRAEGLECTKTCQNYDLECMSMGCVSGCLCPPGMVRHENRCVALERCPCFHQGKEYAPGETVKIGCNTCVCRDRKWNCTDHVCDATCSTIGMAHYLTFDGLKYLFPGECQYVLVQDYCGSNPGTFRILVGNKGCSHPSVKCKKRVTILVEGGEIELFDGEVNVKRPMKDETHFEVVESGRYIILLLGKALSVVWDRHLSISVVLKQTYQEKVCGLCGNFDGIQNNDLTSSNLQVEEDPVDFGNSWKVSSQCADTRKVPLDSSPATCHNNIMKQTMVDSSCRILTSDVFQDCNKLVDPEPYLDVCIYDTCSCESIGDCAAFCDTIAAYAHVCAQHGKVVTWRTATLCPQSCEERNLRENGYEAEWRYNSCAPACQVTCQHPEPLACPVQCVEGCHAHCPPGKILDELLQTCVDPEDCPVCEVAGRRFASGKKVTLNPSDPEHCQICHCDVVNLTCEACQEPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGASSDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	rFVIIIFc-VWF-XTEN (construct 4) (BIVV001)	3,611	Free	Free	Linear	L	Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site	Synthetic	Role in clotting	N.A.	300 IU/kg	33.6	Hours	120960	Cynomolgus monkeys plasma protease	Chromogenic activity assays	Cynomolgus monkeys plasma	In Vivo	PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf	None	ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar
5032	32078672	2020	MQIELSTCFFLCLLRFCFSATRRYYLGAVELSWDYMQSDLGELPVDARFPPRVPKSFPFNTSVVYKKTLFVEFTDHLFNIAKPRPPWMGLLGPTIQAEVYDTVVITLKNMASHPVSLHAVGVSYWKASEGAEYDDQTSQREKEDDKVFPGGSHTYVWQVLKENGPMASDPLCLTYSYLSHVDLVKDLNSGLIGALLVCREGSLAKEKTQTLHKFILLFAVFDEGKSWHSETKNSLMQDRDAASARAWPKMHTVNGYVNRSLPGLIGCHRKSVYWHVIGMGTTPEVHSIFLEGHTFLVRNHRQASLEISPITFLTAQTLLMDLGQFLLFCHISSHQHDGMEAYVKVDSCPEEPQLRMKNNEEAEDYDDDLTDSEMDVVRFDDDNSPSFIQIRSVAKKHPKTWVHYIAAEEEDWDYAPLVLAPDDRSYKSQYLNNGPQRIGRKYKKVRFMAYTDETFKTREAIQHESGILGPLLYGEVGDTLLIIFKNQASRPYNIYPHGITDVRPLYSRRLPKGVKHLKDFPILPGEIFKYKWTVTVEDGPTKSDPRCLTRYYSSFVNMERDLASGLIGPLLICYKESVDQRGNQIMSDKRNVILFSVFDENRSWYLTENIQRFLPNPAGVQLEDPEFQASNIMHSINGYVFDSLQLSVCLHEVAYWYILSIGAQTDFLSVFFSGYTFKHKMVYEDTLTLFPFSGETVFMSMENPGLWILGCHNSDFRNRGMTALLKVSSCDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSQNGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGTSTEPSEGSAPGTSESATPESGPGTSESATPESGPGTSESATPESGPGSEPATSGSETPGSEPATSGSETPGSPAGSPTSTEEGTSTEPSEGSAPGTSTEPSEGSAPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPASSEITRTTLQSDQEEIDYDDTISVEMKKEDFDIYDEDENQSPRSFQKKTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG/MIPARFAGVLLALALILPGTLCAEGTRGRSSTARCSLFGSDFVNTFDGSMYSFAGYCSYLLAGGCQKRSFSIIGDFQNGKRVSLSVYLGEFFDIHLFVNGTVTQGDQRVSMPYASKGLYLETEAGYYKLSGEAYGFVARIDGSGNFQVLLSDRYFNKTCGLCGNFNIFAEDDFMTQEGTLTSDPYDFANSWALSSGEQWCERASPPSSSCNISSGEMQKGLWEQCQLLKSTSVFARCHPLVDPEPFVALCEKTLCECAGGLECACPALLEYARTCAQEGMVLYGWTDHSACSPVCPAGMEYRQCVSPCARTCQSLHINEMCQERCVDGCSCPEGQLLDEGLCVESTECPCVHSGKRYPPGTSLSRDCNTCICRNSQWICSNEECPGECLVTGQSHFKSFDNRYFTFSGICQYLLARDCQDHSFSIVIETVQCADDRDAVCTRSVTVRLPGLHNSLVKLKHGAGVAMDGQDIQLPLLKGDLRIQHTVTASVRLSYGEDLQMDWDGRGRLLVKLSPVYAGKTCGLCGNYNGNQGDDFLTPSGLAEPRVEDFGNAWKLHGDCQDLQKQHSDPCALNPRMTRFSEEACAVLTSPTFEACHRAVSPLPYLRNCRYDVCSCSDGRECLCGALASYAAACAGRGVRVAWREPGRCELNCPKGQVYLQCGTPCNLTCRSLSYPDEECNEACLEGCFCPPGLYMDERGDCVPKAQCPCYYDGEIFQPEDIFSDHHTMCYCEDGFMHCTMSGVPGSLLPDAVLSSPLSHRSKRSLSCRPPMVKLVCPADNLRAEGLECTKTCQNYDLECMSMGCVSGCLCPPGMVRHENRCVALERCPCFHQGKEYAPGETVKIGCNTCVCRDRKWNCTDHVCDATCSTIGMAHYLTFDGLKYLFPGECQYVLVQDYCGSNPGTFRILVGNKGCSHPSVKCKKRVTILVEGGEIELFDGEVNVKRPMKDETHFEVVESGRYIILLLGKALSVVWDRHLSISVVLKQTYQEKVCGLCGNFDGIQNNDLTSSNLQVEEDPVDFGNSWKVSSQCADTRKVPLDSSPATCHNNIMKQTMVDSSCRILTSDVFQDCNKLVDPEPYLDVCIYDTCSCESIGDCAAFCDTIAAYAHVCAQHGKVVTWRTATLCPQSCEERNLRENGYEAEWRYNSCAPACQVTCQHPEPLACPVQCVEGCHAHCPPGKILDELLQTCVDPEDCPVCEVAGRRFASGKKVTLNPSDPEHCQICHCDVVNLTCEACQEPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGASSDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	rFVIIIFc-VWF-XTEN (construct 4) (BIVV001)	3,611	Free	Free	Linear	L	Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site	Synthetic	Role In Clotting	N.A.	100 IU/kg	29.3	Hours	105480	Cynomolgus monkeys plasma protease	ELISA	Cynomolgus monkeys plasma	In Vivo	PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf	None	ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar
5033	32078672	2020	MQIELSTCFFLCLLRFCFSATRRYYLGAVELSWDYMQSDLGELPVDARFPPRVPKSFPFNTSVVYKKTLFVEFTDHLFNIAKPRPPWMGLLGPTIQAEVYDTVVITLKNMASHPVSLHAVGVSYWKASEGAEYDDQTSQREKEDDKVFPGGSHTYVWQVLKENGPMASDPLCLTYSYLSHVDLVKDLNSGLIGALLVCREGSLAKEKTQTLHKFILLFAVFDEGKSWHSETKNSLMQDRDAASARAWPKMHTVNGYVNRSLPGLIGCHRKSVYWHVIGMGTTPEVHSIFLEGHTFLVRNHRQASLEISPITFLTAQTLLMDLGQFLLFCHISSHQHDGMEAYVKVDSCPEEPQLRMKNNEEAEDYDDDLTDSEMDVVRFDDDNSPSFIQIRSVAKKHPKTWVHYIAAEEEDWDYAPLVLAPDDRSYKSQYLNNGPQRIGRKYKKVRFMAYTDETFKTREAIQHESGILGPLLYGEVGDTLLIIFKNQASRPYNIYPHGITDVRPLYSRRLPKGVKHLKDFPILPGEIFKYKWTVTVEDGPTKSDPRCLTRYYSSFVNMERDLASGLIGPLLICYKESVDQRGNQIMSDKRNVILFSVFDENRSWYLTENIQRFLPNPAGVQLEDPEFQASNIMHSINGYVFDSLQLSVCLHEVAYWYILSIGAQTDFLSVFFSGYTFKHKMVYEDTLTLFPFSGETVFMSMENPGLWILGCHNSDFRNRGMTALLKVSSCDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSQNGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGTSTEPSEGSAPGTSESATPESGPGTSESATPESGPGTSESATPESGPGSEPATSGSETPGSEPATSGSETPGSPAGSPTSTEEGTSTEPSEGSAPGTSTEPSEGSAPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPASSEITRTTLQSDQEEIDYDDTISVEMKKEDFDIYDEDENQSPRSFQKKTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG/MIPARFAGVLLALALILPGTLCAEGTRGRSSTARCSLFGSDFVNTFDGSMYSFAGYCSYLLAGGCQKRSFSIIGDFQNGKRVSLSVYLGEFFDIHLFVNGTVTQGDQRVSMPYASKGLYLETEAGYYKLSGEAYGFVARIDGSGNFQVLLSDRYFNKTCGLCGNFNIFAEDDFMTQEGTLTSDPYDFANSWALSSGEQWCERASPPSSSCNISSGEMQKGLWEQCQLLKSTSVFARCHPLVDPEPFVALCEKTLCECAGGLECACPALLEYARTCAQEGMVLYGWTDHSACSPVCPAGMEYRQCVSPCARTCQSLHINEMCQERCVDGCSCPEGQLLDEGLCVESTECPCVHSGKRYPPGTSLSRDCNTCICRNSQWICSNEECPGECLVTGQSHFKSFDNRYFTFSGICQYLLARDCQDHSFSIVIETVQCADDRDAVCTRSVTVRLPGLHNSLVKLKHGAGVAMDGQDIQLPLLKGDLRIQHTVTASVRLSYGEDLQMDWDGRGRLLVKLSPVYAGKTCGLCGNYNGNQGDDFLTPSGLAEPRVEDFGNAWKLHGDCQDLQKQHSDPCALNPRMTRFSEEACAVLTSPTFEACHRAVSPLPYLRNCRYDVCSCSDGRECLCGALASYAAACAGRGVRVAWREPGRCELNCPKGQVYLQCGTPCNLTCRSLSYPDEECNEACLEGCFCPPGLYMDERGDCVPKAQCPCYYDGEIFQPEDIFSDHHTMCYCEDGFMHCTMSGVPGSLLPDAVLSSPLSHRSKRSLSCRPPMVKLVCPADNLRAEGLECTKTCQNYDLECMSMGCVSGCLCPPGMVRHENRCVALERCPCFHQGKEYAPGETVKIGCNTCVCRDRKWNCTDHVCDATCSTIGMAHYLTFDGLKYLFPGECQYVLVQDYCGSNPGTFRILVGNKGCSHPSVKCKKRVTILVEGGEIELFDGEVNVKRPMKDETHFEVVESGRYIILLLGKALSVVWDRHLSISVVLKQTYQEKVCGLCGNFDGIQNNDLTSSNLQVEEDPVDFGNSWKVSSQCADTRKVPLDSSPATCHNNIMKQTMVDSSCRILTSDVFQDCNKLVDPEPYLDVCIYDTCSCESIGDCAAFCDTIAAYAHVCAQHGKVVTWRTATLCPQSCEERNLRENGYEAEWRYNSCAPACQVTCQHPEPLACPVQCVEGCHAHCPPGKILDELLQTCVDPEDCPVCEVAGRRFASGKKVTLNPSDPEHCQICHCDVVNLTCEACQEPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGASSDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	rFVIIIFc-VWF-XTEN (construct 4) (BIVV001)	3,611	Free	Free	Linear	L	Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site	Synthetic	Role In Clotting	N.A.	300 IU/kg	34	Hours	122400	Cynomolgus monkeys plasma protease	ELISA	Cynomolgus monkeys plasma	In Vivo	PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf	None	ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar
5034	32078672	2020	MQIELSTCFFLCLLRFCFSATRRYYLGAVELSWDYMQSDLGELPVDARFPPRVPKSFPFNTSVVYKKTLFVEFTDHLFNIAKPRPPWMGLLGPTIQAEVYDTVVITLKNMASHPVSLHAVGVSYWKASEGAEYDDQTSQREKEDDKVFPGGSHTYVWQVLKENGPMASDPLCLTYSYLSHVDLVKDLNSGLIGALLVCREGSLAKEKTQTLHKFILLFAVFDEGKSWHSETKNSLMQDRDAASARAWPKMHTVNGYVNRSLPGLIGCHRKSVYWHVIGMGTTPEVHSIFLEGHTFLVRNHRQASLEISPITFLTAQTLLMDLGQFLLFCHISSHQHDGMEAYVKVDSCPEEPQLRMKNNEEAEDYDDDLTDSEMDVVRFDDDNSPSFIQIRSVAKKHPKTWVHYIAAEEEDWDYAPLVLAPDDRSYKSQYLNNGPQRIGRKYKKVRFMAYTDETFKTREAIQHESGILGPLLYGEVGDTLLIIFKNQASRPYNIYPHGITDVRPLYSRRLPKGVKHLKDFPILPGEIFKYKWTVTVEDGPTKSDPRCLTRYYSSFVNMERDLASGLIGPLLICYKESVDQRGNQIMSDKRNVILFSVFDENRSWYLTENIQRFLPNPAGVQLEDPEFQASNIMHSINGYVFDSLQLSVCLHEVAYWYILSIGAQTDFLSVFFSGYTFKHKMVYEDTLTLFPFSGETVFMSMENPGLWILGCHNSDFRNRGMTALLKVSSCDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSQNGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGTSTEPSEGSAPGTSESATPESGPGTSESATPESGPGTSESATPESGPGSEPATSGSETPGSEPATSGSETPGSPAGSPTSTEEGTSTEPSEGSAPGTSTEPSEGSAPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPASSEITRTTLQSDQEEIDYDDTISVEMKKEDFDIYDEDENQSPRSFQKKTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG/MIPARFAGVLLALALILPGTLCAEGTRGRSSTARCSLFGSDFVNTFDGSMYSFAGYCSYLLAGGCQKRSFSIIGDFQNGKRVSLSVYLGEFFDIHLFVNGTVTQGDQRVSMPYASKGLYLETEAGYYKLSGEAYGFVARIDGSGNFQVLLSDRYFNKTCGLCGNFNIFAEDDFMTQEGTLTSDPYDFANSWALSSGEQWCERASPPSSSCNISSGEMQKGLWEQCQLLKSTSVFARCHPLVDPEPFVALCEKTLCECAGGLECACPALLEYARTCAQEGMVLYGWTDHSACSPVCPAGMEYRQCVSPCARTCQSLHINEMCQERCVDGCSCPEGQLLDEGLCVESTECPCVHSGKRYPPGTSLSRDCNTCICRNSQWICSNEECPGECLVTGQSHFKSFDNRYFTFSGICQYLLARDCQDHSFSIVIETVQCADDRDAVCTRSVTVRLPGLHNSLVKLKHGAGVAMDGQDIQLPLLKGDLRIQHTVTASVRLSYGEDLQMDWDGRGRLLVKLSPVYAGKTCGLCGNYNGNQGDDFLTPSGLAEPRVEDFGNAWKLHGDCQDLQKQHSDPCALNPRMTRFSEEACAVLTSPTFEACHRAVSPLPYLRNCRYDVCSCSDGRECLCGALASYAAACAGRGVRVAWREPGRCELNCPKGQVYLQCGTPCNLTCRSLSYPDEECNEACLEGCFCPPGLYMDERGDCVPKAQCPCYYDGEIFQPEDIFSDHHTMCYCEDGFMHCTMSGVPGSLLPDAVLSSPLSHRSKRSLSCRPPMVKLVCPADNLRAEGLECTKTCQNYDLECMSMGCVSGCLCPPGMVRHENRCVALERCPCFHQGKEYAPGETVKIGCNTCVCRDRKWNCTDHVCDATCSTIGMAHYLTFDGLKYLFPGECQYVLVQDYCGSNPGTFRILVGNKGCSHPSVKCKKRVTILVEGGEIELFDGEVNVKRPMKDETHFEVVESGRYIILLLGKALSVVWDRHLSISVVLKQTYQEKVCGLCGNFDGIQNNDLTSSNLQVEEDPVDFGNSWKVSSQCADTRKVPLDSSPATCHNNIMKQTMVDSSCRILTSDVFQDCNKLVDPEPYLDVCIYDTCSCESIGDCAAFCDTIAAYAHVCAQHGKVVTWRTATLCPQSCEERNLRENGYEAEWRYNSCAPACQVTCQHPEPLACPVQCVEGCHAHCPPGKILDELLQTCVDPEDCPVCEVAGRRFASGKKVTLNPSDPEHCQICHCDVVNLTCEACQEPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGASSDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	rFVIIIFc-VWF-XTEN (construct 4) (BIVV001)	3,611	Free	Free	Linear	L	Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site	Synthetic	Role In Clotting	N.A.	200 IU/kg	31.8	Hours	114480	HemA mice plasma protease	chromogenic activity assays	HemA mice plasma	In Vivo	PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf	None	ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar
5035	32078672	2020	MQIELSTCFFLCLLRFCFSATRRYYLGAVELSWDYMQSDLGELPVDARFPPRVPKSFPFNTSVVYKKTLFVEFTDHLFNIAKPRPPWMGLLGPTIQAEVYDTVVITLKNMASHPVSLHAVGVSYWKASEGAEYDDQTSQREKEDDKVFPGGSHTYVWQVLKENGPMASDPLCLTYSYLSHVDLVKDLNSGLIGALLVCREGSLAKEKTQTLHKFILLFAVFDEGKSWHSETKNSLMQDRDAASARAWPKMHTVNGYVNRSLPGLIGCHRKSVYWHVIGMGTTPEVHSIFLEGHTFLVRNHRQASLEISPITFLTAQTLLMDLGQFLLFCHISSHQHDGMEAYVKVDSCPEEPQLRMKNNEEAEDYDDDLTDSEMDVVRFDDDNSPSFIQIRSVAKKHPKTWVHYIAAEEEDWDYAPLVLAPDDRSYKSQYLNNGPQRIGRKYKKVRFMAYTDETFKTREAIQHESGILGPLLYGEVGDTLLIIFKNQASRPYNIYPHGITDVRPLYSRRLPKGVKHLKDFPILPGEIFKYKWTVTVEDGPTKSDPRCLTRYYSSFVNMERDLASGLIGPLLICYKESVDQRGNQIMSDKRNVILFSVFDENRSWYLTENIQRFLPNPAGVQLEDPEFQASNIMHSINGYVFDSLQLSVCLHEVAYWYILSIGAQTDFLSVFFSGYTFKHKMVYEDTLTLFPFSGETVFMSMENPGLWILGCHNSDFRNRGMTALLKVSSCDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSQNGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGTSTEPSEGSAPGTSESATPESGPGTSESATPESGPGTSESATPESGPGSEPATSGSETPGSEPATSGSETPGSPAGSPTSTEEGTSTEPSEGSAPGTSTEPSEGSAPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPASSEITRTTLQSDQEEIDYDDTISVEMKKEDFDIYDEDENQSPRSFQKKTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG/MIPARFAGVLLALALILPGTLCAEGTRGRSSTARCSLFGSDFVNTFDGSMYSFAGYCSYLLAGGCQKRSFSIIGDFQNGKRVSLSVYLGEFFDIHLFVNGTVTQGDQRVSMPYASKGLYLETEAGYYKLSGEAYGFVARIDGSGNFQVLLSDRYFNKTCGLCGNFNIFAEDDFMTQEGTLTSDPYDFANSWALSSGEQWCERASPPSSSCNISSGEMQKGLWEQCQLLKSTSVFARCHPLVDPEPFVALCEKTLCECAGGLECACPALLEYARTCAQEGMVLYGWTDHSACSPVCPAGMEYRQCVSPCARTCQSLHINEMCQERCVDGCSCPEGQLLDEGLCVESTECPCVHSGKRYPPGTSLSRDCNTCICRNSQWICSNEECPGECLVTGQSHFKSFDNRYFTFSGICQYLLARDCQDHSFSIVIETVQCADDRDAVCTRSVTVRLPGLHNSLVKLKHGAGVAMDGQDIQLPLLKGDLRIQHTVTASVRLSYGEDLQMDWDGRGRLLVKLSPVYAGKTCGLCGNYNGNQGDDFLTPSGLAEPRVEDFGNAWKLHGDCQDLQKQHSDPCALNPRMTRFSEEACAVLTSPTFEACHRAVSPLPYLRNCRYDVCSCSDGRECLCGALASYAAACAGRGVRVAWREPGRCELNCPKGQVYLQCGTPCNLTCRSLSYPDEECNEACLEGCFCPPGLYMDERGDCVPKAQCPCYYDGEIFQPEDIFSDHHTMCYCEDGFMHCTMSGVPGSLLPDAVLSSPLSHRSKRSLSCRPPMVKLVCPADNLRAEGLECTKTCQNYDLECMSMGCVSGCLCPPGMVRHENRCVALERCPCFHQGKEYAPGETVKIGCNTCVCRDRKWNCTDHVCDATCSTIGMAHYLTFDGLKYLFPGECQYVLVQDYCGSNPGTFRILVGNKGCSHPSVKCKKRVTILVEGGEIELFDGEVNVKRPMKDETHFEVVESGRYIILLLGKALSVVWDRHLSISVVLKQTYQEKVCGLCGNFDGIQNNDLTSSNLQVEEDPVDFGNSWKVSSQCADTRKVPLDSSPATCHNNIMKQTMVDSSCRILTSDVFQDCNKLVDPEPYLDVCIYDTCSCESIGDCAAFCDTIAAYAHVCAQHGKVVTWRTATLCPQSCEERNLRENGYEAEWRYNSCAPACQVTCQHPEPLACPVQCVEGCHAHCPPGKILDELLQTCVDPEDCPVCEVAGRRFASGKKVTLNPSDPEHCQICHCDVVNLTCEACQEPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGASSDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	rFVIIIFc-VWF-XTEN (construct 4) (BIVV001)	3,611	Free	Free	Linear	L	Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site	Synthetic	Role In Clotting	N.A.	200 IU/kg	29.9	Hours	107640	VWF Het mice plasma protease	chromogenic activity assays	VWF Het mice plasma	In Vivo	PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf	None	ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar
