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Th1084 details

Primary information
ID 1454
ThPP ID Th1084
Therapeutic Peptide/Protein Name Becaplermin
Sequence SLGSLTIAEPAMIAECKTRTEVFEISRRLIDRTNANFLVWPPCVEVQRCS view full sequnce in fasta
Functional Classification Ib
Molecular Weight 12294.4
Chemical Formula C532H892N162O153S9
Isoelectric Point 9.38
Hydrophobicity -0.16
Melting Point (℃) N.A.
Half Life N.A.
Description Recombinant platelet derived growth factor (PDGF), the gene for B chain, produced in yeast by cloning and expression of, Saccharomyces cerevisiae. Molecular weight ~25 KD is the homodimer composed of two identical polypeptide chains linked by disulfide bonds.
Indication/Disease For topical treatment of skin ulcers (from diabetes)
Pharmacodynamics Used for the topical treatment of skin ulcers, Regranex has a biological activity similar to that of endogenous platelet-derived growth factor, which includes promoting the chemotactic recruitment and proliferation of cells involved in wound repair and enhancing the formation of granulation tissue.
Mechanism of Action Binds to the beta platelet-derived growth factor (PDGF) receptor, a tyrosine kinase receptor. PDGF is known to exist as a dimer, and activates its signaling pathway by a ligand induced receptor dimerization and autophosphorylation. PDGF receptors also contain many auto-phosphorylation sites, which serve to mediate binding of SH2 sites and subsequently signal corresponding pathways. There are five different isoforms of PDGF that activate through two different receptors (alpha and beta).
Toxicity N.A.
Metabolism N.A.
Absorption N.A.
Volume of Distribution N.A.
Clearance N.A.
Categories Angiogenesis Inducing Agents
Patents Number CA1340846
Date of Issue 08/12/03
Date of Expiry 16/12/19
Drug Interaction N.A.
Target T-cell surface glycoprotein CD1a,Major histocompatibility complex class I-related gene protein,Integrin alpha-L,T-lymphocyte activation antigen CD86,Low affinity immunoglobulin gamma Fc region receptor II-b,T-cell surface glycoprotein CD4,Integrin beta-1,Integrin alpha-V,Integrin beta-3
Information of corresponding available drug in the market
Brand Name REGRANEX
Company OMJ Pharmaceuticals, Inc. San German, Puerto Rico
Brand Discription REGRANEX Gel contains becaplermin, a recombinant human platelet-derived growth factor for topical administration. Becaplermin is produced by recombinant DNA technology by insertion of the gene for the B chain of platelet-derived growth factor (PDGF) into the yeast, Saccharomyces cerevisiae. Becaplermin has a molecular weight of approximately 25 KD and is a homodimer composed of two identical polypeptide chains that are bound together by disulfide bonds. REGRANEX Gel is a non-sterile, low bioburden, preserved, sodium carboxymethylcellulose-based (CMC) topical gel, containing the active ingredient becaplermin and the following inactive ingredients: carboxymethylcellulose sodium, glacial acetic acid, l-lysine hydrochloride, m-cresol, methylparaben, propylparaben, sodium acetate trihydrate, sodium chloride, and water for injection. Each gram of REGRANEX Gel contains 100 mcg of becaplermin.
Prescribed for for the treatment of lower extremity diabetic neuropathic ulcers that extend into the subcutaneous tissue or beyond and have an adequate blood supply, when used as an adjunct to, and not a substitute for, good ulcer care practices including initial sharp debridement, pressure relief and infection control.
Chemical Name N.A.
Formulation 0.01 % clear to straw-colored gel
Physcial Appearance Gel: 0.01 %; clear, colorless to straw-colored gel
Route of Administration For topical use; not for oral, ophthalmic or intra
Recommended Dosage Gel to be applied will vary depending upon the size of the ulcer area.
Contraindication A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.
Side Effects hives; difficulty breathing; swelling of your face, lips, tongue, or throat.
Useful Link http://www.rxlist.com/regranex-side-effects-drug-center.htm
PubMed ID 23962308, 21173589, 20941855, 20486728, 20479444, 19837327, 18251718
3-D Structure Th1084 (View) or (Download)

