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Th1137 details
Primary information
ID1624
ThPP IDTh1137
Therapeutic Peptide/Protein NameTeduglutide
SequenceHGDGSFSDEMNTILDNLAARDFINWLIQTKITD view full sequnce in fasta
Functional ClassificationIa
Molecular Weight3752
Chemical FormulaC164H252N44O55S
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half LifeTerminal half-life - 2 hrs.
DescriptionRecombinant (E.coli derived) glucagon-like peptide-2 (GLP-2) analogue, made up of 33 amino acids. It differs from GLP-2 by one amino acid (A to G), which makes it more resistant to dipeptidyl peptidase-4 proteolysis, giving it a longer half-life as compared to endogenous GLP-2. FDA approved on December 21, 2012.
Indication/DiseaseTreatment of short bowel syndrome (SBS), malabsorption associated with the removal of the intestine, in adults patients who are dependent on parenteral support.
PharmacodynamicsAn enhancement of gastrointestinal fluid absorption (750-1000 mL/day) was observed following daily administrations of teduglutide. An increase in villus height and crypt depth of the intestinal mucosa was also noted. A decrease in fecal weight has also been observed. Teduglutide does not prolong the QTc interval.
Mechanism of ActionTeduglutide is an analog of naturally occurring human glucagon-like peptide-2 (GLP-2), a peptide secreted by L-cells of the distal intestine in response to meals. GLP-2 increases intestinal and portal blood flow and inhibit gastric acid secretion. Teduglutide binds to the glucagon-like peptide-2 receptors located in enteroendocrine cells, subepithelial myofibroblasts and enteric neurons of the submucosal and myenteric plexus. This causes the release of insulin-like growth factor (IGF)-1, nitric oxide and keratinocyte growth factor (KGF). These growth factors may contribute to the increase in crypt cell growth and surface area of the gastric mucosa. Ultimately, absorption through the intestine is enhanced.
ToxicityThe most common adverse reactions (≥ 10%) across all studies with GATTEX are abdominal pain, injection site reactions, nausea, headaches, abdominal distension, upper respiratory tract infection. In addition, vomiting and fluid overload were reported in the SBS studies (1 and 3) at rates ≥ 10%.
MetabolismAlthough a formal investigation has not been conducted, it is expected because teduglutide is a peptide-based drug, it will be degraded into smaller peptides and amino acids via catabolic pathways. The cytochrome P450 enzyme system is not involved in the metabolism of this drug.
AbsorptionThe pharmacokinetic profile of teduglutide (when administered subcutaneously) is described by a one-compartment model with first order absorption in the abdomen, arm, and thigh. With escalating doses, teduglutide demonstrates linear pharmacokinetics. Absolute bioavailability, SubQ = 88%; Tmax, SubQ = 3-5 hours; Cmax, 0.05 mg/kg SubQ, SBS patients = 36 ng/mL; AUC, 0.05 mg/kg SubQ, SBS patients = 0.15 µg hr/mL; Teduglutide does not accumulate following multiple subcutaneous administrations.
Volume of DistributionVd, healthy subjects = 103 mL/kg
ClearancePlasma clearance, healthy subjects = 123 mL/hr/kg;This value indicates that teduglutide is primarily cleared by the kidney.
CategoriesN.A.
Patents NumberUS5789379
Date of Issue22/12/16
Date of Expiry15/04/19
Drug InteractionN.A.
TargetGlucagon-like peptide 2 receptor
Information of corresponding available drug in the market
Brand NameGattex
CompanyNPS Pharmaceuticals, Inc
Brand DiscriptionThe active ingredient in GATTEX (teduglutide [rDNA origin]) for injection is teduglutide (rDNA origin), which is a 33 amino acid glucagon-like peptide-2 (GLP2) analog manufactured using a strain of Escherichia coli modified by recombinant DNA technology
Prescribed forShort Bowel Syndrome (SBS)
Chemical NameN.A.
FormulationEach single-use vial of GATTEX contains 5 mg of teduglutide as a white lyophilized powder for solution for subcutaneous injection. In addition to the active pharmaceutical ingredient (teduglutide), each vial of GATTEX contains 3.88 mg L-histidine, 15 mg mannitol, 0.644 mg monobasic sodium phosphate monohydrate, 3.434 mg dibasic sodium phosphate heptahydrate as excipients. No preservatives are present.