5036	32078672	2020	MQIELSTCFFLCLLRFCFSATRRYYLGAVELSWDYMQSDLGELPVDARFPPRVPKSFPFNTSVVYKKTLFVEFTDHLFNIAKPRPPWMGLLGPTIQAEVYDTVVITLKNMASHPVSLHAVGVSYWKASEGAEYDDQTSQREKEDDKVFPGGSHTYVWQVLKENGPMASDPLCLTYSYLSHVDLVKDLNSGLIGALLVCREGSLAKEKTQTLHKFILLFAVFDEGKSWHSETKNSLMQDRDAASARAWPKMHTVNGYVNRSLPGLIGCHRKSVYWHVIGMGTTPEVHSIFLEGHTFLVRNHRQASLEISPITFLTAQTLLMDLGQFLLFCHISSHQHDGMEAYVKVDSCPEEPQLRMKNNEEAEDYDDDLTDSEMDVVRFDDDNSPSFIQIRSVAKKHPKTWVHYIAAEEEDWDYAPLVLAPDDRSYKSQYLNNGPQRIGRKYKKVRFMAYTDETFKTREAIQHESGILGPLLYGEVGDTLLIIFKNQASRPYNIYPHGITDVRPLYSRRLPKGVKHLKDFPILPGEIFKYKWTVTVEDGPTKSDPRCLTRYYSSFVNMERDLASGLIGPLLICYKESVDQRGNQIMSDKRNVILFSVFDENRSWYLTENIQRFLPNPAGVQLEDPEFQASNIMHSINGYVFDSLQLSVCLHEVAYWYILSIGAQTDFLSVFFSGYTFKHKMVYEDTLTLFPFSGETVFMSMENPGLWILGCHNSDFRNRGMTALLKVSSCDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSQNGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGTSTEPSEGSAPGTSESATPESGPGTSESATPESGPGTSESATPESGPGSEPATSGSETPGSEPATSGSETPGSPAGSPTSTEEGTSTEPSEGSAPGTSTEPSEGSAPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPASSEITRTTLQSDQEEIDYDDTISVEMKKEDFDIYDEDENQSPRSFQKKTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG/MIPARFAGVLLALALILPGTLCAEGTRGRSSTARCSLFGSDFVNTFDGSMYSFAGYCSYLLAGGCQKRSFSIIGDFQNGKRVSLSVYLGEFFDIHLFVNGTVTQGDQRVSMPYASKGLYLETEAGYYKLSGEAYGFVARIDGSGNFQVLLSDRYFNKTCGLCGNFNIFAEDDFMTQEGTLTSDPYDFANSWALSSGEQWCERASPPSSSCNISSGEMQKGLWEQCQLLKSTSVFARCHPLVDPEPFVALCEKTLCECAGGLECACPALLEYARTCAQEGMVLYGWTDHSACSPVCPAGMEYRQCVSPCARTCQSLHINEMCQERCVDGCSCPEGQLLDEGLCVESTECPCVHSGKRYPPGTSLSRDCNTCICRNSQWICSNEECPGECLVTGQSHFKSFDNRYFTFSGICQYLLARDCQDHSFSIVIETVQCADDRDAVCTRSVTVRLPGLHNSLVKLKHGAGVAMDGQDIQLPLLKGDLRIQHTVTASVRLSYGEDLQMDWDGRGRLLVKLSPVYAGKTCGLCGNYNGNQGDDFLTPSGLAEPRVEDFGNAWKLHGDCQDLQKQHSDPCALNPRMTRFSEEACAVLTSPTFEACHRAVSPLPYLRNCRYDVCSCSDGRECLCGALASYAAACAGRGVRVAWREPGRCELNCPKGQVYLQCGTPCNLTCRSLSYPDEECNEACLEGCFCPPGLYMDERGDCVPKAQCPCYYDGEIFQPEDIFSDHHTMCYCEDGFMHCTMSGVPGSLLPDAVLSSPLSHRSKRSLSCRPPMVKLVCPADNLRAEGLECTKTCQNYDLECMSMGCVSGCLCPPGMVRHENRCVALERCPCFHQGKEYAPGETVKIGCNTCVCRDRKWNCTDHVCDATCSTIGMAHYLTFDGLKYLFPGECQYVLVQDYCGSNPGTFRILVGNKGCSHPSVKCKKRVTILVEGGEIELFDGEVNVKRPMKDETHFEVVESGRYIILLLGKALSVVWDRHLSISVVLKQTYQEKVCGLCGNFDGIQNNDLTSSNLQVEEDPVDFGNSWKVSSQCADTRKVPLDSSPATCHNNIMKQTMVDSSCRILTSDVFQDCNKLVDPEPYLDVCIYDTCSCESIGDCAAFCDTIAAYAHVCAQHGKVVTWRTATLCPQSCEERNLRENGYEAEWRYNSCAPACQVTCQHPEPLACPVQCVEGCHAHCPPGKILDELLQTCVDPEDCPVCEVAGRRFASGKKVTLNPSDPEHCQICHCDVVNLTCEACQEPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGASSDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	rFVIIIFc-VWF-XTEN (construct 4) (BIVV001)	3,611	Free	Free	Linear	L	Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site	Synthetic	Role In Clotting	N.A.	200 IU/kg	26.9	Hours	96840	DKO mice plasma protease	chromogenic activity assays	DKO mice plasma	In Vivo	PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf	None	ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar
5045	33336763	2020	SDYYKNLINNAKTVEGVKALIDEILAALPFNPR	LM06	33	Free	Free	Linear	L	None	OXM analogs	Antidiabetes	The serum sample of SD rats and monkeys were collected at the time points of 0, 4, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h from the tails of SD rats and right fore of monkeys, respectively	50 nmol/kg	53.19 ± 1.42	Hours	191484	SD rats serum protease	LC-MS/MS	SD rats serum	In Vivo	None	None	EC50 (nM) = 0.352 (Receptor activation of LM peptides for GLP-1R)
5046	33336763	2020	SDYYKNLINNAKTVEGVKALIDEILAALPFNPR	LM06	33	Free	Free	Linear	L	None	OXM analogs	Antidiabetes	The serum sample of SD rats and monkeys were collected at the time points of 0, 4, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h from the tails of SD rats and right fore of monkeys, respectively	100 nmol/kg	58.37 ± 4.51	Hours	210132	SD rats serum protease	LC-MS/MS	SD rats serum	In Vivo	None	None	EC50 (nM) = 0.352 (Receptor activation of LM peptides for GLP-1R)
5047	33336763	2020	SDYYKNLINNAKTVEGVKALIDEILAALPFNPR	LM06	33	Free	Free	Linear	L	None	OXM analogs	Antidiabetes	The serum sample of SD rats and monkeys were collected at the time points of 0, 4, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h from the tails of SD rats and right fore of monkeys, respectively	200 nmol/kg	73.68 ± 6.52	Hours	265248	SD rats serum protease	LC-MS/MS	SD rats serum	In Vivo	None	None	EC50 (nM) = 0.352 (Receptor activation of LM peptides for GLP-1R)
5048	33336763	2020	SDYYKNLINNAKTVEGVKALIDEILAALPFNPR	LM06	33	Free	Free	Linear	L	None	OXM analogs	Antidiabetes	The serum sample of SD rats and monkeys were collected at the time points of 0, 4, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h from the tails of SD rats and right fore of monkeys, respectively	50 nmol/kg	56.40 ± 2.71	Hours	203040	Cynomolgus monkeys serum protease	LC-MS/MS	Cynomolgus monkeys serum	In Vivo	None	None	EC50 (nM) = 0.352 (Receptor activation of LM peptides for GLP-1R)
5049	33336763	2020	SDYYKNLINNAKTVEGVKALIDEILAALPFNPR	LM06	33	Free	Free	Linear	L	None	OXM analogs	Antidiabetes	The serum sample of SD rats and monkeys were collected at the time points of 0, 4, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h from the tails of SD rats and right fore of monkeys, respectively	100 nmol/kg	63.15 ± 4.93	Hours	227340	Cynomolgus monkeys serum protease	LC-MS/MS	Cynomolgus monkeys serum	In Vivo	None	None	EC50 (nM) = 0.352 (Receptor activation of LM peptides for GLP-1R)
5050	33336763	2020	SDYYKNLINNAKTVEGVKALIDEILAALPFNPR	LM06	33	Free	Free	Linear	L	None	OXM analogs	Antidiabetes	The serum sample of SD rats and monkeys were collected at the time points of 0, 4, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h from the tails of SD rats and right fore of monkeys, respectively	200 nmol/kg	114.91 ±7.32	Hours	413676	Cynomolgus monkeys serum protease	LC-MS/MS	Cynomolgus monkeys serum	In Vivo	None	None	EC50 (nM) = 0.352 (Receptor activation of LM peptides for GLP-1R)
5107	32841660	2020	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1R agonist	Attenuates renal fibrosis	N.A.	90 nmol/kg	64.74 ± 3.06	Hours	233064	SD rats serum protease	N.A.	SD rats serum	In Vivo	None	None	EC50 (nM) = 0.11 (In vitro receptor activation profiles of GLP-1 peptides for GLP-1R)
5108	32841660	2020	EGTFQAKQWLPQDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	XFL6	43	Free	Free	Linear	L	Modifcation of lysine site at position at 16 with C16 fatty acid	GLP-1/GIP/Gcg receptor triagonist	Antidiabetes, Antiobesity	N.A.	10 nmol/kg	41.35 ± 1.42	Hours	148860	SD rats serum protease	N.A.	SD rats serum	In Vivo	None	None	EC50 (nM) = 0.12 (In vitro receptor activation profiles of XFL peptides for GLP-1R)
5109	32841660	2020	EGTFQAKQWLPQDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	XFL6	43	Free	Free	Linear	L	Modifcation of lysine site at position at 16 with C16 fatty acid	GLP-1/GIP/Gcg receptor triagonist	Antidiabetes, Antiobesity	N.A.	30 nmol/kg	58.23 ± 2.17	Hours	209628	SD rats serum protease	N.A.	SD rats serum	In Vivo	None	None	EC50 (nM) = 0.12 (In vitro receptor activation profiles of XFL peptides for GLP-1R)
5110	32841660	2020	EGTFQAKQWLPQDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	XFL6	43	Free	Free	Linear	L	Modifcation of lysine site at position at 16 with C16 fatty acid	GLP-1/GIP/Gcg receptor triagonist	Antidiabetes, Antiobesity	N.A.	90 nmol/kg	75.81 ± 3.58	Hours	272916	SD rats serum protease	N.A.	SD rats serum	In Vivo	None	None	EC50 (nM) = 0.12 (In vitro receptor activation profiles of XFL peptides for GLP-1R)
5113	32808659	2020	GEPKSCDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGKGGGSGGGSGGGSLRKHNCLQRRCMPLHSRVPFP	Fc-ELA-21	266	Fc joined with ELA-21 by linker (GGGS)3	Free	Linear	L	None	Derived from ELA	Anti-Heart Failure Activity	About 10 μl of blood was collected at each time point of 0, 1, 2, 4, 8, 24, 32, 48, 56, and 72 h after administration	5 mg/kg	∼44	Hours	158400	Mice plasma protease	Western blotting	Mice plasma	In Vivo	https://sci-hub.se/10.1016/j.ijcard.2019.04.089	None	EC50 =1.58 nM (cAMP supression)
5124	32736262	2020	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSLKEAKEKAIEELKKAGITSDYYFDLINKAKTVEGVNALKDEILKA	EX-ABD	84	Free	ABD	Linear	L	None	Synthetic	Antiobesity	Blood was withdrawn at 0, 10 min, 1 h, 3 h, 8 h, 1 day, 2 day, 3 day, 4 day, 7 day, 10 day, and 14 day post-administratio	50 nmol/kg	84.02	Hours	302472	ICR mice plasma protease	ELISA	ICR mice plasma	In Vivo	None	None	Kd(M) = 6.97 * 10-8(binding affinities of EX-ABD-AFF to glucagon-like peptide-1 receptor (GLP-1))
5125	32736262	2020	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSLKEAKEKAIEELKKAGITSDYYFDLINKAKTVEGVNALKDEILKAVDAKYAKEFESAAHEIRWLPNLTYDQRVAFIHKLSDDPSQSSELLSEAKKLNDSQAPK	EX-ABD-AFF	142	Free	ABD-AFF	Linear	L	None	Synthetic	Antiobesity	blood was withdrawn at 0, 10 min, 1 h, 3 h, 8 h, 1 day, 2 day, 3 day, 4 day, 7 day, 10 day, and 14 day post-administratio	50 nmol/kg	166.4	Hours	599040	ICR mice plasma protease	ELISA	ICR mice plasma	In Vivo	None	None	Kd(M) = 6.97 * 10-8(binding affinities of EX-ABD-AFF to glucagon-like peptide-1 receptor (GLP-1))
5126	32736262	2020	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSLKEAKEKAIEELKKAGITSDYYFDLINKAKTVEGVNALKDEILKAVDAKYAKEFESAAHEIRWLPNLTYDQRVAFIHKLSDDPSQSSELLSEAKKLNDSQAPK	EX-ABD-AFF	142	Free	ABD-AFF	Linear	L	None	Synthetic	Antiobesity	blood was withdrawn at 0, 10 min, 1 h, 3 h, 8 h, 1 day, 2 day, 3 day, 4 day, 7 day, 10 day, and 14 day post-administratio	50 nmol/kg	140.2	Hours	504720	ICR mice plasma protease	ELISA	ICR mice plasma	In Vivo	None	None	Kd(M) = 6.97 * 10-8(binding affinities of EX-ABD-AFF to glucagon-like peptide-1 receptor (GLP-1))
5157	32506501	2020	SYSMEHFRWGKPVG	des-Ac-a-MSH	14	Free	Amidation	Linear	L	None	Derived from POMC	Antiinflammatory, Antipyretic	37 °C	2 µM	32.06	Hours	115416	Human plasma protease	Glo-sensor transfected cell-based luminescence assay	Human CSF	In Vitro	None	None	EC50 (M) = 1.667E-09 for MC1R-des-Ac-a-MSH
5158	32506501	2020	SYSMEHFRWGKPVGKKRRPVKVYPNGAEDESAEAFPLEF	ACTH	39	Free	Free	Linear	L	None	Derived from POMC	Stimulates the adrenal glands to release cortisol	37 °C	2 µM	86.33	Hours	310788	Human CSF protease	Glo-sensor transfected cell-based luminescence assay	Human CSF	In Vitro	None	None	EC50 (M) = 1.54E-09 for MC1R-ACTH
5160	32464231	2020	KGH	FP-EGCG-NPs	3	Free	Folate peptide (FA-Pep-1) conjugated to EGCG-loaded nanoparticles (EGCG-NPs)	Linear	L	None	Polyphenolic constituent of green tea	Antitumor (Against Mda-Mb-231 Tumor Xenograft)	blood samples were collected at different time intervals (0.5, 1, 2, 4, 6, 8, 12, 24 and 48 h post-administration	0.1 mL	25.13 ± 8.62	Hours	90468	Male SD rats plasma protease	HPLC	Male SD rats plasma	In Vivo	None	None	IC50 = 15.56 for FP-EGCG-NPs(µg/mL) in MDA-MB-231
5163	32387412	2020	HGEGTFTSDVSSYLEGQAAKEFIAWLVKGRCHGEGTFTSDVSSYLEGQAAKEFIAWLVKGRC	DIG-2	62	Free	bisMal-PEG(10KDa)	Linear	L	Radioiodinated , A8G, G31C modification in GLP-1	DIG conjugates	Antidiabetes	The collected samples at predose, 0.5, 1, 2, 4, 8, 24, 36, 48, 96, 144 and 168 h were stored at −80 °C	50 nmol/kg	62.6	Hours	225360	Cynomolgus monkeys plasma protease	RP-HPLC	Cynomolgus monkeys plasma	In Vivo	None	None	kd (1/s) = 6.54 × 10−3 (binding results for DIG conjugates 2 with human GLP-1R ECD
5164	32387412	2020	HGEGTFTSDVSSYLEGQAAKEFIAWLVKGRCHGEGTFTSDVSSYLEGQAAKEFIAWLVKGRC	DIG-2	62	Free	bisMal-PEG(10KDa)	Linear	L	Radioiodinated , A8G, G31C modification in GLP-1	DIG conjugates	Antidiabetes	The collected samples at predose, 0.5, 1, 2, 4, 8, 24, 36, 48, 96, 144 and 168 h were stored at −80 °C	100 nmol/kg	97.2	Hours	349920	Cynomolgus monkeys plasma protease	RP-HPLC	Cynomolgus monkeys plasma	In Vivo	None	None	kd (1/s) = 6.54 × 10−3 (binding results for DIG conjugates 2 with human GLP-1R ECD
