==== 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 Th1028 which contains 5 entries.


Entry 1
(1) Primary information
ID1210
ThPP IDTh1028
Therapeutic Peptide/Protein NameTenecteplase
SequenceSYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKS view full sequnce in fasta
Functional ClassificationIb
Molecular Weight58951.2
Chemical FormulaC2561H3919N747O781S40
Isoelectric Point7.61
Hydrophobicity-0.528
Melting Point (℃)60
Half Life1.9 hours (mammalian reticulocytes, in vitro)
DescriptionTenecteplase(527 amino acid) is a glycoprotein developed by introducing the following modifications to the complementary DNA for natural human tPA: a substitution of threonine 103 with asparagine, and a substitution of asparagine 117 with glutamine, both within the kringle 1 domain, and a tetra-alanine substitution at amino acids 296-299 in the protease domain.
Indication/DiseaseTo treat myocardial infarction and lysis of intracoronary emboli.
PharmacodynamicsTenecteplase is a fibrin-specific tissue-plasminogen activator. It binds to fibrin rich clots and 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. This helps eliminate blood clots or arterial blockages that cause myocardial infarction.
Mechanism of ActionTenecteplase 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.
Clearance99 - 119 mL/min [acute myocardial infarction patients]
CategoriesFibrinolytic Agents
Patents NumberCA2129660
Date of Issue28/06/05
Date of Expiry28/05/13
Drug InteractionAprotonin may antagonize the effect of Tenecteplase. Monitor for decreased effects of Tenecteplase.
TargetPlasminogen,Fibrinogen alpha chain,Urokinase plasminogen activator surface receptor,Plasminogen activator inhibitor 1,Plasminogen activator inhibitor 2,Tetranectin,Keratin, type II cytoskeletal 8,Annexin A2,Calreticulin,Calnexin,Prolow-density lipoprotein
Information of corresponding available drug in the market
Brand NameTNKase
CompanyGenentech Inc
Brand DiscriptionTNKase is a tissue plasminogen activator produced by recombinant DNA technology using an established mammalian cell line of Chinese Hamster Ovary cells. Tenecteplase(527 amino acid) is a glycoprotein developed by introducing the following modifications to
Prescribed forTo prevent death from a heart attack (acute myocardial infarction).
Chemical NameN.A.
FormulationEach vial of TNKase nominally contains 52.5 mg Tenecteplase, 0.55 g L-arginine, 0.17 g phosphoric acid, and 4.3 mg polysorbate 20, which includes a 5% overfill. Each vial will deliver 50 mg of Tenecteplase.
Physcial AppearanceSterile, white to off-white, lyophilized powder
Route of AdministrationIntravenous Injection
Recommended DosageThe recommended total dose should not exceed 50 mg and is based upon patient weight. For less than 60 kg of body weight recommended dose is 30 mg of TNKase. Similarly 35 mg for 60-70 kg, 40 mg for 70-80 kg, 45 mg for 80-90 kg and 50 mg for more than 90 kg.
ContraindicationActive internal bleeding, History of cerebrovascular accident
Side EffectsNausea, vomiting; or fever.
Useful Linkhttp://www.drugs.com/mtm/tnkase.html
PubMed ID16488800, 16380055, 16084152, 15744554, 15650539
3-D StructureTh1028 (View) or (Download)


Entry 2
(2) Primary information
ID1211
ThPP IDTh1028
Therapeutic Peptide/Protein NameTenecteplase
SequenceSYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKS view full sequnce in fasta
Functional ClassificationIb
Molecular Weight58951.2
Chemical FormulaC2561H3919N747O781S40
Isoelectric Point7.61
Hydrophobicity-0.528
Melting Point (℃)60
Half Life1.9 hours (mammalian reticulocytes, in vitro)
DescriptionTenecteplase(527 amino acid) is a glycoprotein developed by introducing the following modifications to the complementary DNA for natural human tPA: a substitution of threonine 103 with asparagine, and a substitution of asparagine 117 with glutamine, both within the kringle 1 domain, and a tetra-alanine substitution at amino acids 296-299 in the protease domain.
Indication/DiseaseTo treat myocardial infarction and lysis of intracoronary emboli.
PharmacodynamicsTenecteplase is a fibrin-specific tissue-plasminogen activator. It binds to fibrin rich clots and 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. This helps eliminate blood clots or arterial blockages that cause myocardial infarction.
Mechanism of ActionTenecteplase 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.
Clearance99 - 119 mL/min [acute myocardial infarction patients]
CategoriesThrombolytic Agents
Patents NumberCA1341432
Date of Issue17/06/03
Date of Expiry17/06/20
Drug InteractionDrotrecogin alfa increases risk of bleeding.
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.
ContraindicationIntracranial neoplasm, Known bleeding diathesis
Side EffectsChest pain, slow or uneven heartbeats; pain, swelling, hot or cold feeling, skin changes, or discoloration anywhere on your body; sudden leg or foot pain, foot ulcer, purple toes or fingers; swelling or severe pain or signs of infection in your fingers.
Useful Linkhttp://www.rxlist.com/tnkase-drug.htm
PubMed ID16488800, 16380055, 16084152, 15744554, 15650539
3-D StructureTh1028 (View) or (Download)