Physcial AppearanceTeduglutide drug substance is a clear, colorless to light-straw–colored liquid.
Route of AdministrationSubcutaneous
Recommended Dosage 0.05 mg/kg body weight administered by subcutaneous injection once daily
ContraindicationN.A.
Side Effectsabdominal pain , injection site reactions, nausea, headaches , abdominal distension, upper respiratory tract infection.
Useful Linkhttp://www.rxlist.com/gattex-drug.htm https://www.gattex.com/ http://www.drugs.com/gattex.html
PubMed ID25567782, 25525380, 25066226, 24871569, 23729002, 23591284, 22570676
3-D StructureTh1137 (View) or (Download)
Primary information
ID1625
ThPP IDTh1137
Therapeutic Peptide/Protein NameTeduglutide
SequenceHGDGSFSDEMNTILDNLAARDFINWLIQTKITD view full sequnce in fasta
Functional ClassificationIa
Molecular Weight3752
Chemical FormulaC164H252N44O55S
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half LifeTerminal half-life - 2 hrs.
DescriptionRecombinant (E.coli derived) glucagon-like peptide-2 (GLP-2) analogue, made up of 33 amino acids. It differs from GLP-2 by one amino acid (A to G), which makes it more resistant to dipeptidyl peptidase-4 proteolysis, giving it a longer half-life as compared to endogenous GLP-2. FDA approved on December 21, 2012.
Indication/DiseaseTreatment of short bowel syndrome (SBS), malabsorption associated with the removal of the intestine, in adults patients who are dependent on parenteral support.
PharmacodynamicsAn enhancement of gastrointestinal fluid absorption (750-1000 mL/day) was observed following daily administrations of teduglutide. An increase in villus height and crypt depth of the intestinal mucosa was also noted. A decrease in fecal weight has also been observed. Teduglutide does not prolong the QTc interval.
Mechanism of ActionTeduglutide is an analog of naturally occurring human glucagon-like peptide-2 (GLP-2), a peptide secreted by L-cells of the distal intestine in response to meals. GLP-2 increases intestinal and portal blood flow and inhibit gastric acid secretion. Teduglutide binds to the glucagon-like peptide-2 receptors located in enteroendocrine cells, subepithelial myofibroblasts and enteric neurons of the submucosal and myenteric plexus. This causes the release of insulin-like growth factor (IGF)-1, nitric oxide and keratinocyte growth factor (KGF). These growth factors may contribute to the increase in crypt cell growth and surface area of the gastric mucosa. Ultimately, absorption through the intestine is enhanced.
ToxicityThe most common adverse reactions (≥ 10%) across all studies with GATTEX are abdominal pain, injection site reactions, nausea, headaches, abdominal distension, upper respiratory tract infection. In addition, vomiting and fluid overload were reported in the SBS studies (1 and 3) at rates ≥ 10%.
MetabolismAlthough a formal investigation has not been conducted, it is expected because teduglutide is a peptide-based drug, it will be degraded into smaller peptides and amino acids via catabolic pathways. The cytochrome P450 enzyme system is not involved in the metabolism of this drug.
AbsorptionThe pharmacokinetic profile of teduglutide (when administered subcutaneously) is described by a one-compartment model with first order absorption in the abdomen, arm, and thigh. With escalating doses, teduglutide demonstrates linear pharmacokinetics. Absolute bioavailability, SubQ = 88%; Tmax, SubQ = 3-5 hours; Cmax, 0.05 mg/kg SubQ, SBS patients = 36 ng/mL; AUC, 0.05 mg/kg SubQ, SBS patients = 0.15 µg hr/mL; Teduglutide does not accumulate following multiple subcutaneous administrations.
Volume of DistributionVd, healthy subjects = 103 mL/kg
ClearancePlasma clearance, healthy subjects = 123 mL/hr/kg;This value indicates that teduglutide is primarily cleared by the kidney.
CategoriesN.A.
Patents NumberUS7056886
Date of Issue22/12/16
Date of Expiry19/09/26
Drug InteractionN.A.
TargetN.A.