5165	32387412	2020	HGEGTFTSDVSSYLEGQAAKEFIAWLVKGRCHGEGTFTSDVSSYLEGQAAKEFIAWLVKGRC	DIG-2	62	Free	bisMal-PEG(10KDa)	Linear	L	Radioiodinated , A8G, G31C modification in GLP-1	DIG conjugates	Antidiabetes	The collected samples at predose, 0.5, 1, 2, 4, 8, 24, 36, 48, 96, 144 and 168 h were stored at −80 °C	150 nmol/kg	120.4	Hours	433440	Cynomolgus monkeys plasma protease	RP-HPLC	Cynomolgus monkeys plasma	In Vivo	None	None	kd (1/s) = 6.54 × 10−3 (binding results for DIG conjugates 2 with human GLP-1R ECD
5179	32301996	2020	KLDLKLDLKLDLK	89Zr-NFP	13	mPEG2000, 89Zr labeling	Cy5.5 labelling	Linear	L	None	Synthetic	Diffuse intrinsic pontine glioma treatment	Mice were euthanized after 4 and 21 days for organ collection	20 μCi	60.3	Days	5209920	Mice brain homogenize protease	Gamma counter	Mice brain homogenize	In Vivo	None	None	IC50 (nM) = 5.6 ± 0.4 for DM1 in SF8628
5180	32243177	2020	MTTASTSQVRQNYHQDSEAAINRQINLELYASYVYLSMSYYFDRDDVALKNFAKYFLHQSHEEREHAEKLMKLQNQRGGRIFLQDIKKPDCDDWESGLNAMECALHLEKNVNQSLLELHKLATDKNDPHLCDFIETHYLNEQVKAIKELGDHVTNLRKMGAPESGLAEYLFDKHTLGDSDNES	FITC-labeled HFt	183	FITC labelled	Free	Linear	L	None	Derived from human Ft	Antidiabetes	At different time points (30 min, 1, 2, 4, 8, 10, 24, 48, 72, and 96 h) after injection	100 μg	51.1	Hours	183960	Mice plasma protease	BCA protein assay	Mice plasma	In Vivo	None	None	The GLP-HFt nanocage dose-dependently reduced the nonfasting blood glucose of the STZ-induced diabetic mice
5181	32243177	2020	HGEGTFTSDVSSYLEGQAAKEFIAWLVKGRGSGGMTTASTSQVRQNYHQDSEAAINRQINLELYASYVYLSMSYYFDRDDVALKNFAKYFLHQSHEEREHAEKLMKLQNQRGGRIFLQDIKKPDCDDWESGLNAMECALHLEKNVNQSLLELHKLATDKNDPHLCDFIETHYLNEQVKAIKELGDHVTNLRKMGAPESGLAEYLFDKHTLGDSDNES	GLP-HFt	217	GLP-1 A8G modification linked by GSGG	Free	Linear	L	None	Synthetic	Antidiabetes	At different time points (30 min, 1, 2, 4, 8, 10, 24, 48, 72, and 96 h) after injection	100 μg	51.9	Hours	186840	Mice plasma protease	BCA protein assay	Mice plasma	In Vivo	None	None	The GLP-HFt nanocage dose-dependently reduced the nonfasting blood glucose of the STZ-induced diabetic mice
5191	35496622	2020	HGEGTFTSDLSQMEEEAVRLFIEWLKNGGPSSGAPPSKKKKKK	Lixisenatide 1c	44	Free	Amidation	Linear	L	(X3) MPAs modification on Lys12	lixisenatide analogues	Antidiabetes	incubated at 37 °C for 6, 12, 24, and 48 h	1000 ng/mL	30	Hours	108000	Rats blood plasma protease	LC-MS/MS	Rats blood plasma	In Vitro	None	None	EC50(nM) = 0.98 ± 0.24 for Lixisenatide 1c (in vitro GLP-1 receptor activation potency)
5194	35496622	2020	HGEGTFTSDLSKQMEEEAVRLFIEWLNGGPSSGAPPSKKKKKK	Lixisenatide 1f	44	Free	Amidation	Linear	L	(X3) MPAs modification on Lys12	lixisenatide analogues	Antidiabetes	incubated at 37 °C for 6, 12, 24, and 48 h	1000 ng/mL	33.4	Hours	120240	Rats blood plasma protease	LC-MS/MS	Rats blood plasma	In Vitro	None	None	EC50(nM) = 0.32 ± 0.13 for Lixisenatide 1f (in vitro GLP-1 receptor activation potency)
5197	35496622	2020	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPSKKKKK	Lixisenatide 1i	44	Free	Amidation	Linear	L	(X3) MPAs modification on Lys12	lixisenatide analogues	Antidiabetes	incubated at 37 °C for 6, 12, 24, and 48 h	1000 ng/mL	31.6	Hours	113760	Rats blood plasma protease	LC-MS/MS	Rats blood plasma	In Vitro	None	None	EC50(nM) = 4.68 ± 0.85 for Lixisenatide 1i (in vitro GLP-1 receptor activation potency)
5207	32082972	2020	PHWSYGLRPGGGGGSGGGGSGGGGSESKYGPPCPSCPAPEFLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTLPPSQEEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSRLTVDKSRWQEGNVFSCSVMHEALHNHYTQKSLSLSGGGGSGGGGSGGGGSIVRRADRAAVPGGGGACDCRGDCFC	LMRAP	291	Free	hIgG4 Fc-linker-AP25	Linear	L	None	Synthetic	Antitumor	The experimental sampling time points were: SD rats at 5 min before administration and then 0, 5, 10, 30 min, 1, 2, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, and 216 h after LMRAP administration	12.5 mg/kg	45.237 (Elimination Half Life)	Hours	162853.2	SD rats plasma protease	ELISA	SD rats plasma	In Vivo	None	None	The inhibition rates of each dose of LMRAP at 0.1, 0.2, 0.4, 0.8 and 1.6 μmol/L were 45.8 ± 5.9%, 43.8 ± 18.4%, 57.2 ± 10.2%, 76.6 ± 3.2% and 84.9 ± 2.8%, respectively
5208	32082972	2020	PHWSYGLRPGGGGGSGGGGSGGGGSESKYGPPCPSCPAPEFLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTLPPSQEEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSRLTVDKSRWQEGNVFSCSVMHEALHNHYTQKSLSLSGGGGSGGGGSGGGGSIVRRADRAAVPGGGGACDCRGDCFC	LMRAP	291	Free	hIgG4 Fc-linker-AP25	Linear	L	None	Synthetic	Antitumor	The experimental sampling time points were: SD rats at 5 min before administration and then 0, 5, 10, 30 min, 1, 2, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, and 216 h after LMRAP administration	12.5 mg/kg	29.187 (Elimination Half Life)	Hours	105073.2	SD rats plasma protease	ELISA	SD rats plasma	In Vivo	None	None	The inhibition rates of each dose of LMRAP at 0.1, 0.2, 0.4, 0.8 and 1.6 μmol/L were 45.8 ± 5.9%, 43.8 ± 18.4%, 57.2 ± 10.2%, 76.6 ± 3.2% and 84.9 ± 2.8%, respectively
5209	32082972	2020	PHWSYGLRPGGGGGSGGGGSGGGGSESKYGPPCPSCPAPEFLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTLPPSQEEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSRLTVDKSRWQEGNVFSCSVMHEALHNHYTQKSLSLSGGGGSGGGGSGGGGSIVRRADRAAVPGGGGACDCRGDCFC	LMRAP	291	Free	hIgG4 Fc-linker-AP25	Linear	L	None	Synthetic	Antitumor	The experimental sampling time points were: SD rats at 5 min before administration and then 0, 5, 10, 30 min, 1, 2, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, and 216 h after LMRAP administration	12.5 mg/kg	50.979 (Eliminatoin Half Life)	Hours	183524.4	SD rats plasma protease	ELISA	SD rats plasma	In Vivo	None	None	The inhibition rates of each dose of LMRAP at 0.1, 0.2, 0.4, 0.8 and 1.6 μmol/L were 45.8 ± 5.9%, 43.8 ± 18.4%, 57.2 ± 10.2%, 76.6 ± 3.2% and 84.9 ± 2.8%, respectively
5211	32082972	2020	PHWSYGLRPGGGGGSGGGGSGGGGSESKYGPPCPSCPAPEFLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTLPPSQEEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSRLTVDKSRWQEGNVFSCSVMHEALHNHYTQKSLSLSGGGGSGGGGSGGGGSIVRRADRAAVPGGGGACDCRGDCFC	LMRAP	291	Free	hIgG4 Fc-linker-AP25	Linear	L	None	Synthetic	Antitumor	The experimental sampling time points were: SD rats at 5 min before administration and then 0, 5, 10, 30 min, 1, 2, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, and 216 h after LMRAP administration	12.5 mg/kg	27.879 (Elimination Half Life)	Hours	100364.4	SD rats plasma protease	ELISA	SD rats plasma	In Vivo	None	None	The inhibition rates of each dose of LMRAP at 0.1, 0.2, 0.4, 0.8 and 1.6 μmol/L were 45.8 ± 5.9%, 43.8 ± 18.4%, 57.2 ± 10.2%, 76.6 ± 3.2% and 84.9 ± 2.8%, respectively
5212	32082972	2020	PHWSYGLRPGGGGGSGGGGSGGGGSESKYGPPCPSCPAPEFLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTLPPSQEEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSRLTVDKSRWQEGNVFSCSVMHEALHNHYTQKSLSLSGGGGSGGGGSGGGGSIVRRADRAAVPGGGGACDCRGDCFC	LMRAP	291	Free	hIgG4 Fc-linker-AP25	Linear	L	None	Synthetic	Antitumor	The experimental sampling time points were: SD rats at 5 min before administration and then 0, 5, 10, 30 min, 1, 2, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, and 216 h after LMRAP administration	12.5 mg/kg	28.452 (Elimination Half Life)	Hours	102427.2	SD rats plasma protease	ELISA	SD rats plasma	In Vivo	None	None	The inhibition rates of each dose of LMRAP at 0.1, 0.2, 0.4, 0.8 and 1.6 μmol/L were 45.8 ± 5.9%, 43.8 ± 18.4%, 57.2 ± 10.2%, 76.6 ± 3.2% and 84.9 ± 2.8%, respectively
5225	32075870	2020	HGDGSFSDE-Nle-fTILDLLAARDFINWLIQTKITD	Apraglutide	33	Free	Amidation	Linear	L	Gly2, Nle10, D-Phe11, Leu16 modification	Derived from hGLP-2	Treatment of Short Bowel Syndrome	Blood samples were collected at multiple time points up to 169 h post injection	0.25 mg/kg	32.4 ± 6.1 (Terminal Half Life)	Hours	116640	Male cynomolgus monkeys plasma protease	LC-MS/MS	Male cynomolgus monkeys	In Vivo	None	None	EC50(nM) = 0.24 for hGLP-2 receptor
5226	32075870	2020	HGDGSFSDE-Nle-fTILDLLAARDFINWLIQTKITD	Apraglutide	33	Free	Amidation	Linear	L	Gly2, Nle10, D-Phe11, Leu16 modification	Derived from hGLP-2	Treatment of Short Bowel Syndrome	Blood samples were collected at multiple time points up to 169 h post injection	0.15 mg/kg	30.1 ± 3.1 (Terminal Half Life)	Hours	108360	Göttingen minipigs plasma protease	LC-MS/MS	Göttingen minipigs plasma	In Vivo	None	None	EC50(nM) = 0.24 for hGLP-2 receptor
5240	31901754	2020	HGQGTFTSDYSKYLDXRRAQDFVEWLKNGGPSSGAPPPS	Compound 16a	39	Free	Amidation	Linear	L	Amino acid residues located at 24 substituted by the residues of Exenatide in the same location, Position 16 was replaced by Cys for coupling hybrid peptides with fatty chains	OXM analogs	Antiobesity, Antidiabetes	At 0, 1, 2, 4, 6, 8, 12, 24, 36, 48, 72 and 96 h time points, 100 μL of mixture was aliquoted	1000 ng/mL	71.79	Hours	258444	Rats plasma protease	LC-MS/MS	Rats plasma	In Vitro	None	None	EC50 = 3.8 ± 0.4 pM for mGLP1R
5245	31786794	2020	GGGSGGGGSGGGGSA	DR10601	15	Free	IgG4 hinge-Fc fragment	Linear	L	None	Synthetic	Antiobesity, Antidiabetes	Blood samples were collected at 3, 8, 24, 36, 48, 72, 96, 120, 144 and 168 h after administration	16.3 nmol/kg	51.9 ± 12.2	Hours	186840	SD rats serum protease	ELISA	SD rats serum	In Vivo	None	None	(EC50) value of DR10601 for GCGR was 37.39±3.95 nmol/L
5281	US 201715829596 A	2020	Aib-Z-HsQGTFTSDLSKQKESKAAQDFIEWLKAGGPSSGAPPPS	HA-Aib-Linker-SEQ ID No. 5	40	HA = Hyaluronic acid hydrogel linked with GLP-1 analogue	Amidation	Linear	Mix	Linker Z = Structure mentioned in patent, dSer substituitions at position 2	GLP-1-Linker-Ha Conjugate	Antidiabetes, Antiobesity	Plasma sample were taken at 0,1,4,8,24,48 H And Once A Day On Day 3 to 21 at the same time	0.623 mg/kg	139	Hours	500400	Minipigs plasma protease	LC-MS/MS	Minipigs plasma	In Vivo	None	US 201715829596 A	EC50 hGLP-1R = 1.9 pM for Sequence No. 5
5299	31818212	2019	DKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGKGGGGSGGGGSGGGGSQLYSALANKCCHVGCTKRSLARFCGGGGSGGGGSGGGGSSWMEEVIKLCGRELVRAQIAICGMSTWS	RELAX10	309	Free	Free	Linear	L	Fusion of Human Relaxin 2 with Fc IgG using linker	Human Relaxin analogue	Treatment prevents and reverses isoproterenol induced hypertrophy and fibrosis in mouse heart	Blood samples were collected at various time points after drug administration	4 mg/kg	3.59	Days	310176	Wistar rats plasma protease	ELISA	Wistar rats plasma	In Vivo	https://www.lens.org/lens/patent/078-521-931-782-236/fulltext	None	RELAX10 was active in CHO cells overexpressing the relaxin‐2 receptor, RXFP1, with an average half‐maximal effective concentration value of 1.94 nmol/L
5300	31818212	2019	DKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGKGGGGSGGGGSGGGGSQLYSALANKCCHVGCTKRSLARFCGGGGSGGGGSGGGGSSWMEEVIKLCGRELVRAQIAICGMSTWS	RELAX10	309	Free	Free	Linear	L	Fusion of Human Relaxin 2 with Fc IgG using linker	Human Relaxin analogue	Treatment prevents and reverses isoproterenol induced hypertrophy and fibrosis in mouse heart	Blood samples were collected at various time points after drug administration	4 mg/kg	3.75	Days	324000	Wistar rats plasma protease	ELISA	Wistar rats plasma	In Vivo	https://www.lens.org/lens/patent/078-521-931-782-236/fulltext	None	RELAX10 was active in CHO cells overexpressing the relaxin‐2 receptor, RXFP1, with an average half‐maximal effective concentration value of 1.94 nmol/L
5301	31818212	2019	DKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGKGGGGSGGGGSGGGGSQLYSALANKCCHVGCTKRSLARFCGGGGSGGGGSGGGGSSWMEEVIKLCGRELVRAQIAICGMSTWS	RELAX10	309	Free	Free	Linear	L	Fusion of Human Relaxin 2 with Fc IgG using linker	Human Relaxin analogue	Treatment prevents and reverses isoproterenol induced hypertrophy and fibrosis in mouse heart	Blood samples were collected at various time points after drug administration	6 mg/kg	5.58	Days	482112	Wistar rats plasma protease	ELISA	Wistar rats plasma	In Vivo	https://www.lens.org/lens/patent/078-521-931-782-236/fulltext	None	RELAX10 was active in CHO cells overexpressing the relaxin‐2 receptor, RXFP1, with an average half‐maximal effective concentration value of 1.94 nmol/L
