==== Reference: Usmani SS, Bedi G, Samuel JS, Singh S, Kalra S, Kumar P, et al. (2017) THPdb: Database of FDA-approved peptide and protein therapeutics. PLoS ONE 12(7) e0181748.====

Detailed description page of THPdb


Details of Th1012 which contains 4 entries.


Entry 1
(1) Primary information
ID1067
ThPP IDTh1012
Therapeutic Peptide/Protein NameReteplase
SequenceSYQGNSDCYFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQ view full sequnce in fasta
Functional ClassificationIb
Molecular Weight39589.6
Chemical FormulaC1736H2671N499O522S22
Isoelectric Point6.86
Hydrophobicity-0.435
Melting Point (℃)60
Half LifeN.A.
DescriptionHuman tissue plasminogen activator which is glycosylated and purified (355 residues) from CHO cells. Retavase is considered a third-generation thrombolytic agent, genetically engineered to retain and delete certain portions of human tPA. Retavase is a deletion mutein of human tPA formed by deleting various amino acids present in endogenous human tPA. Retavase contains 355 of the 527 amino acids of native human tPA (amino acids 1-3 and 176-527), and retains the activity-related kringle-2 and serine protease domains of human tPA. Three domains are deleted from retavase – kringle-1, finger, and epidermal growth factor (EGF).
Indication/DiseaseFor lysis of acute pulmonary emboli, intracoronary emboli and management of myocardial infarction.
PharmacodynamicsReteplase cleaves Arg/Val bonds in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus thereby exerting its thrombolytic action. This helps eliminate blood clots or arterial blockages that further cause myocardial infarction.
Mechanism of ActionReteplase binds to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain. The protease domain then cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action.
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of DistributionN.A.
ClearanceN.A.
CategoriesFibrinolytic Agents
Patents NumberCA2107476
Date of Issue18/12/07
Date of Expiry15/04/12
Drug InteractionAdditive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided with Ginkgo biloba
TargetPlasminogen,Fibrinogen alpha chain,Urokinase plasminogen activator surface receptor,Plasminogen activator inhibitor 1
Information of corresponding available drug in the market
Brand NameRetavase
CompanyCentocor
Brand DiscriptionRetavase(39,571 daltons) is a non-glycosylated deletion mutein of tissue plasminogen activator containing the kringle 2 and the protease domains of human tPA. Retavase contains 355 of the 527 amino acids of native tPA (amino acids 1-3 and 176-527). Retava
Prescribed forImproves heart function and reduces long-term effects of a heart attack.
Chemical NameN.A.
FormulationEach single-use vial contains:Reteplase 18.1 mg, Tranexamic Acid 8.32 mg, Dipotassium Hydrogen Phosphate 136.24 mg, Phosphoric Acid 51.27 mg, Sucrose 364.0 mg, Polysorbate 805.20 mg
Physcial AppearanceSterile, white, lyophilized powder
Route of AdministrationIntravenous Injection
Recommended DosageRetavase is administered as a 10 + 10 unit double-bolus injection. Two 10 unit bolus injections are required for a complete treatment. Each bolus is administered as an Intravenous infusion over 2 minutes. The second bolus is given 30 minutes after initial one.
ContraindicationAllergic, or you have an aneurysm, heart or blood vessel defects, bleeding disorders
Side EffectsRash; hives; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue.
Useful Linkhttp://www.drugs.com/cdi/retavase.html
PubMed ID15650539
3-D StructureTh1012 (View) or (Download)


Entry 2
(2) Primary information
ID1068
ThPP IDTh1012
Therapeutic Peptide/Protein NameReteplase
SequenceSYQGNSDCYFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQ view full sequnce in fasta
Functional ClassificationIb
Molecular Weight39589.6
Chemical FormulaC1736H2671N499O522S22
Isoelectric Point6.86
Hydrophobicity-0.435
Melting Point (℃)60
Half LifeN.A.
DescriptionHuman tissue plasminogen activator which is glycosylated and purified (355 residues) from CHO cells. Retavase is considered a third-generation thrombolytic agent, genetically engineered to retain and delete certain portions of human tPA. Retavase is a deletion mutein of human tPA formed by deleting various amino acids present in endogenous human tPA. Retavase contains 355 of the 527 amino acids of native human tPA (amino acids 1-3 and 176-527), and retains the activity-related kringle-2 and serine protease domains of human tPA. Three domains are deleted from retavase – kringle-1, finger, and epidermal growth factor (EGF).
Indication/DiseaseFor lysis of acute pulmonary emboli, intracoronary emboli and management of myocardial infarction.
PharmacodynamicsReteplase cleaves Arg/Val bonds in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus thereby exerting its thrombolytic action. This helps eliminate blood clots or arterial blockages that further cause myocardial infarction.
Mechanism of ActionReteplase binds to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain. The protease domain then cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exe
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of DistributionN.A.
ClearanceN.A.
CategoriesThrombolytic Agents
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionIncreased bleeding risk. Monitor for signs of bleeding when given in combination with Ticlopidine
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.
ContraindicationSevere uncontrolled high blood pressure
Side EffectsBlack, tarry stools; bleeding at the injection site
Useful Linkhttp://www.rxlist.com/retavase-drug.htm
PubMed ID15650539
3-D StructureTh1012 (View) or (Download)