OSDDlinux

Raghava's Group

IMTECH

CSIR

CRDD
CPPSITE 2.0

Primary information
ID	1454
ThPP ID	Th1084
Therapeutic Peptide/Protein Name	Becaplermin
Sequence	SLGSLTIAEPAMIAECKTRTEVFEISRRLIDRTNANFLVWPPCVEVQRCS view full sequnce in fasta
Functional Classification	Ib
Molecular Weight	12294.4
Chemical Formula	C532H892N162O153S9
Isoelectric Point	9.38
Hydrophobicity	-0.16
Melting Point (℃)	N.A.
Half Life	N.A.
Description	Recombinant platelet derived growth factor (PDGF), the gene for B chain, produced in yeast by cloning and expression of, Saccharomyces cerevisiae. Molecular weight ~25 KD is the homodimer composed of two identical polypeptide chains linked by disulfide bonds.
Indication/Disease	For topical treatment of skin ulcers (from diabetes)
Pharmacodynamics	Used for the topical treatment of skin ulcers, Regranex has a biological activity similar to that of endogenous platelet-derived growth factor, which includes promoting the chemotactic recruitment and proliferation of cells involved in wound repair and enhancing the formation of granulation tissue.
Mechanism of Action	Binds to the beta platelet-derived growth factor (PDGF) receptor, a tyrosine kinase receptor. PDGF is known to exist as a dimer, and activates its signaling pathway by a ligand induced receptor dimerization and autophosphorylation. PDGF receptors also contain many auto-phosphorylation sites, which serve to mediate binding of SH2 sites and subsequently signal corresponding pathways. There are five different isoforms of PDGF that activate through two different receptors (alpha and beta).
Toxicity	N.A.
Metabolism	N.A.
Absorption	N.A.
Volume of Distribution	N.A.
Clearance	N.A.
Categories	Angiogenesis Inducing Agents
Patents Number	CA1340846
Date of Issue	08/12/03
Date of Expiry	16/12/19
Drug Interaction	N.A.
Target	T-cell surface glycoprotein CD1a,Major histocompatibility complex class I-related gene protein,Integrin alpha-L,T-lymphocyte activation antigen CD86,Low affinity immunoglobulin gamma Fc region receptor II-b,T-cell surface glycoprotein CD4,Integrin beta-1,Integrin alpha-V,Integrin beta-3
Information of corresponding available drug in the market
Brand Name	REGRANEX
Company	OMJ Pharmaceuticals, Inc. San German, Puerto Rico
Brand Discription	REGRANEX Gel contains becaplermin, a recombinant human platelet-derived growth factor for topical administration. Becaplermin is produced by recombinant DNA technology by insertion of the gene for the B chain of platelet-derived growth factor (PDGF) into the yeast, Saccharomyces cerevisiae. Becaplermin has a molecular weight of approximately 25 KD and is a homodimer composed of two identical polypeptide chains that are bound together by disulfide bonds. REGRANEX Gel is a non-sterile, low bioburden, preserved, sodium carboxymethylcellulose-based (CMC) topical gel, containing the active ingredient becaplermin and the following inactive ingredients: carboxymethylcellulose sodium, glacial acetic acid, l-lysine hydrochloride, m-cresol, methylparaben, propylparaben, sodium acetate trihydrate, sodium chloride, and water for injection. Each gram of REGRANEX Gel contains 100 mcg of becaplermin.
Prescribed for	for the treatment of lower extremity diabetic neuropathic ulcers that extend into the subcutaneous tissue or beyond and have an adequate blood supply, when used as an adjunct to, and not a substitute for, good ulcer care practices including initial sharp debridement, pressure relief and infection control.
Chemical Name	N.A.
Formulation	0.01 % clear to straw-colored gel
Physcial Appearance	Gel: 0.01 %; clear, colorless to straw-colored gel
Route of Administration	For topical use; not for oral, ophthalmic or intra
Recommended Dosage	Gel to be applied will vary depending upon the size of the ulcer area.
Contraindication	A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.
Side Effects	hives; difficulty breathing; swelling of your face, lips, tongue, or throat.
Useful Link	http://www.rxlist.com/regranex-side-effects-drug-center.htm
PubMed ID	23962308, 21173589, 20941855, 20486728, 20479444, 19837327, 18251718
3-D Structure	Th1084 (View) or (Download)