5302	31818212	2019	DKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGKGGGGSGGGGSGGGGSQLYSALANKCCHVGCTKRSLARFCGGGGSGGGGSGGGGSSWMEEVIKLCGRELVRAQIAICGMSTWS	RELAX10	309	Free	Free	Linear	L	Fusion of Human Relaxin 2 with Fc IgG using linker	Human Relaxin analogue	Treatment prevents and reverses isoproterenol induced hypertrophy and fibrosis in mouse heart	Blood samples were collected at various time points after drug administration	6 mg/kg	7.06	Days	609984	Wistar rats plasma protease	ELISA	Wistar rats plasma	In Vivo	https://www.lens.org/lens/patent/078-521-931-782-236/fulltext	None	RELAX10 was active in CHO cells overexpressing the relaxin‐2 receptor, RXFP1, with an average half‐maximal effective concentration value of 1.94 nmol/L
5303	31818212	2019	DKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGKGGGGSGGGGSGGGGSQLYSALANKCCHVGCTKRSLARFCGGGGSGGGGSGGGGSSWMEEVIKLCGRELVRAQIAICGMSTWS	RELAX10	309	Free	Free	Linear	L	Fusion of Human Relaxin 2 with Fc IgG using linker	Human Relaxin analogue	Treatment prevents and reverses isoproterenol induced hypertrophy and fibrosis in mouse heart	Blood samples were collected at various time points after drug administration	1, 6, or 30 mg/kg	4.59 - 7.06	Days	396576	Wistar rats plasma protease	ELISA	Wistar rats plasma	In Vivo	https://www.lens.org/lens/patent/078-521-931-782-236/fulltext	None	RELAX10 was active in CHO cells overexpressing the relaxin‐2 receptor, RXFP1, with an average half‐maximal effective concentration value of 1.94 nmol/L
5305	31805154	2019	DCAWHLGELVWCTMTWEEWDKKIEEYTKKIEELIKKS	IBP-CP24	37	IBP conjugation to the N-terminus of CP24	Free	Linear	L	None	Synthetic	Antiviral (HIV-1 Fusion Inhibitory Peptide)	Serial blood samples were collected from monkeys that received CP24 or IBP-CP24 before injection and at 2, 4, 6, 24, 72 and 144 h post-injection	10 mg/kg	46.11	Hours	165996	Rhesus monkeys plasma protease	Sandwich ELISA	Rhesus monkeys plasma	In Vivo	None	None	IC50(nM) = 0.7±0.3 for IBP-CP24 in virus subtype A (92UG029)
5313	31615671	2019	NSEIQNAVEVEEVVLPSIESPTENLPNNGSVVQPPSRSSPAGRPAIWIKDFVWGHIRPRRLTNDRLADMPLERRESWARMQRREWEEIEEEKGETQEEGG	Free-ADI	100	Free	Free	Linear	L	None	Purified from the mycelia of A. nidulan	Anticancer	20 days	100 μl	50.14	Hours	180504	Mice serum protease	HPLC	Mice serum	In Vivo	None	None	IC50 = 6.3 ± 0.6(μmol/mg/min) in HepG-2 cells
5314	31615671	2019	NSEIQNAVEVEEVVLPSIESPTENLPNNGSVVQPPSRSSPAGRPAIWIKDFVWGHIRPRRLTNDRLADMPLERRESWARMQRREWEEIEEEKGETQEEGG	Dextran-ADI	100	Free	Free	Linear	L	ADI was conjugated to dextran- reactive aldehyde groups via the formation of aldimine linkage	Purified from the mycelia of A. nidulan	Anticancer	20 days	100 μl	66.8	Hours	240480	Mice serum protease	HPLC	Mice serum	In Vivo	None	None	IC50 = 4.7 ± 0.9 (μmol/mg/min) in HepG-2 cells
5330	31389463	2019	ACAELVDNAVAIGGQGTFTSDYSYLDSRRAQDFVQWLMNTARNRNNIA	PP18	49	Free	Free	Linear	L	Ser23 linked with X3 = Structure givven in paper	OXM analogs	Antidiabetes, Antiobesity	blood was sampled pre-dose and at 0.5, 1, 2, 4, 8, 24, 48, 72, and 96 h post-dose	30 nmoL/kg	38.5 ± 5.9	Hours	138600	SD rats plasma protease	LC-MS, ELISA	SD rats plasma	In Vivo	None	None	EC50(nM) = 0.487 for Human GLP-1R
5333	31341417	2019	AEAAAKEAAAKEAAAKEAAAKAACDCRGDCFCGGGGIVRRADRAAVP	PSG4R	25	hIgG4 Fc conjugation through linker AEAAAKEAAAKEAAAKEAAAKA	Free	Cyclic (Two Disulfide Bonds Arranged As Cys2-Cys10 And Cys4-Cys8 In Ap25)	L	None	RGD-4C and endostatin fragment ES-2 fusion protein derived	Antitumor	100 to 200 µL orbital blood samples were taken at 5 min before drug administration or 0 min, 5 min, 10 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 12 h, 18 h, 24 h, 36 h, 48 h, 72 h, 96 h, 120 h, 144 h, 168 h, 192 h, 216 h after drug administration	5 mg/kg	56.27 (Elimination Half Life)	Hours	202572	Rats plasma protease	Indirect competitive ELISA	Rats plasma	In Vivo	None	None	IC50 = 1.82 ± 0.25 μmol/L for PSG4R on HUVEC proliferation
5334	31341417	2019	ACDCRGDCFCGGGGIVRRADRAAVP	AP25	25	Free	Free	Cyclic (Two Disulfide Bonds Arranged As Cys2-Cys10 And Cys4-Cys8)	L	None	Synthetic	Antitumor	100 to 200 µL orbital blood samples were taken at 5 min before drug administration or 0 min, 5 min, 10 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 12 h, 18 h, 24 h, 36 h, 48 h, 72 h, 96 h, 120 h, 144 h, 168 h, 192 h, 216 h after drug administration	5 mg/kg	50 (Elimination Half Life)	Minutes	180000	Rats plasma protease	ELISA	rats plasma	In Vivo	None	None	IC50 = 1.60 ± 0.15μmol/L for AP25 on HUVEC proliferation
5356	31235532	2019	LQEHPNARKYKGANKKGLSKGCFGLKLDRIGSMSGLGC	TransCon CNP (CNP-38)	38	Free	Free	Cyclic (1 Disulfide Bond)	L	4xPEG10KDa modification at Lys26 through transient linker	CNP-38 analog	Treatment of Comorbidities Associated with Fibroblast Growth Factor Receptor 3–related Skeletal Dysplasias	Blood samples for CNP38 analysis were collected and analyzed following the 1st and the 26th dose at the following time points: 0 (prior to dosing), 6, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose	40 μg/kg per week for 26 weeks	92.6	Hours	333360	Cynomolgus monkeys plasma protease	HPLC-MS/MS	Cynomolgus monkeys plasma	In Vivo	None	None	Ratio IC50 CNP-38/IC50 CNP-38 conjugate = <1 for TransCon CNP (NPR-C Affinity)
5357	31235532	2019	LQEHPNARKYKGANKKGLSKGCFGLKLDRIGSMSGLGC	TransCon CNP (CNP-38)	38	Free	Free	Cyclic (1 Disulfide Bond)	L	4xPEG10KDa modification at Lys26 through transient linker	CNP-38 analog	Treatment of Comorbidities Associated with Fibroblast Growth Factor Receptor 3–related Skeletal Dysplasias	Blood samples for CNP38 analysis were collected and analyzed following the 1st and the 26th dose at the following time points: 0 (prior to dosing), 6, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose	100 μg/kg per week for 26 weeks	86.7	Hours	312120	Cynomolgus monkeys plasma protease	HPLC-MS/MS	Cynomolgus monkeys plasma	In Vivo	None	None	Ratio IC50 CNP-38/IC50 CNP-38 conjugate = <1 for TransCon CNP (NPR-C Affinity)
5360	31235532	2019	LQEHPNARKYKGANKKGLSKGCFGLKLDRIGSMSGLGC	5-kDa PEG-linker CNP-38	38	PEG5KDa through permanent linker	Free	Cyclic (1 Disulfide Bond)	L	None	CNP-38 analog	Treatment of Comorbidities associated with Fibroblast Growth Factor Receptor 3–Related Skeletal Dysplasias	4 days	100 μg/ml	65.4	Hours	235440	Recombinant Human Nep Protease	HPLC-UV	Recombinant human NEP (2.5 mg/ml) + digest buffer (50 mM Tris-HCl, 10 mM NaCl, pH 7.4)	In Vitro	None	None	Ratio IC50 CNP-38/IC50 CNP-38 conjugate = 83 ± 7 (NPR-C Affinity)
5378	31156041	2019	LQVDIVPSQGEISVGESKFFLCQVAGDAKDKDISWFSPNGEKLTPNQQRISVVWNDDSSSTLTIYNANIDDAGIYKCVVTGEDGSESEATVNVKIFQAAADYKDDDDKAADYKDDDDK	AD-114-PA600-6H	118	Free	PA-600-6H	Linear	L	None	Fusion protein of AD-114 with PA600	Attenuates Renal fibrosis through blockade Of CXCR	Blood samples were collected immediately following dosing and at 5, 15, and 30 min and 1, 2, 4, 8, 12, 24, 36, 48, 60, 72, 84, 96, 120, 144, 168, and 192-h post-dosing	2 mg/kg	24.27 ± 0.24	Hours	87372	Cynomolgus monkeys plasma protease	LC–MS/MS	Cynomolgus monkeys plasma	In Vivo	PDB id: >5AEA_1	None	Kd(nM) = 5.2 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K
5379	31156041	2019	LQVDIVPSQGEISVGESKFFLCQVAGDAKDKDISWFSPNGEKLTPNQQRISVVWNDDSSSTLTIYNANIDDAGIYKCVVTGEDGSESEATVNVKIFQAAADYKDDDDKAADYKDDDDK	AD-114-PA600	118	Free	PA-600	Linear	L	None	Fusion protein of AD-114 with PA600	Attenuates Renal fibrosis through blockade Of CXCR	Blood samples were collected pre-dosing and at the following time points post each dosing: 30 min, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, and 144 h	3 mg/kg	25.41 ± 5.17	Hours	91476	Cynomolgus monkeys plasma protease	LC–MS/MS	Cynomolgus monkeys plasma	In Vivo	PDB id: >5AEA_1	None	Kd(nM) = 4 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K
5406	31064153	2019	K-GlyΨ[Trl]-GlyΨ[Trl]-R	Triazolopeptides compounds 3	4	Free	Free	Linear	L	Lys1 linked with Har = Homo-Arginine, GlyΨ[Trl] is a glycyl-1,2,3-triazole unit mimicking glycine (triazole ring substitution instead of peptide bond)	Derived from triazolopeptide	Inhibits the interaction between Neuropilin-1 and Vascular Endothelial Growth Factor-165	37 °C	1.1 µmol/mL	>> 48	Hours	172800	Human plasma protease	HPLC-MS/MS	Human plasma	In Vitro	None	None	IC50 = 8.39 μM
5407	31064153	2019	k-GlyΨ[Trl]-GlyΨ[Trl]-R	Triazolopeptides compounds 4	4	D-Lys at the first position which contains Har = Homo-Arginine side chain	Free	Linear	Mix	GlyΨ[Trl] is a glycyl-1,2,3-triazole unit mimicking glycine (triazole ring substitution instead of peptide bond)	Derived from triazolopeptide	Inhibits the interaction between Neuropilin-1 and Vascular Endothelial Growth Factor-165	37 °C	1.1 µmol/mL	>> 48	Hours	172800	Human plasma protease	HPLC-MS/MS	Human plasma	In Vitro	None	None	IC50 = 10.22 μM
5408	31064153	2019	K-Dab	Lys(Har)-Dab	2	Lys at the first position contains Har = Homo-Arginine side chain	Dab (2,4-diaminobutyric acid)	Linear	L	None	KPPR analogs	Peptidic inhibitor of the VEGF165/NRP-1 interaction	All samples were incubated at 37 °C and 100 µL of aliquots were withdrawn at different time intervals (for 4 and 5: 0, 10, 20, 30, 40, 50, 60, 70, 80 min, 1.5h, 2h, 2.5h, 3h, 4h, 6h	1.1 µmol/mL	34	Hours	122400	Human plasma protease	HPLC-MS/MS	Human plasma	In Vitro	None	None	IC50 = 0.2 μM
5409	31064153	2019	Dap-PR	Peptidotriazoles	3	Dap (2,3-diaminopropionic acid) substiuition at 1st position	Free	Linear	L	None	KPPR analogs	Peptidic inhibitor of the VEGF165/NRP-1 interaction	All samples were incubated at 37 °C and 100 µL of aliquots were withdrawn at different time intervals (for 4 and 5: 0, 10, 20, 30, 40, 50, 60, 70, 80 min, 1.5h, 2h, 2.5h, 3h, 4h, 6h	1.1 µmol/mL	41	Hours	147600	Human plasma protease	HPLC-MS/MS	Human plasma	In Vitro	None	None	IC50 = 0.2 μM
5415	31038930	2019	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSC-Mal-DBCO-N3-KPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	Exenatide-Fc	261	Free	Conjugation between Ex-Mal-DBCO and N3−Lys-Fc	Linear	L	None	Derived from the Lys-Fc directly expressed by Expi293F	Antidiabetes	Blood samples (ca. 0.6 mL) were collected from the posterior aorta 1, 2, 8, 24, 48, 72, 96, 120, and 168 h after administration	3.13 nmo/kg	43.8	Hours	157680	Mice plasma protease	ELISA	Mice plasma	In Vivo	PDB id: 7MLL	None	Exenatide-Fc presented similar GLP-1 activities with EC50 values of 1.5 nM
5416	31038930	2019	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSC-Mal-DBCO-N3-KPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	Exenatide-Fc	261	Free	Conjugation between Ex-Mal-DBCO and N3−Lys-Fc	Linear	L	None	Derived from the Lys-Fc directly expressed by Expi293F	Antidiabetes	Blood samples (ca. 0.6 mL) were collected from the posterior aorta 1, 2, 8, 24, 48, 72, 96, 120, and 168 h after administration	12.5 nmol/kg	40.4	Hours	145440	Mice plasma protease	ELISA	Mice plasma	In Vivo	PDB id: 7MLL	None	Exenatide-Fc presented similar GLP-1 activities with EC50 values of 1.5 nM
5417	31038930	2019	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSC-Mal-DBCO-N3-KPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	Exenatide-Fc	261	Free	Conjugation between Ex-Mal-DBCO and N3−Lys-Fc	Linear	L	None	Derived from the Lys-Fc directly expressed by Expi293F	Antidiabetes	Blood samples (ca. 0.6 mL) were collected from the posterior aorta 1, 2, 8, 24, 48, 72, 96, 120, and 168 h after administration	25 nmol/kg	87.8	Hours	316080	Mice plasma protease	ELISA	Mice plasma	In Vivo	PDB id: 7MLL	None	Exenatide-Fc presented similar GLP-1 activities with EC50 values of 1.5 nM
5425	30938069	2019	GLVLVAFSQYLQQCPFEDHVK	ESA-CJC-1295	30	Free	(DAC) maleimidopropionic acid conjugated with Equine serum albumin	Cyclic	Mix	None	Synthetic	Stimulates The Production Of Growth Hormone (Gh) From The Pituitary Gland	One mL aliquots were removed for analysis at 0, 24, 48, 72 and 96 hours at 4°C	700 pg/mL	20	Days	1728000	Equine plasma protease	Mass spectrometry	Equine plasma	In Vivo	None	None	N.A.