Information of corresponding available drug in the market
Brand NameN.A.
CompanyN.A.
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearanceN.A.
Route of AdministrationN.A.
Recommended DosageN.A.
ContraindicationN.A.
Side EffectsN.A.
Useful LinkN.A.
PubMed ID25567782, 25525380, 25066226, 24871569, 23729002, 23591284, 22570676
3-D StructureTh1137 (View) or (Download)
Primary information
ID1626
ThPP IDTh1137
Therapeutic Peptide/Protein NameTeduglutide
SequenceHGDGSFSDEMNTILDNLAARDFINWLIQTKITD view full sequnce in fasta
Functional ClassificationIa
Molecular Weight3752
Chemical FormulaC164H252N44O55S
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half LifeTerminal half-life - 2 hrs.
DescriptionRecombinant (E.coli derived) glucagon-like peptide-2 (GLP-2) analogue, made up of 33 amino acids. It differs from GLP-2 by one amino acid (A to G), which makes it more resistant to dipeptidyl peptidase-4 proteolysis, giving it a longer half-life as compared to endogenous GLP-2. FDA approved on December 21, 2012.
Indication/DiseaseTreatment of short bowel syndrome (SBS), malabsorption associated with the removal of the intestine, in adults patients who are dependent on parenteral support.
PharmacodynamicsAn enhancement of gastrointestinal fluid absorption (750-1000 mL/day) was observed following daily administrations of teduglutide. An increase in villus height and crypt depth of the intestinal mucosa was also noted. A decrease in fecal weight has also been observed. Teduglutide does not prolong the QTc interval.
Mechanism of ActionTeduglutide is an analog of naturally occurring human glucagon-like peptide-2 (GLP-2), a peptide secreted by L-cells of the distal intestine in response to meals. GLP-2 increases intestinal and portal blood flow and inhibit gastric acid secretion. Teduglutide binds to the glucagon-like peptide-2 receptors located in enteroendocrine cells, subepithelial myofibroblasts and enteric neurons of the submucosal and myenteric plexus. This causes the release of insulin-like growth factor (IGF)-1, nitric oxide and keratinocyte growth factor (KGF). These growth factors may contribute to the increase in crypt cell growth and surface area of the gastric mucosa. Ultimately, absorption through the intestine is enhanced.
ToxicityThe most common adverse reactions (≥ 10%) across all studies with GATTEX are abdominal pain, injection site reactions, nausea, headaches, abdominal distension, upper respiratory tract infection. In addition, vomiting and fluid overload were reported in the SBS studies (1 and 3) at rates ≥ 10%.
MetabolismAlthough a formal investigation has not been conducted, it is expected because teduglutide is a peptide-based drug, it will be degraded into smaller peptides and amino acids via catabolic pathways. The cytochrome P450 enzyme system is not involved in the metabolism of this drug.
AbsorptionThe pharmacokinetic profile of teduglutide (when administered subcutaneously) is described by a one-compartment model with first order absorption in the abdomen, arm, and thigh. With escalating doses, teduglutide demonstrates linear pharmacokinetics. Absolute bioavailability, SubQ = 88%; Tmax, SubQ = 3-5 hours; Cmax, 0.05 mg/kg SubQ, SBS patients = 36 ng/mL; AUC, 0.05 mg/kg SubQ, SBS patients = 0.15 µg hr/mL; Teduglutide does not accumulate following multiple subcutaneous administrations.
Volume of DistributionVd, healthy subjects = 103 mL/kg
ClearancePlasma clearance, healthy subjects = 123 mL/hr/kg;This value indicates that teduglutide is primarily cleared by the kidney.
CategoriesN.A.
Patents NumberUS7847061
Date of Issue22/12/16
Date of Expiry02/11/29
Drug InteractionN.A.
TargetN.A.
Information of corresponding available drug in the market
Brand NameN.A.
CompanyN.A.
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearanceN.A.
Route of AdministrationN.A.
Recommended DosageN.A.
ContraindicationN.A.
Side EffectsN.A.
Useful LinkN.A.
PubMed ID25567782, 25525380, 25066226, 24871569, 23729002, 23591284, 22570676
3-D StructureTh1137 (View) or (Download)