Entry 3
(3) Primary information
ID1212
ThPP IDTh1028
Therapeutic Peptide/Protein NameTenecteplase
SequenceSYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKS view full sequnce in fasta
Functional ClassificationIb
Molecular Weight58951.2
Chemical FormulaC2561H3919N747O781S40
Isoelectric Point7.61
Hydrophobicity-0.528
Melting Point (℃)60
Half Life1.9 hours (mammalian reticulocytes, in vitro)
DescriptionTenecteplase(527 amino acid) is a glycoprotein developed by introducing the following modifications to the complementary DNA for natural human tPA: a substitution of threonine 103 with asparagine, and a substitution of asparagine 117 with glutamine, both within the kringle 1 domain, and a tetra-alanine substitution at amino acids 296-299 in the protease domain.
Indication/DiseaseTo treat myocardial infarction and lysis of intracoronary emboli.
PharmacodynamicsTenecteplase is a fibrin-specific tissue-plasminogen activator. It binds to fibrin rich clots and 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. This helps eliminate blood clots or arterial blockages that cause myocardial infarction.
Mechanism of ActionTenecteplase 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.
Clearance99 - 119 mL/min [acute myocardial infarction patients]
CategoriesN.A.
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionAdditive anticoagulant/antiplatelet effects may increase bleed risk, so Ginkgo biloba's (DB01381) concomitant therapy should be avoided.
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.
ContraindicationIntracranial or intraspinal surgery or trauma within 2 months
Side EffectsSudden numbness or weakness, problems with speech or balance, vision problems; little or no urinating; unexplained muscle pain.
Useful LinkN.A.
PubMed ID16488800, 16380055, 16084152, 15744554, 15650539
3-D StructureTh1028 (View) or (Download)


Entry 4
(4) Primary information
ID1213
ThPP IDTh1028
Therapeutic Peptide/Protein NameTenecteplase
SequenceSYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKS view full sequnce in fasta
Functional ClassificationIb
Molecular Weight58951.2
Chemical FormulaC2561H3919N747O781S40
Isoelectric Point7.61
Hydrophobicity-0.528
Melting Point (℃)60
Half Life1.9 hours (mammalian reticulocytes, in vitro)
DescriptionTenecteplase(527 amino acid) is a glycoprotein developed by introducing the following modifications to the complementary DNA for natural human tPA: a substitution of threonine 103 with asparagine, and a substitution of asparagine 117 with glutamine, both within the kringle 1 domain, and a tetra-alanine substitution at amino acids 296-299 in the protease domain.
Indication/DiseaseTo treat myocardial infarction and lysis of intracoronary emboli.
PharmacodynamicsTenecteplase is a fibrin-specific tissue-plasminogen activator. It binds to fibrin rich clots and 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. This helps eliminate blood clots or arterial blockages that cause myocardial infarction.
Mechanism of ActionTenecteplase 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.
Clearance99 - 119 mL/min [acute myocardial infarction patients]
CategoriesN.A.
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionGinseng increases risk of bleeding.
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.
ContraindicationArteriovenous malformation or aneurysm
Side EffectsMuscle weakness or loss of function, loss of bowel or bladder control; or severe pain in your upper stomach spreading to your back.
Useful LinkN.A.
PubMed ID16488800, 16380055, 16084152, 15744554, 15650539
3-D StructureTh1028 (View) or (Download)


Entry 5
(5) Primary information
ID1214
ThPP IDTh1028
Therapeutic Peptide/Protein NameTenecteplase
SequenceSYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKS view full sequnce in fasta
Functional ClassificationIb
Molecular Weight58951.2
Chemical FormulaC2561H3919N747O781S40
Isoelectric Point7.61
Hydrophobicity-0.528
Melting Point (℃)60
Half Life1.9 hours (mammalian reticulocytes, in vitro)
DescriptionTenecteplase(527 amino acid) is a glycoprotein developed by introducing the following modifications to the complementary DNA for natural human tPA: a substitution of threonine 103 with asparagine, and a substitution of asparagine 117 with glutamine, both within the kringle 1 domain, and a tetra-alanine substitution at amino acids 296-299 in the protease domain.
Indication/DiseaseTo treat myocardial infarction and lysis of intracoronary emboli.
PharmacodynamicsTenecteplase is a fibrin-specific tissue-plasminogen activator. It binds to fibrin rich clots and 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. This helps eliminate blood clots or arterial blockages that cause myocardial infarction.
Mechanism of ActionTenecteplase 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.
Clearance99 - 119 mL/min [acute myocardial infarction patients]
CategoriesN.A.
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionTiclopidine increases bleeding risk. Monitor for signs of bleeding.
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 hypertension
Side EffectsTenderness, or weakness especially if you also have fever, unusual tiredness, and dark colored urine.
Useful LinkN.A.
PubMed ID16488800, 16380055, 16084152, 15744554, 15650539
3-D StructureTh1028 (View) or (Download)