5437	30853651	2019	(PAS)40	DiR dye-loaded PAS40 nanoghosts	120	Free	Free	Linear	L	None	Synthetic	Increases the circulation time of a cell membrane based nanotherapeutic	Measuring the residual fluorescence intensity of the dye in serum at 0, 8, 24 and 48 h	50 mg/kg	37	Hours	133200	Mouse serum protease	Fluorescence assay	Mouse serum	In Vivo	None	None	N.A.
5451	30742145	2019	MAQAKHKQRKRLKSSCKRHPLYVDFSDVGWNDWIVAPPGYHAFYCHGECPFPLADHLNSTNHAIVQTLVNSVNSKIPKACCVPTELSAISMLYLDENEKVVLKNYQDMVVEGCGCR	n(BMP-2)	116	Free	Free	Linear	L	None	Synthetic	Promotes Bone repair	N.A.	0.5 mg/kg	48	Hours	172800	N.A.	Fluorescence spectrometry	Rats	In Vivo	PDB id: 1ES7	None	n(BMP-2) did not enhance ALP expression in MSCs compared with native BMP-2 unless pretreated with IV collagenase, which significantly enhanced ALP expression and calcium deposition
5461	30690406	2019	KFRKFRRQRPRLSHKGPMPF	Apelin3	20	R1 = NH2-Lys-Phe-Arg	Free	Linear	L	R2=Me, Methylation at Glu8	Apelin analogs	Blood Pressure lowering agents	37 C for up to 72 h	N.A.	>30	Hours	108000	RHNEP	LC-MS	Apelin3	In Vitro	None	None	EC50(nM) = 4.9 ± 1.0
5465	30690406	2019	KFRKFRRQRPRLSHKGPMPF	Apelin7	20	R1 = PEG-Lys-Phe-Arg	Free	Linear	L	None	Apelin analogs	Blood Pressure lowering agents	37 C for up to 72 h	N.A.	>30	Hours	108000	RHNEP	LC-MS	Apelin7	In Vitro	None	None	EC50(nM) = 6.3 ± 1.0
5466	30690406	2019	KFRKFRRQRPRLSHKGPMPF	Apelin8	20	R1 = PALM-Lys-Phe-Arg	Free	Linear	L	R2= Me, Methylation at Gln8	Apelin analogs	Blood Pressure lowering agents	37 C for up to 72 h	N.A.	>30	Hours	108000	RHNEP	LC-MS	Apelin8	In Vitro	None	None	EC50(nM) = 11.3 ± 2.1
5467	30690406	2019	KFRKFRRQRPRLSHKGPMPF	Apelin9	20	R1 = PEG-Lys-Phe-Arg	Free	Linear	L	R2= Me, Methylation at Gln8	Apelin analogs	Blood Pressure lowering agents	37 C for up to 72 h	N.A.	>30	Hours	108000	RHNEP	LC-MS	Apelin9	In Vitro	None	None	EC50(nM) = 2.5 ± 1.5
5485	30690406	2019	KFRKFRRQRPRLSHKGPMPF	Apelin9	20	R1 = PEG-Lys-Phe-Arg	Free	Linear	L	R2= Me, Methylation at Gln8	Apelin analogs	Blood Pressure lowering agents	37 C for up to 72 h	N.A.	27	Hours	97200	hplasma protease	LC-MS	hplasma	In Vitro	None	None	EC50(nM) = 2.5 ± 1.5
5487	30658804	2019	IVRRADRAAVP	HTCOSC-ES2	11	Chitooligosaccharide chloride	FITC	Linear	L	None	derived from the C-terminus of endostatin	Antiangiogenic	Immediately, 0.5, 1, 2, 4, 6, 8, 12, 24, and 36 h after injection, blood was collected	80 mg/kg	29.17 ± 3.91	Hours	105012	Mice plasma protease	Fluorescence assay	Mice plasma	In Vivo	None	None	Antitumor activity = 68.21%
5488	30624060	2019	D-sTyr-LGW-Nle-DMeAsp-F	Compound 7	9	yGlu-(OEG)2 linker between C18 fatty acid and peptide	Amidation	Linear	Mix	sTyr = Sulfated-Tyrosine, Nle = Nor-leucine, DMeAsp = N-methylated DAsp	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	115 (Terminal Half Life)	Hours	414000	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.35 (In Vitro CCK-1R Potency)
5489	30624060	2019	D-Phe(4sm)-Nle-GW-Nle-MeAsp-MePhe	Compound 8	9	yGlu-(OEG)2 linker between C18 fatty acid and peptide	Amidation	Linear	L	Phe(4sm) = 4-sulfomethylphenylalanine, Nle = Nor-leucine, MeAsp = N-methylated Asp	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	145 (Terminal Half Life)	Hours	522000	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.97 (In Vitro CCK-1R Potency)
5490	30624060	2019	D-Phe(4sm)-Nle-GW-Nle-DMeAsp-MePhe	Compound 9	9	yGlu-(OEG)2 linker between C18 fatty acid and peptide	Amidation	Linear	Mix	Phe(4sm) = 4-sulfomethylphenylalanine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	113 (Terminal Half Life)	Hours	406800	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.60 (In Vitro CCK-1R Potency)
5492	30624060	2019	D-Phe(4sm)-LGW-Nle-DMeAsp-MePhe	Compound 15	9	yGlu-(OEG)2 linker between C16 fatty acid and peptide	Amidation	Linear	Mix	Phe(4sm) = 4-sulfomethylphenylalanine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	37 (Terminal Half Life)	Hours	133200	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.72 (In Vitro CCK-1R Potency)
5493	30624060	2019	D-Phe(4sm)-LGW-Nle-DMeAsp-MePhe	Compound 16	9	yGlu-(OEG)2 linker between C20 fatty acid and peptide	Amidation	Linear	Mix	Phe(4sm) = 4-sulfomethylphenylalanine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	153 (Terminal Half Life)	Hours	550800	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.43 (In Vitro CCK-1R Potency)
5494	30624060	2019	D-sTyr-Nle-GW-Nle-DMeAsp-MePhe	Compound 17	9	yGlu-PEG10-PEG10 linker between C18 fatty acid and peptide	Amidation	Linear	Mix	Phe(4sm) = 4-sulfomethylphenylalanine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	103 (Terminal Half Life)	Hours	370800	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.54 (In Vitro CCK-1R Potency)
5495	30624060	2019	D-sTyr-Nle-GW-Nle-DMeAsp-MePhe	Compound 18	9	yGlu-PEG10-PEG10 linker between C18 fatty acid and peptide	Amidation	Linear	Mix	Phe(4sm) = 4-sulfomethylphenylalanine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	161 (Terminal Half Life)	Hours	579600	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.50 (In Vitro CCK-1R Potency)
5496	30624060	2019	yGlu-(OEG)2-K-OEG-Asp-phe(4sm)-Nle-GW-Nle-DMeAsp-MePhe	Compound 19	10	C18 fatty acid	Amidation	Linear	Mix	sTyr = Sulfated-Tyrosine, Nle = Nor-leucine, DMeAsp = N-methylated DAsp, MePhe = Methylated-phenylalanine	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	36 (Terminal Half Life)	Hours	129600	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.67 (In Vitro CCK-1R Potency)
5498	30624060	2019	DYLGW-Nle-DMeAsp-MePhe	Compound 25	9	yGlu-(OEG)2 linker between C18 fatty acid and peptide	Amidation	Linear	Mix	Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	45 (Terminal Half Life)	Hours	162000	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.81 (In Vitro CCK-1R Potency)
5500	30624060	2019	D-sTyr-LGW-Nle-DMeAsp-MePhe	Compound 30	9	yGlu-(OEG)2 linker between C18 fatty acid and peptide	Amidation	Linear	Mix	sTyr = Sulfated Tyrosine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	112 (Terminal Half Life)	Hours	403200	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.44 (In Vitro CCK-1R Potency)
5501	30624060	2019	D-sTyr-LGW-Nle-DMeAsp-Me1Nal	Compound 48	9	yGlu-(OEG)2 linker between C18 fatty acid and peptide	Amidation	Linear	Mix	sTyr = Sulfated Tyrosine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine, Me1Nal = N-methyl-1-naphthylalanine	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	147 (Terminal Half Life)	Hours	529200	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.39 (In Vitro CCK-1R Potency)
5502	30624060	2019	D-sTyr-Nle-GW-Nle-DMeAsp-1Nal	Compound 49	9	yGlu-(OEG)2 linker between C18 fatty acid and peptide	Amidation	Linear	Mix	sTyr = Sulfated Tyrosine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine, Me1Nal = N-methyl-1-naphthylalanine	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	140 (Terminal Half Life)	Hours	504000	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.44 (In Vitro CCK-1R Potency)
5503	30624060	2019	βAsp-Phe(4sm)-Nle-GW-Nle-DMeAsp-MePhe	Compound 56	9	yGlu-(OEG)2 linker between C18 fatty acid and peptide	Amidation	Linear	Mix	sTyr = Sulfated Tyrosine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine, Phe(4sm) = 4-sulfomethylphenylalanine, βAsp at position 1	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	106 (Terminal Half Life)	Hours	381600	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.50 (In Vitro CCK-1R Potency)
5505	30606721	2019	ACYNEFGCEDFYDIC	BCY-B3	15	Acetylation	Free	Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C8, C15)	L	None	Bicyclic peptide derivative	For imaging and targeting of proteins overexpressed by tumors	37C up to 24 hours	4 μmol/L	>48	Hours	172800	Mouse plasma protease	Radio-HPLC	Mouse plasma	In Vitro	None	None	KD(nM) = 1.22 ± 0.40
5506	30606721	2019	ACaNE-1Nal-aCEDFYDC	BCY-C3	15	Acetylation	Free	Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C9, C15)	Mix	(1Nal),(D-Ala) at position 3,(tBuGly) at Asp14	Bicyclic peptide derivative	For imaging and targeting of proteins overexpressed by tumors	37C up to 24 hours	4 μmol/L	>48	Hours	172800	Mouse plasma protease	LC-MS	Mouse plasma	In Vitro	None	None	N.A.
5507	30606721	2019	ACaNE-1Nal-aCEDFYDC	BCY-C2.	15	Acetylation	Free	Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C9, C15)	Mix	(1Nal),(D-Ala) at position 3,(tBuGly) at Asp14	Bicyclic peptide derivative	For imaging and targeting of proteins overexpressed by tumors	37C up to 24 hours	4 μmol/L	>48	Hours	172800	Mouse plasma protease	Radio-HPLC	Mouse plasma	In Vitro	None	None	KD(nM) = 0.5 ± 0.2
5508	30606721	2019	ACYNEFGCEDFYDIC	BCY-B5	15	Acetylation	Free	Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C8, C15)	L	None	Bicyclic peptide derivative	For imaging and targeting of proteins overexpressed by tumors	37C up to 24 hours	4 μmol/L	>48	Hours	172800	Human plasma protease	LC-MS/MS	Human plasma	In Vitro	None	None	N.A.
5509	30606721	2019	ACYNEFGCEDFYDIC	BCY-B3	15	Acetylation	Free	Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C8, C15)	L	None	Bicyclic peptide derivative	For imaging and targeting of proteins overexpressed by tumors	37C up to 24 hours	4 μmol/L	>48	Hours	172800	Human plasma protease	Radio-HPLC	Human plasma	In Vitro	None	None	KD(nM) = 1.22 ± 0.40
5510	30606721	2019	ACaNE-1Nal-aCEDFYDC	BCY-C3	15	Acetylation	Free	Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C9, C15)	Mix	(1Nal),(D-Ala) at position 3,(tBuGly) at Asp14	Bicyclic peptide derivative	For imaging and targeting of proteins overexpressed by tumors	37C up to 24 hours	4 μmol/L	>48	Hours	172800	Human plasma protease	LC-MS	Human plasma	In Vitro	None	None	N.A.