Entry 3
(3) Primary information
ID1069
ThPP IDTh1012
Therapeutic Peptide/Protein NameReteplase
SequenceSYQGNSDCYFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQ view full sequnce in fasta
Functional ClassificationIb
Molecular Weight39589.6
Chemical FormulaC1736H2671N499O522S22
Isoelectric Point6.86
Hydrophobicity-0.435
Melting Point (℃)60
Half LifeN.A.
DescriptionHuman tissue plasminogen activator which is glycosylated and purified (355 residues) from CHO cells. Retavase is considered a third-generation thrombolytic agent, genetically engineered to retain and delete certain portions of human tPA. Retavase is a deletion mutein of human tPA formed by deleting various amino acids present in endogenous human tPA. Retavase contains 355 of the 527 amino acids of native human tPA (amino acids 1-3 and 176-527), and retains the activity-related kringle-2 and serine protease domains of human tPA. Three domains are deleted from retavase – kringle-1, finger, and epidermal growth factor (EGF).
Indication/DiseaseFor lysis of acute pulmonary emboli, intracoronary emboli and management of myocardial infarction.
PharmacodynamicsReteplase cleaves Arg/Val bonds in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus thereby exerting its thrombolytic action. This helps eliminate blood clots or arterial blockages that further cause myocardial infarction.
Mechanism of ActionReteplase binds to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain. The protease domain then cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exe
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of DistributionN.A.
ClearanceN.A.
CategoriesN.A.
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
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.
ContraindicationIf you have had brain or spinal surgery; or you have suffered recent trauma
Side EffectsVomiting blood or material that looks like coffee grounds
Useful Linkhttp://www.drugs.com/drug-interactions/reteplase,retavase-index.html?filter=1
PubMed ID15650539
3-D StructureTh1012 (View) or (Download)


Entry 4
(4) Primary information
ID1070
ThPP IDTh1012
Therapeutic Peptide/Protein NameReteplase
SequenceSYQGNSDCYFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQ view full sequnce in fasta
Functional ClassificationIb
Molecular Weight39589.6
Chemical FormulaC1736H2671N499O522S22
Isoelectric Point6.86
Hydrophobicity-0.435
Melting Point (℃)60
Half LifeN.A.
DescriptionHuman tissue plasminogen activator which is glycosylated and purified (355 residues) from CHO cells. Retavase is considered a third-generation thrombolytic agent, genetically engineered to retain and delete certain portions of human tPA. Retavase is a deletion mutein of human tPA formed by deleting various amino acids present in endogenous human tPA. Retavase contains 355 of the 527 amino acids of native human tPA (amino acids 1-3 and 176-527), and retains the activity-related kringle-2 and serine protease domains of human tPA. Three domains are deleted from retavase – kringle-1, finger, and epidermal growth factor (EGF).
Indication/DiseaseFor lysis of acute pulmonary emboli, intracoronary emboli and management of myocardial infarction.
PharmacodynamicsReteplase cleaves Arg/Val bonds in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus thereby exerting its thrombolytic action. This helps eliminate blood clots or arterial blockages that further cause myocardial infarction.
Mechanism of ActionReteplase binds to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain. The protease domain then cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exe
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of DistributionN.A.
ClearanceN.A.
CategoriesN.A.
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
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.
ContraindicationA history of stroke, or internal bleeding
Side EffectsChest pain; severe bleeding; sudden, severe headache; trouble breathing
Useful LinkN.A.
PubMed ID15650539
3-D StructureTh1012 (View) or (Download)