5511	30606721	2019	ACaNE-1Nal-aCEDFYDC	BCY-C2.	15	Acetylation	Free	Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C9, C15)	Mix	(1Nal),(D-Ala) at position 3,(tBuGly) at Asp14	Bicyclic peptide derivative	For imaging and targeting of proteins overexpressed by tumors	37C up to 24 hours	4 μmol/L	>48	Hours	172800	Human plasma protease	Radio-HPLC	Human plasma	In Vitro	None	None	KD(nM) = 0.5 ± 0.2
5551	30165247	2019	MAPTSAFLTALVLLSCNAICSLGCDLPQTHSLAHTRALRLLAQMRRISPFSCLDHRRDFGSPHEAFGGNQVQKAQAMALVHEMLQQTFQLFSTEGSAAAWNESLLHQFCTGLDQQLRDLEACVMQEAGLEGTPLLEEDSILAVRKYFHRLTLYLQEKSYSPCAWEIVRAEVMRSFSSSRNLQDRLRKKEMEKEKKVKYFLRKSAFGLASVSAAFLVGSTVFAVDSPIEDTPIIRNGGELTNLLGNSETTLALRNEESATADLTAAAVADTVAAAAAENAGAAAWEAAAAADALAKAKADALKEFNKYGVSDYYKNLINNAKTVEGVKDLQAQVVESAKKARISEATDGLSDFLKSQTPAEDTVKSIELAEAKVLANRELDKYGVSDYHKNLINNAKTVEGVKDLQAQVVESAKKARISEATDGLSDFLKSQTPAEDTVKSIELAEAKVLANRELDKYGVSDYYKNLINNAKTVEGVKALIDEILAALPKTDTYKLILNGKTLKGETTTEAVDAATAEKVFKQYANDNGVDGEWTYDDATKTFTVTEKPEVIDASELTPAVTTYKLVINGKTLKGETTTEADAATAEKVFKQYANDNGVDGEWTYDDATKTFTVTEKPEVIDASELTPAVTTYKLVINGKTLKGETTTKAVDAETAEKAFKQYANDNGVDGVWTYDDATKTFTVTEMVTEVPGDAPTEPEKPEASIPLVPLTPATPIAKDDAKKDDTKKEDAKKPEAKKEDAKKAETLPTTGEGSNPFFTAAALAVMAGAGALAVASKRKED	PoIFNα -C2	781	Free	SPG C2 domain	Linear	L	None	Fusion protein of Ig-binding C2 domain of streptococcal protein G (SPG) with PoIFN-α	Antiviral And Immune Regulatory Effects	Serum samples were collected at 0.5, 2.0, 4.0, 8.0, 12, 24,48, 72, 96, 120 and 144 h post injection	2.5 mg/kg	56.82 ± 0.70	Hours	204552	Rats serum protease	ELISA	Rats serum	In Vivo	GenBank accession no. AY345969, X06173.1	None	On MDBK cell, PoIFNα-C2 protein showed almost 10-fold lower anti-VSV activity (3.0 × 107 U/μM) than that (2.4 × 108 U/μM) of PoIFN-α standard
5553	30165247	2019	MAPTSAFLTALVLLSCNAICSLGCDLPQTHSLAHTRALRLLAQMRRISPFSCLDHRRDFGSPHEAFGGNQVQKAQAMALVHEMLQQTFQLFSTEGSAAAWNESLLHQFCTGLDQQLRDLEACVMQEAGLEGTPLLEEDSILAVRKYFHRLTLYLQEKSYSPCAWEIVRAEVMRSFSSSRNLQDRLRKKEMEKEKKVKYFLRKSAFGLASVSAAFLVGSTVFAVDSPIEDTPIIRNGGELTNLLGNSETTLALRNEESATADLTAAAVADTVAAAAAENAGAAAWEAAAAADALAKAKADALKEFNKYGVSDYYKNLINNAKTVEGVKDLQAQVVESAKKARISEATDGLSDFLKSQTPAEDTVKSIELAEAKVLANRELDKYGVSDYHKNLINNAKTVEGVKDLQAQVVESAKKARISEATDGLSDFLKSQTPAEDTVKSIELAEAKVLANRELDKYGVSDYYKNLINNAKTVEGVKALIDEILAALPKTDTYKLILNGKTLKGETTTEAVDAATAEKVFKQYANDNGVDGEWTYDDATKTFTVTEKPEVIDASELTPAVTTYKLVINGKTLKGETTTEADAATAEKVFKQYANDNGVDGEWTYDDATKTFTVTEKPEVIDASELTPAVTTYKLVINGKTLKGETTTKAVDAETAEKAFKQYANDNGVDGVWTYDDATKTFTVTEMVTEVPGDAPTEPEKPEASIPLVPLTPATPIAKDDAKKDDTKKEDAKKPEAKKEDAKKAETLPTTGEGSNPFFTAAALAVMAGAGALAVASKRKED	PoIFNα -C2	781	Free	SPG C2 domain	Linear	L	None	Fusion protein of Ig-binding C2 domain of streptococcal protein G (SPG) with PoIFN-α	Antiviral And Immune Regulatory Effects	Serum samples were collected at 0.5, 2.0, 4.0, 8.0, 12, 24,48, 72, 96, 120 and 144 h post injection	2.5 mg/kg	61.58 ± 1.998	Hours	221688	Rats serum protease	ELISA	Rats serum	In Vivo	None	None	On MDBK cell, PoIFNα-C2 protein showed almost 10-fold lower anti-VSV activity (3.0 × 107 U/μM) than that (2.4 × 108 U/μM) of PoIFN-α standard
5644	30309736	2018	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSC	PE	40	Free	PEG(20k)	Linear	L	None	Exendin-4 analogs	Antidiabetes	Blood samples were collected at 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72,96, and 144 h	100 nmoL/kg	31.4 ± 1.6	Hours	113040	SD rats serum protease	ELISA	SD rats serum	In Vivo	PDB id: 1JRJ	None	EC50 values of Exendin-4, those of PE to activate GLP-1R in vitro was slightly decreased by 6.9- fold
5645	30309736	2018	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSC	PE	40	Free	PEG(20k)	Linear	L	None	Exendin-4 analogs	Antidiabetes	Blood samples were collected at 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72,96, and 144 h	200 nmol/kg	31.7 ± 1.5	Hours	114120	SD rats serum protease	ELISA	SD rats serum	In Vivo	None	None	EC50 values of Exendin-4, those of PE to activate GLP-1R in vitro was slightly decreased by 6.9- fold
5646	30309736	2018	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSC	PE	40	Free	PEG(20k)	Linear	L	None	Exendin-4 analogs	Antidiabetes	Blood samples were collected at 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72,96, and 144 h	400 nmol/kg	30.7 ± 2.2	Hours	110520	SD rats serum protease	ELISA	SD rats serum	In Vivo	None	None	EC50 values of Exendin-4, those of PE to activate GLP-1R in vitro was slightly decreased by 6.9- fold
5648	30309736	2018	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSC	PE	40	Free	PEG(20k)	Linear	L	Introduction of Cys at C terminal of Exendin-4	Exendin-4 analogs	Antidiabetes	For 33 consecutive days, after the first administration for 6 days,eight rats received PE (100 nmoL/kg, 200 mL, s.c.) once every 84 h	100 nmoL/kg	27.6 ± 5.1	Hours	99360	SD rats serum protease	ELISA	SD rats serum	In Vivo	None	None	EC50 values of Exendin-4, those of PE to activate GLP-1R in vitro was slightly decreased by 6.9- fold
5654	30174173	2018	GCLEFWWKCNPNDDKCCRPKLKCSKLFKLCNFSSA	GsMTx4	35	Free	Free	Linear	L	None	Isolated from the venom of the spider Grammostola spatulata	Treatment of Duchenne Muscular Dystrophy	6 times over 14 days – sacrifice on day 28	10 mg/kg	1	Week	604800	Mice plasma protease	LC-MS	Mice plasma	In Vivo	https://pmc.ncbi.nlm.nih.gov/articles/PMC2217226/	None	1 μM GsMTx4 in vitro experiments shows 0.1–5.0 μM effective in suppressing MSC activity in various disease models
5685	30023916	2018	HGEGTFTSDVSSYLEGQAAKEFIAWLVKGRC	Conjugate 2	31	CH90 linked by linker EDA–(LMDS)	Free	Linear	L	Substituition of G for A at position 2	Synthetic	Antidiabetes	Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration	300 nmol/kg	25.3 (T1/2 Elimination Half life)	Hours	91080	Mice plasma protease	ELISA	Mice plasma	In Vivo	None	None	EC50 = 9.9 nM
5686	30023916	2018	HGEGTFTSDVSSYLEGQAAKEFIAWLVKGRC	Conjugate 2	31	CH90 linked by linker EDA–(LMDS)	Free	Linear	L	Substituition of G for A at position 2	Synthetic	Antidiabetes	Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration	300 nmol/kg	30.3 (T1/2 Elimination Half life)	Hours	109080	Mice plasma protease	ELISA	Mice plasma	In Vivo	None	None	EC50 = 9.9 nM
5687	30023916	2018	HGEGTFTSDVSSYLEGQAAKEFIAWLVKGRC	Conjugate 3	31	Free	HPN50 linked by linker EDA–(LMDS)	Linear	L	Substituition of G for A at position 2	Synthetic	Antidiabetes	Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration	300 nmol/kg	33.6 (T1/2 Elimination Half life)	Hours	120960	Mice plasma protease	ELISA	Mice plasma	In Vivo	None	None	EC50 = 7.0 nM
5688	30023916	2018	HGEGTFTSDVSSYLEGQAAKEFIAWLVKGRC	Conjugate 3	31	Free	HPN50 linked by linker EDA–(LMDS)	Linear	L	Substituition of G for A at position 2	Synthetic	Antidiabetes	Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration	300 nmol/kg	25.8 (T1/2 Elimination Half life)	Hours	92880	Mice plasma protease	ELISA	Mice plasma	In Vivo	None	None	EC50 = 7.0 nM
5692	30023916	2018	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG	10 kDa PEG-modified GLP-1	31	PEG10K	Free	Linear	L	None	Synthetic	Antidiabetes	37 °C for 2 h	N.A.	105.5 (T1/2 Elimination Half life)	Hours	378000	0.125 U/12.5 Μl C-Abc And 0.0125 U/12.5 Μl Chondroitinase Acii	HPLC	N.A.	In Vitro	None	None	N.A.
5695	30012756	2018	L-threonyl-L-tryptophanyl-L-isoleucyl-L-2,4-diaminobutyryl-L-ornithyl-D-2,4-diaminobutyryl-L-2,4-diaminobutyryl-L-tryptophanyl-L-2,4-diaminobutyryl-L-2,4-diaminobutyryl-L-alanyl-L-seryl,D-prolyl-L-prolyl	Murepavadin	14	Free	Free	Cyclic (N-C terminal end)	Mix	Acetate	Synthetic	Antimicrobial	Blood samples were taken predose and 1, 2, 3, 3.5, 4, 5, 6, 9, 15, and 27 h after the start of infusion. For subjects with renal impairment, additional samples were taken at 30, 36, and 48 h, and at 72 h for subjects with severe renal function impairment	2.2 mg/kg	24.1	Hours	86760	Human plasma protease	LC-MS with electrospray ionization assay	Human plasma (Severe Renal impairment group)	In Vivo	https://sci-hub.st/10.1080/14787210.2018.1441024	None	MIC50 = 0.12 mg/L against P. aeruginosa
5706	29799205	2018	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG	Liraglutide	32	Free	Free	Linear	L	Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu	GLP-1 analogs	Antidiabetes	37°C over 72 h	1000 ng/mL	35.4	Hours	127440	SD rats plasma protease	LC-MS/MS.	Rats plasma	In Vitro	None	None	N.A.
5708	29799205	2018	HGEGTYTNDVTEYLEEEAA-X2-EFIEWLIKGK	4b	29	Free	Free	Linear	L	X2 = structure given in paper	Xenopus GLP-1 analogs	Antidiabetes	37°C over 72 h	1000 ng/mL	27.7	Hours	99720	Rats plasma protease	LC-MS/MS.	Rats plasma	In Vitro	None	None	EC50(nM) = 0.97 ± 0.11
5709	29799205	2018	HGEGTYTNDVTEYLEEEAA-X3-EFIEWLIKGK	4c	29	Free	Free	Linear	L	X3 = structure given in paper	Xenopus GLP-1 analogs	Antidiabetes	37°C over 72 h	1000 ng/mL	37.7	Hours	135720	Rats plasma protease	LC-MS/MS.	Rats plasma	In Vitro	None	None	EC50(nM) = 1.49 ± 0.13
5711	29799205	2018	HGEGTYTNDVTEYLEEEAAKEFIEWLI-X2-GK	4e	29	Free	Free	Linear	L	X2 = structure given in paper	Xenopus GLP-1 analogs	Antidiabetes	37°C over 72 h	1000 ng/mL	29.4	Hours	105840	Rats plasma protease	LC-MS/MS.	Rats plasma	In Vitro	None	None	EC50(nM) = 1.68 ± 0.18
5712	29799205	2018	HGEGTYTNDVTEYLEEEAAKEFIEWLI-X3-GK	4f	29	Free	Free	Linear	L	X3 = structure given in paper	Xenopus GLP-1 analogs	Antidiabetes	37°C over 72 h	1000 ng/mL	37.3	Hours	134280	Rats plasma protease	LC-MS/MS.	Rats plasma	In Vitro	None	None	EC50(nM) =6.35 ± 0.39
5714	29799205	2018	HGEGTYTNDVTEYLEEEAA-X2-EFIEWLIKGKPSSGAPPPS	4h	38	Free	Free	Linear	L	X2 = structure given in paper	Xenopus GLP-1 analogs	Antidiabetes	37°C over 72 h	1000 ng/mL	31.6	Hours	113760	Rats plasma protease	LC-MS/MS.	Rats plasma	In Vitro	None	None	EC50(nM) = 0.57 ± 0.19
5715	29799205	2018	HGEGTYTNDVTEYLEEEAA-X3-EFIEWLIKGKPSSGAPPPS	4i	38	Free	Free	Linear	L	X3 = structure given in paper	Xenopus GLP-1 analogs	Antidiabetes	37°C over 72 h	1000 ng/mL	39.5	Hours	142200	Rats plasma protease	LC-MS/MS.	Rats plasma	In Vitro	None	None	EC50(nM) =0.88 ± 0.43
5716	29799205	2018	HGEGTYTNDVTEYLEEEAAKEFIEWLI-X1-GKPSSGAPPPS	4j	38	Free	Free	Linear	L	X1 = structure given in paper	Xenopus GLP-1 analogs	Antidiabetes	37°C over 72 h	1000 ng/mL	24.1	Hours	86760	Rats plasma protease	LC-MS/MS.	Rats plasma	In Vitro	None	None	EC50(nM) = 0.31 ± 0.03
5717	29799205	2018	HGEGTYTNDVTEYLEEEAAKEFIEWLI-X2-GKPSSGAPPPS	4k	38	Free	Free	Linear	L	X2 = structure given in paper	Xenopus GLP-1 analogs	Antidiabetes	37°C over 72 h	1000 ng/mL	30.1	Hours	108360	Rats plasma protease	LC-MS/MS.	Rats plasma	In Vitro	None	None	EC50(nM) = 0.68 ± 0.24
5718	29799205	2018	HGEGTYTNDVTEYLEEEAAKEFIEWLI-X3-GKPSSGAPPPS	4l	38	Free	Free	Linear	L	X3 = structure given in paper	Xenopus GLP-1 analogs	Antidiabetes	37°C over 72 h	1000 ng/mL	40.5	Hours	145800	Rats plasma protease	LC-MS/MS.	Rats plasma	In Vitro	None	None	EC50(nM) = 2.09 ± 0.21
5720	29799205	2018	HGEGTYTNDVTEYLEEEAA-X2-EFIEWLIKGKPSSGAPPSKKKKKK	4n	43	Free	Free	Linear	L	X2 = structure given in paper	Xenopus GLP-1 analogs	Antidiabetes	37°C over 72 h	1000 ng/mL	26.6	Hours	95760	Rats plasma protease	LC-MS/MS.	Rats plasma	In Vitro	None	None	EC50(nM) = 0.44 ± 0.11
5721	29799205	2018	HGEGTYTNDVTEYLEEEAA-X3-EFIEWLIKGKPSSGAPPSKKKKKK	4o	43	Free	Free	Linear	L	X3 = structure given in paper	Xenopus GLP-1 analogs	Antidiabetes	37°C over 72 h	1000 ng/mL	36.4	Hours	131040	Rats plasma protease	LC-MS/MS.	Rats plasma	In Vitro	None	None	EC50(nM) = 0.98 ± 0.18
5723	29799205	2018	HGEGTYTNDVTEYLEEEAAKEFIEWLI-X2-GKPSSGAPPSKKKKKK	4q	43	Free	Free	Linear	L	X2 = structure given in paper	Xenopus GLP-1 analogs	Antidiabetes	37°C over 72 h	1000 ng/mL	27.2	Hours	97920	Rats plasma protease	LC-MS/MS.	Rats plasma	In Vitro	None	None	EC50(nM) = 0.48 ± 0.08
5724	29799205	2018	HGEGTYTNDVTEYLEEEAAKEFIEWLI-X3-GKPSSGAPPSKKKKKK	4r	43	Free	Free	Linear	L	X3 = structure given in paper	Xenopus GLP-1 analogs	Antidiabetes	37°C over 72 h	1000 ng/mL	38.7	Hours	139320	Rats plasma protease	LC-MS/MS.	Rats plasma	In Vitro	None	None	EC50(nM) = 0.61 ± 0.24
5741	29732120	2018	RGDfV, RGDfV	Analogue 11 and 9b	5	Free	Free	Macrocyclic (N-C terminal end)	Mix	Thio substiuition in Asp (analogue 11) and Phe (analogue 9b)	Synthetic	Inhibits pro-angiogenic integrins	At various time points (0, 1, 3, 5. 7, 9, 12, 24, 36, 48, 60 and 72 h)	1 mg/ml	36	Hours	129600	Human serum protease	HPLC	Human serum	In Vitro	None	None	IC50 value of 11 shows that 11 is poorer than Cilen
5745	29693715	2018	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	Antidiabetes	Blood samples were taken on day 1 at up to 30 minutes prior to the first administration of semaglutide and 1 hour after dosing; predose on days 2, 4, 6, 8, and 9; on day 10 at up to 30 minutes predose	5 mg for 5 days followed by 10 mg for 5 days	156.4	Hours	563040	Human plasma protease	LC‐MS/MS	Human plasma (Normal hepatic function) after 10th dosing	In Vivo	None	None	N.A.
5746	29693715	2018	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	Antidiabetes	Blood samples were taken on day 1 at up to 30 minutes prior to the first administration of semaglutide and 1 hour after dosing; predose on days 2, 4, 6, 8, and 9; on day 10 at up to 30 minutes predose	5 mg for 5 days followed by 10 mg for 5 days	142.1	Hours	511560	Human plasma protease	LC‐MS/MS	Human plasma (Mild hepatic function) after 10th dosing	In Vivo	None	None	N.A.
5747	29693715	2018	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	Antidiabetes	Blood samples were taken on day 1 at up to 30 minutes prior to the first administration of semaglutide and 1 hour after dosing; predose on days 2, 4, 6, 8, and 9; on day 10 at up to 30 minutes predose	5 mg for 5 days followed by 10 mg for 5 days	146.7	Hours	528120	Human plasma protease	LC‐MS/MS	Human plasma (Moderate hepatic function) after 10th dosing	In Vivo	None	None	N.A.
5748	29693715	2018	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	Antidiabetes	Blood samples were taken on day 1 at up to 30 minutes prior to the first administration of semaglutide and 1 hour after dosing; predose on days 2, 4, 6, 8, and 9; on day 10 at up to 30 minutes predose	5 mg for 5 days followed by 10 mg for 5 days	153.7	Hours	553320	Human plasma protease	LC‐MS/MS	Human plasma (Severe hepatic function) after 10th dosing	In Vivo	None	None	N.A.
5767	29623579	2018	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	Antidiabetes	After 10th dosing	5 days of semaglutide 5 mg followed by 5 days of semaglutide 10 mg	151.7	Hours	546120	Human plasma protease	LC–MS/MS	Human plasma (Normal renal function)	In Vivo	https://pmc.ncbi.nlm.nih.gov/articles/PMC8736331/	None	N.A.
5768	29623579	2018	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	Antidiabetes	After 10th dosing	5 days of semaglutide 5 mg followed by 5 days of semaglutide 10 mg	159.3	Hours	573480	Human plasma protease	LC–MS/MS	Human plasma (Mild renal function )	In Vivo	None	None	N.A.
5769	29623579	2018	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	Antidiabetes	After 10th dosing	5 days of semaglutide 5 mg followed by 5 days of semaglutide 10 mg	162.8	Hours	586080	Human plasma protease	LC–MS/MS	Human plasma (Moderate renal function)	In Vivo	None	None	N.A.
5770	29623579	2018	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	Antidiabetes	After 10th dosing	5 days of semaglutide 5 mg followed by 5 days of semaglutide 10 mg	164.9	Hours	593640	Human plasma protease	LC–MS/MS	Human plasma (Severe renal function group)	In Vivo	None	None	N.A.
5771	29623579	2018	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	Antidiabetes	After 10th dosing	5 days of semaglutide 5 mg followed by 5 days of semaglutide 10 mg	152.8	Hours	550080	Human plasma protease	LC–MS/MS	Human plasma (ESRD Renal function group)	In Vivo	None	None	N.A.
5785	29577579	2018	RPRLSHKGPMPF	Fc‐apelin‐13 fusion protein	12	Fc linked by (GGGS)3 linker at N terminus	Free	Linear	L	None	Fc‐apelin‐13 fusion protein	Antidiabetes and Anti‐Heart Failure Activities	About 10 μL of blood was collected at each time point of 0, 1, 2, 4, 8, 24, 32, 48, 56, and 72 hours after administration	5 mg/kg	~33	Hours	118800	Mice Plasma Protease	Western blotting	Mice plasma	In Vivo	None	None	EC50 values of the Fc‐apelin‐13 fusion protein= 12.0 ± 1.1 nM for cAMP suppression
5790	29536338	2018	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	Antidiabetes	GLP-1R agonist	Blood samples for pharmacokinetic assessment of semaglutide were taken before the first dose (0 h), for 1 week following a single 0.25 mg dose(6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120,144, 168 h), then weekly prior to the next dose(trough values), and for 5 weeks following thefinal dose (0 h then 6, 12, 18, 24, 30, 36, 42, 48,60, 72, 84, 96, 120, 144, 168, 336, 504, 672 and 840 h).	0.5 mg	145	Hours	522000	Human plasma protease	LC–MS/MS	Human plasma (Japanese subjects)	In Vivo	None	None	N.A.
5791	29536338	2018	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	Antidiabetes	GLP-1R agonist	Blood samples for pharmacokinetic assessment of semaglutide were taken before the first dose (0 h), for 1 week following a single 0.25 mg dose(6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120,144, 168 h), then weekly prior to the next dose(trough values), and for 5 weeks following thefinal dose (0 h then 6, 12, 18, 24, 30, 36, 42, 48,60, 72, 84, 96, 120, 144, 168, 336, 504, 672 and 840 h).	1 mg	163	Hours	586800	Human plasma protease	LC–MS/MS	Human plasma (Japanese subjects)	In Vivo	None	None	N.A.
5792	29536338	2018	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	Antidiabetes	GLP-1R agonist	Blood samples for pharmacokinetic assessment of semaglutide were taken before the first dose (0 h), for 1 week following a single 0.25 mg dose(6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120,144, 168 h), then weekly prior to the next dose(trough values), and for 5 weeks following thefinal dose (0 h then 6, 12, 18, 24, 30, 36, 42, 48,60, 72, 84, 96, 120, 144, 168, 336, 504, 672 and 840 h).	0.5 mg	159	Hours	572400	Human plasma protease	LC–MS/MS	Human plasma (Caucasian subjects)	In Vivo	None	None	N.A.
5793	29536338	2018	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	Antidiabetes	GLP-1R agonist	Blood samples for pharmacokinetic assessment of semaglutide were taken before the first dose (0 h), for 1 week following a single 0.25 mg dose(6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120,144, 168 h), then weekly prior to the next dose(trough values), and for 5 weeks following thefinal dose (0 h then 6, 12, 18, 24, 30, 36, 42, 48,60, 72, 84, 96, 120, 144, 168, 336, 504, 672 and 840 h).	1 mg	167	Hours	601200	Human plasma protease	LC–MS/MS	Human plasma (Caucasian subjects)	In Vivo	None	None	N.A.
5805	29517911	2018	CSFPY-hArg-CAHQDLC	2d	13	Acetylation	Free	Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene)	L	Trp3 → Phe3, Pro4 → Aze4, Ala5 → Tyr5, Arg6 → HArg6, Leu8 → Ala(ψCH2NH)6 substituitions	2a analogue	Antidiabetes (Treatment of Diabetic Macular Edema)	The animals were sacrificed 15 min, 1 h, 4 h, 8 h, 24 h, 48, and 96 h after injection	2 mg/mL	39 ± 2	Hours	140400	Rabbit eye plasma protease	HPLC	Rabbit eye plasma	In Vivo	None	None	Ki Values (nM) = 3,400 ± 200 against PKal from Rabbit
5865	29421564	2018	CRPKPQQFFGLM	HDL-SP	34	MPB-Mal modified, additional cysteine residue on N-terminus of SP	Free	Linear	L	None	Synthetic	Therapeutic Angiogenesis in Diabetic Hindlimb Ischemia	0 to 72 h at 37°C	5 nmol	117	Hours	421200	Human serum protease	ELISA	Human serum	In Vitro	None	None	N.A.
5867	29421564	2018	CRPKPQQFFGLM	HDL-SP	34	MPB-Mal modified, additional cysteine residue on N-terminus of SP	Free	Linear	L	None	Synthetic	Therapeutic Angiogenesis in Diabetic Hindlimb Ischemia	0 to 72 h at 37°C	5 nmol	30	Hours	108000	Diabetic rats serum protease	ELISA	Diabetic rats serum	In Vitro	None	None	N.A.
5870	29421564	2018	CRPKPQQFFGLM	HDL-SP	34	MPB-Mal modified, additional cysteine residue on N-terminus of SP	Free	Linear	L	None	Synthetic	Therapeutic Angiogenesis In Diabetic Hindlimb Ischemia	0 to 72 h at 37°C	5 nmol	60	Hours	216000	Mice serum protease	ELISA	Mice serum	In Vivo	None	None	N.A.
5872	29421564	2018	CRPKPQQFFGLM	HDL-SP	34	MPB-Mal modified, additional cysteine residue on N-terminus of SP	Free	Linear	L	None	Synthetic	Therapeutic Angiogenesis In Diabetic Hindlimb Ischemia	0 to 72 h at 37°C	5 nmol	96	Hours	345600	Diabetic rats serum protease	ELISA	Diabetic rats serum	In Vitro	None	None	N.A.
5897	28954201	2018	GFCRCLCRRGVCRCICTR	RTD-1	18	Free	Free	Cyclic	L	None	Derived from rhesus	Attenuates Endotoxin-Induced Acute Lung Injury	Received RTD-1 at 0, 0.2, 1,5, or 25 mg/kg 0.5 hour before LPS challenge	5 or 25 mg/kg	30 (Terminal Half Life)	Hours	108000	Mice plasma protease	LC-MS	Mice plasma (LPS-challenged )	In Vivo	https://pmc.ncbi.nlm.nih.gov/articles/PMC3024902/	None	IC50= 4.5 μg/ml
5967	28741871	2017	Y-Aib-EGTFTSDYSIYLDKQAA-Aib-EFVNWLLAGGPSSGAPPPSK	RG7697	40	Free	Acylated at a C-terminal lysine with a saturated C16 lipid	Cyclic (L14-E21, Q17-N24 Lactam Bridge)	L	Aib modification at position 2, 20	chimera of GLP-1 and GIP peptides	Antidiabetes	RG7697 were collected in EDTA-containing tubes initially at predose, 1, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 30, 36, 48, 60, 72 and 96 hours post dose, and at follow-up visit (first 2 cohorts). In later cohorts, additional time points were collected at 2.5, 3 and 3.5 hours post dose, while the 96-hour sample was deleted	1.8 mg	25.4 (T1/2b- Appearant Terminal Half Life)	Hours	91440	Human plasma protease	LC-MS	Human plasma	In Vivo	None	None	for human GLP-1 (EC50 = 5 pM) and GIP (EC50 = 3 pM) receptors
5991	28619366	2017	HAEGTFTSDVSSYLEGQAAKEFIAWLVRGRG	BPI-3016	30	Free	Free	Linear	L	substituting –NHCO– amide bond of Ala2 with –CH(CF3)NH– to form (A'), Lys20 conjugation with C18, K34R modification	hGLP-1 analogs	Antidiabetes	Blood samples collected at −2 (pre-administration), 2, 8, 22, 46, 94, 118, 142, and 166 h after administration	0.2 mg/kg	95 ± 20	Hours	342000	Diabetic cynomoglus monkeys plasma protease	electrospray ionization LC–MS/MS	Diabetic cynomoglus monkeys plasma	In Vivo	None	None	Single subcutaneous injection of 0.4 mg/kg BPI-3016 significantly lowered the fasting glucose level at 46 h after administration
5993	28605180	2017	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	MS-exenatide (MeSO2-)	39	Tetra PEG hydrogel linked with exenatide using linker MeSO2-	Amidation	Linear	L	None	Exenatide analogs	Antidiabetes	Blood samples (300 µL) were drawn at 0, 1, 2, 4, 8, 24, 48, 72, 120, 168, 240, 336, 432, 504, 600, 672 h for both linkers and additional samples were obtained at 840, 1008, 1176, 1344, 1512, 1680, 1848, and 2016 h for the linker with Mod = CN	1.3 µmol/g	244	Hours	878400	Mouse serum protease	LC-MS/MS	Mouse serum	In Vivo	PDB id: 7MLL	None	IC50(nM) = 0.21 ±0.0 for exenatide
5994	28605180	2017	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	MS-exenatide (-CN)	39	Tetra PEG hydrogel linked with exenatide using linker -CN	Amidation	Linear	L	None	Exenatide analogs	Antidiabetes	Blood samples (300 µL) were drawn at 0, 1, 2, 4, 8, 24, 48, 72, 120, 168, 240, 336, 432, 504, 600, 672 h for both linkers and additional samples were obtained at 840, 1008, 1176, 1344, 1512, 1680, 1848, and 2016 h for the linker with Mod = CN	1.4 µmol/g	730	Hours	2628000	Mouse serum protease	LC-MS/MS	Mouse serum	In Vivo	PDB id: 7MLL	None	IC50(nM) = 0.21 ±0.0 for exenatide
5995	28605180	2017	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	MS-exenatide (MeSO2-)	39	Tetra PEG hydrogel linked with exenatide using linker MeSO2-	Amidation	Linear	L	None	Exenatide analogs	Antidiabetes	Blood samples (300 µL) were drawn at 0, 1, 2, 4, 8, 24, 48, 72, 120, 168, 240, 336, 432, 504, 600, 672 h for both linkers and additional samples were obtained at 840, 1008, 1176, 1344, 1512, 1680, 1848, and 2016 h for the linker with Mod = CN	1.3 µmol/g	310	Hours	1116000	Rats serum protease	LC-MS/MS	Rats serum	In Vivo	PDB id: 7MLL	None	IC50(nM) = 0.21 ±0.0 for exenatide
5996	28605180	2017	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	MS-exenatide (-CN)	39	Tetra PEG hydrogel linked with exenatide using linker -CN	Amidation	Linear	L	None	Exenatide analogs	Antidiabetes	Blood samples (300 µL) were drawn at 0, 1, 2, 4, 8, 24, 48, 72, 120, 168, 240, 336, 432, 504, 600, 672 h for both linkers and additional samples were obtained at 840, 1008, 1176, 1344, 1512, 1680, 1848, and 2016 h for the linker with Mod = CN	1.4 µmol/g	880	Hours	3168000	Rats serum protease	LC-MS/MS	Rats serum	In Vivo	PDB id: 7MLL	None	IC50(nM) = 0.21 ±0.0 for exenatide
6020	28437610	2017	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	m-exendin-4	39	Free	Amidation	Linear	L	None	GLP-1 analogs	Antidiabetes	N.A.	25 nmol/kg	43.11	Hours	155196	Murine plasma protease	ELISA	Murine plasma	In Vivo	PDB id: 7MLL	None	N.A.
6024	28389388	2017	ASCRTPKDCADPCRKETGCPYGKCMNRKCKCNRC	PEG-HsTX1[R14A]	34	PEGylation	Amidation	Cyclic (C3-C24, C9-C29, C13-C34 Disulfide Linkage)	L	Substituting arginine 14 with alanine	From scorpion Heterometrus spinnifer	Immunomodulation in Inflammatory Arthritis	2 hours	1 mg/kg	37.3	Hours	134280	Lewis rats serum protease	Anti-PEG ELISA	Lewis rats serum	In Vivo	https://pmc.ncbi.nlm.nih.gov/articles/PMC3968461/	None	IC50 of 35.9 ± 6.3 nM
6031	28323965	2017	SSSSKAPPPSLPSPSRLPGPSDTPILPQFPTIPLSRLFQNAMLRAHRLHQLAFDTYEEFEEAYIPKEQKYSFLQAPQASLCFSESIPTPSNREQAQQKSNLQLLRISLLLIQSWLEPVGFLRSVFANSLVYGASDSDVYDLLKDLEEGIQTLMGRLEDGSPRTGQAFKQTYAKFDANSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGFSSSSKAPPPSLPSPSRLPGPSDTPILPQSSSSKAPPPSLPSPSRLPGPSDTPILPQ	MOD-4023	275	CTP fused to hGH	2 CTP fused	Linear	L	None	Synthetic	Treatment of GHD	Measured at the final randomized dose (following the second dose)	0.25 mg/kg	36.1	Hours	129960	Human serum protease	IDS-iSys chemiluminescence assay	Human serum	In Vivo	https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU, https://sci-hub.se/10.1021/acs.molpharmaceut.5b00868	None	EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells)
6048	28068664	2017	DPDNEAYEMPSEEGYQDYEPEA	scFv57R-ATS	22	Free	(ATS) was fused to the C-terminus of the anti-RV scFv57R	Linear	L	None	scFv57R-ATS fusion protein	Antiviral (against Rabies Virus)	37o C for 0-72 hours	0.5 mg/ml	33.9	Hours	122040	N.A.	ELISA	PBS	In Vitro	None	None	Neutralizing potency (IU/ml) = 2.9 ± 0.5 for polymer
6086	US 201715445066 A	2017	GASDEEIQDVSGTWYLKAMTVDRFKIASWPRSVTPMTLTTLEGGNLEAKVTMNWWGRSQEVKAVLERTDEPGKYTAQGDRHVAYIIRSHVKDHYIFYSEGNLQGETVPGVWLVGRDPKNNLEALEDFEKAAGARGLSTESILIPRQSETSSPGKLGGGGSLAEAKEAANAELDSYGVSDFYKRLIDKAKTVEGVEALKDAILAALPGKLN	SEQ ID NO 84	210	Free	ABP-G148 (Albumin binding protein) conjugation	Linear	L	None	Lipocalin muteins	Pcsk9-Specific Lipocalin Muteins	N.A.	N.A.	32	Hours	115200	Rats plasma protease	Sandwich ELISA	Rats plasma	In Vivo	None	US 201715445066 A	IC50(nM) = 1.09 without HSA for LDLR binding
6115	27558296	2016	QRPRLSHKGP-Nle-Aib-F	Compound 31	13	Palmitic acid conjugation	Free	Linear	L	Nle= Nor-leucine at position 11, Aib = 2-Aminoisobutyric acid at position 12	Apelin analogs	Inotropic Agent	Time points (0, 0.17, 0.5, 1, 2, 4, 6, 24 and 27 h)	1 µg/mL	29	Hours	104400	Wistar rats plasma protease	ESI-MS	Wistar rats plasma	In Vitro	None	None	EC50(nM) = 21.6 ± 4.5 for compound 31
6119	27393654	2016	CDLPQTHSLGSRRTLMLLAQMRKISLFSCLKDRHDFGFPQEEFGNQFQKAETIPVLHEMIQQIFNLFSTKDSSAAWDETLLDKFYTELYQQLNDLEACVIQGVGVTETPLMKEDSILAVRKYFQRITLYLKEKKYSPCAWEVVRAEIMRSFSLSTNLQESLRSKE-(PMPC)	IFN-PMPC	165	Free	poly(2-methacryloyloxyethyl phosphorylcholine)	Linear	L	None	Human derived	Antiproliferative, Immunoregulatory and Antiviral	At desired time points (1, 5, 15, 30 min, 1, 3, 6, 24,48, 72 and 96 h)	1 mg IFN-α equivalent/kg	51.6 (T1/2b-Terminal Half Life)	Hours	185760	Mice plasma protease	ELISA	Mice plasma	In Vivo	None	None	IC50 = 20.02 pg/mL
6120	27364558	2016	LPAGEKPEEGEPVLHVEAEPGFTARDKE	Biotinylated SSTN(IGF1R)	28	Free	Free	Linear	L	Biotinylation	Mouse derived	Dually Attack MM Tumor Cell Survival And Tumor Angiogenesis	terminally bled at 0, 0.1, 0.3, 1, 3, 6, 12 and 24 hr post-injection	0.365 mg/kg	27	Hours	97200	Female BALB/c mice serum	IR scanning using anti-biotin antibody	Female BALB/c mice serum	In Vivo	https://pmc.ncbi.nlm.nih.gov/articles/PMC3651771/	None	The growth of human CAG, RPMI-8226, KMS-12, U266, MM.1R and the mouse P3X63Ag8 myeloma cells was significantly reduced by a three-day treatment with 30 μM SSTNIGF1R
6128	27232339	2016	HAEGTFTSDVSSYLEGQAAKG{mut:E}FIAWLVKGGG	GLP-1-IgG2σ-Fc	31	Free	Human IgG2σ constant heavy-chain linked via a peptide linker (GGGSGGGSGGGS) with human GLP-1 (A8G/G26E/R36G) at C terminal	Linear	L	GLP-1 variant (A8G/G26E/R36G) linked to the human IgG2σ constant heavy-chain by a peptide linker (GGGSGGGSGGGS)	GLP-1 analogs	Antidiabetes	Blood (0.6 mL) was collected from the foreleg vein immediately pre-administration (time 0), and at 2, 4, 8, 12, 48, 72, 96, 192,240, and 288 h after a single subcutaneous injection of GLP-1-IgG2σ-Fc	0.1 mg/kg	57.1 ± 4.5	Hours	205560	Cynomolgus monkeys plasma protease	ELISA	Cynomolgus monkeys plasma	In Vivo	PDB id: 5VAI	None	Cells incubated with medium containing 16.8 mM glucose secreted significantly more insulin in the presence of 10 nM (5.2 ± 0.4 ng/mL) and 100 nM (7.3 ± 0.3 ng/mL) GLP-1-IgG2σ-Fc, as compared with control cells (2.5 ± 0.5 ng/mL)
6133	27217590	2016	CYIQNCGKG	PF1	9	Free	Amidation	Cyclic (C1-C6 Disulfide Linkage)	L	Substitution of the Pro7 to Gly and Leu8 to a Lys appended with a polyethylene glycol space and a palmitoyl group, Palm = Palmitic acid	OT analog	Non–brain-penetrant OT receptor agonist	Serial blood samples were collected from each mouse via the retro-orbital sinus at the following time points postdose: 0.5, 1, 2, 4, 6, and 24 hours	20 mg/kg	309	Hours	1112400	C57Bl/6J mice plasma protease	LC-MS/MS	C57BL/6J mice plasma	In Vivo	None	None	EC50(nM) = 0.025 (OTR agonist)
6136	27166982	2016	KG-Dpr-RFGTETVQKLAHQIYQFTDKDKDNVAPRSKISPQGY	ADM analogue 17	38	Tam (6-Carboxytetramethylrhodamine) labeling, Glycine substitution at position 1	Amidation	Cyclic (Dpr3-E8 Lactam Bridge)	L	K1, Dpr3 = Diaminopropionic acid,E8 substituitions and Pam = Palmitoylation modification at side chain of Lys1	ADM analogue	Treatment of Cardiovascular Diseases	37°C	0.00001 M	84.6	Hours	304560	Human blood plasma protease	RP-HPLC	Human blood plasma	In Vitro	None	None	EC50 = 13.2 nM for ADM analogue 15
6137	27166982	2016	KG-Dpr-RFGTETVQKLAHQIYQFTDKDKDNVAPRSKISPQGY	ADM analogue 20	38	Tam (6-Carboxytetramethylrhodamine) labeling, Glycine substitution at position 1	Amidation	Cyclic (Dpr3-E8 Lactam Bridge)	L	Nα-Methylation of Lysine at position 33, K1, Dpr3 = Diaminopropionic acid,E8 substituitions and Pam = Palmitoylation modification at side chain of Lys1	ADM analogue	Treatment of Cardiovascular Diseases	37°C	0.00001 M	126.2	Hours	454320	Human blood plasma protease	RP-HPLC	Human blood plasma	In Vitro	None	None	EC50 = 13.2 nM for ADM analogue 15
6141	27155328	2016	HGEGTFTSDLSQMEEEAVRLFIEWLKNGGPSSGAPPPS	I-3	38	Free	Amidation	Linear	L	X3(Fatty acid structure given in paper) linked with Ser11	Exendin-4 analogs	Antidiabetes	At 0, 1, 2, 4, 6, 8, 12, 24, 36, 48 and 72 h time points, 100 lL mixture was aliquoted	1000 ng/mL	35.6	Hours	128160	SD rats plasma protease	LC-MS/MS	SD rats plasma	In Vitro	None	None	EC50(pM) =38.47 ± 9.86
6152	26905040	2016	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSC	EX4-2K	40	Free	PEG(2KDa) linked with Ex-4 through Mal (Maleimide)	Linear	L	None	Exendin-4 analogs	Antidiabetes	37 °C	200 μg/mL	69.2	Hours	249120	Mice plasma protease	RP-HPLC	CLP-induced septic mice plasma	In Vitro	None	None	WT-EX4 bound to GLP-1R, with a dissociation constant of Kd(app) ≈ 0.142 nM
6153	26905040	2016	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSC	EX4-5K	40	Free	PEG(5KDa) linked with Ex-4 through Mal (Maleimide)	Linear	L	None	Exendin-4 analogs	Antidiabetes	37 °C	200 μg/mL	62.8	Hours	226080	Mice plasma protease	RP-HPLC	CLP-induced septic mice plasma	In Vitro	None	None	WT-EX4 bound to GLP-1R, with a dissociation constant of Kd(app) ≈ 0.142 nM
6154	26905040	2016	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSC	EX4-20K	40	Free	PEG(20KDa) linked with Ex-4 through Mal (Maleimide)	Linear	L	None	Exendin-4 analogs	Antidiabetes	37 °C	200 μg/mL	69.7	Hours	250920	Mice plasma protease	RP-HPLC	CLP-induced septic mice plasma	In Vitro	None	None	WT-EX4 bound to GLP-1R, with a dissociation constant of Kd(app) ≈ 0.142 nM
6155	26905040	2016	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSC	EX4-50K	40	Free	(PEG(50KDa))3 linked with Ex-4 through Mal (Maleimide)	Linear	L	None	Exendin-4 analogs	Antisepsis	37 °C	200 μg/mL	234.2	Hours	843120	Mice plasma protease	RP-HPLC	CLP-induced septic mice plasma	In Vitro	None	None	A dissociation constant of Kd(app) ≈ 0.159 nM was obtained for the interaction between GLP-1R and EX4-50
6157	26877782	2016	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSC	Abextide	40	Free	tEB (Truncated Evans blue) dye linked via Maleimide	Linear	L	Cys addition at C terminal of Ex4	Exendin-4 analogs	Antidiabetes	At predetermined times (0, 1, 2, 4, 6, 8, 12, 24, 48, 72, 96 h), blood samples were collected from tail vein of each animal	25 nmol/kg	36.28 ± 7.01	Hours	130608	DB/DB mice plasma protease	Exendin-4 EIA	DB/DB mice plasma	In Vivo	None	None	IC50 = 0.18 ± 0.06 nM
6196	28989813	2016	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSLPET	54.6 kDa EG9	43	Free	AEBMP: N-(2-(2-(2-(2-aminoacetamido)acet-amido)acetamido) ethyl)-2-bromo-2-methylpropanamide, OEGMA(54.6KDa)	Linear	L	Fluorescently labeled with Alexa Fluor	Exendin-4 analogs	Antidiabetes	10 μL of blood samples were collected from the tail vein into 100 μL of a heparin solution (1kU/ml in PBS, Sigma Aldrich) at 40 s, 40 min, 2.5 h, 4.5 h, 8 h, 24 h, 48 h, 72 h, 96 h and 120 h after injection	75 nmol/kg	42.4 ± 2.9 (T1/2 Elimination Half Life)	Hours	152640	Mice plasma protease	Fluorescence assay	Mice plasma	In Vivo	None	None	EC50(nM) = 1.91 ± 0.35
6197	28989813	2016	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSLPET	55.6 kDa EG3	43	Free	AEBMP: N-(2-(2-(2-(2-aminoacetamido)acet-amido)acetamido) ethyl)-2-bromo-2-methylpropanamide, OEGMA(55.6KDa)	Linear	L	Fluorescently labeled with Alexa Fluor	Exendin-4 analogs	Antidiabetes	10 μL of blood samples were collected from the tail vein into 100 μL of a heparin solution (1kU/ml in PBS, Sigma Aldrich) at 40 s, 40 min, 2.5 h, 4.5 h, 8 h, 24 h, 48 h, 72 h, 96 h and 120 h after injection	75 nmol/kg	61.2 ± 5.0 (T1/2 Elimination Half Life)	Hours	220320	Mice plasma protease	Fluorescence assay	Mice plasma	In Vivo	None	None	EC50(nM) = 4.17 ± 0.13
6198	28989813	2016	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSLPET	71.6 kDa EG3	43	Free	AEBMP: N-(2-(2-(2-(2-aminoacetamido)acet-amido)acetamido) ethyl)-2-bromo-2-methylpropanamide, OEGMA(71.6KDa)	Linear	L	Fluorescently labeled with Alexa Fluor	Exendin-4 analogs	Antidiabetes	10 μL of blood samples were collected from the tail vein into 100 μL of a heparin solution (1kU/ml in PBS, Sigma Aldrich) at 40 s, 40 min, 2.5 h, 4.5 h, 8 h, 24 h, 48 h, 72 h, 96 h and 120 h after injection	75 nmol/kg	61.5 ± 3.2 (T1/2 Elimination Half Life)	Hours	221400	Mice plasma protease	Fluorescence assay	Mice plasma	In Vivo	None	None	EC50(nM) = 5.11 ± 0.23
6229	26507721	2016	HGEGTFTSDVSSYLEEQAAKEFIAWLVKGGGGGGGSGGGGSGGGGSAESKYGPPCPPCPAPEAAGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTLPPSQEEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSRLTVDKSRWQEGNVFSCSVMHEALHNHYTQKSLSLSLG	Dulaglutide	275	Free	IgG4 Fc fused at C terminal using GS linker	Linear	L	None	GLP-1 analogs	Antidiabetes	4 to 6 weeks	0.75 mg	5.5 (GM)	Days	475200	Human plasma protease	RIA	Human plasma after multiple doses of dulaglutide once weekly, ranging from 4 to 6 weeks	In Vivo	DB id: DB09045	None	N.A.
6230	26507721	2016	HGEGTFTSDVSSYLEEQAAKEFIAWLVKGGGGGGGSGGGGSGGGGSAESKYGPPCPPCPAPEAAGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTLPPSQEEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSRLTVDKSRWQEGNVFSCSVMHEALHNHYTQKSLSLSLG	Dulaglutide	275	Free	IgG4 Fc fused at C terminal using GS linker	Linear	L	None	GLP-1 analogs	Antidiabetes	4 to 6 weeks	1.5 mg	4.7 (GM)	Days	406080	Human plasma protease	RIA	Human plasma after multiple doses of dulaglutide once weekly, ranging from 4 to 6 weeks	In Vivo	DB id: DB09045	None	N.A.
6231	26381279	2016	ptlhthnrrrrr	3H-RD2	12	3H labelled	Amidation	Linear	D	All D-amino acid substituitions	D3 derivative	Therapeutically active against toxic Β-Amyloid oligomers	Time points: 3 min, 5 min, 10 min, 15 min, 30 min, 1 h, 4 h, 1 d, 2 d, 7 d, 28 d	3.3 mg/kg	59 (Terminal Half Life)	Hours	212400	Mouse plasma protease	TLC	Mouse plasma	In Vivo	DB id: DB09045	None	Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3%
6232	26381279	2016	ptlhthnrrrrr	3H-RD2	12	3H labelled	Amidation	Linear	D	All D-amino acid substituitions	D3 derivative	Therapeutically active against toxic Β-Amyloid oligomers	Time points: 10 min, 20 min, 30 min, 1 h, 2 h, 4 h, 6 h, 1 d, 2 d, 7 d, 28 d	10 mg/kg	62 (Terminal Half Life)	Hours	223200	Mouse plasma protease	TLC	Mouse plasma	In Vivo	DB id: DB09045	None	Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3%
6233	26381279	2016	ptlhthnrrrrr	3H-RD2	12	3H labelled	Amidation	Linear	D	All D-amino acid substituitions	D3 derivative	Therapeutically active against toxic Β-Amyloid oligomers	Time points: 10 min, 20 min, 30 min, 1 h, 2 h, 4 h, 6 h, 1 d, 2 d, 7 d, 28 d	10 mg/kg	60 (Terminal Half Life)	Hours	216000	Mouse plasma protease	TLC	Mouse plasma	In Vivo	DB id: DB09045	None	Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3%
6234	26381279	2016	ptlhthnrrrrr	3H-RD2	12	3H labelled	Amidation	Linear	D	All D-amino acid substituitions	D3 derivative	Therapeutically active against toxic Β-Amyloid oligomers	Time points: 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 18 h, 1 d, 2 d, 3 d, 7 d, 28 d	10 mg/kg	58 (Terminal Half Life)	Hours	208800	Mouse plasma protease	TLC	Mouse plasma	In Vivo	DB id: DB09045	None	Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3%
6235	26381279	2016	ptlhthnrrrrr	3H-RD2	12	3H labelled	Amidation	Linear	D	All D-amino acid substituitions	D3 derivative	Therapeutically active against toxic Β-Amyloid oligomers	Time points: 3 min, 5 min, 10 min, 15 min, 30 min, 1 h, 4 h, 1 d, 2 d, 7 d, 28 d	3.3 mg/kg	60 (Terminal Half Life)	Hours	216000	Mouse brain homogenate protease	TLC	Mouse brain homogenate	In Vivo	DB id: DB09045	None	Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3%
6236	26381279	2016	ptlhthnrrrrr	3H-RD2	12	3H labelled	Amidation	Linear	D	All D-amino acid substituitions	D3 derivative	Therapeutically active against toxic Β-Amyloid oligomers	Time points: 10 min, 20 min, 30 min, 1 h, 2 h, 4 h, 6 h, 1 d, 2 d, 7 d, 28 d	10 mg/kg	61 (Terminal Half Life)	Hours	219600	Mouse brain homogenate protease	TLC	Mouse brain homogenate	In Vivo	DB id: DB09045	None	Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3%
6237	26381279	2016	ptlhthnrrrrr	3H-RD2	12	3H labelled	Amidation	Linear	D	All D-amino acid substituitions	D3 derivative	Therapeutically active against toxic Β-Amyloid oligomers	Time points: 10 min, 20 min, 30 min, 1 h, 2 h, 4 h, 6 h, 1 d, 2 d, 7 d, 28 d	10 mg/kg	94 (Terminal Half Life)	Hours	338400	Mouse brain homogenate protease	TLC	Mouse brain homogenate	In Vivo	DB id: DB09045	None	Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3%
6238	26381279	2016	ptlhthnrrrrr	3H-RD2	12	3H labelled	Amidation	Linear	D	All D-amino acid substituitions	D3 derivative	Therapeutically active against toxic Β-Amyloid oligomers	Time points: 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 18 h, 1 d, 2 d, 3 d, 7 d, 28 d	10 mg/kg	73 (Terminal Half Life)	Hours	262800	Mouse brain homogenate protease	TLC	Mouse brain homogenate	In Vivo	DB id: DB09045	None	Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3%