==== 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 Th1158 which contains 4 entries.


Entry 1
(1) Primary information
ID1667
ThPP IDTh1158
Therapeutic Peptide/Protein NameAprotinin
SequenceRPDFCLEPPYTGPCKARIIRYFYNAKAGLCQTFVYGGCRAKRNNFKSAED view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight6511.439
Chemical FormulaC284H432N84O79S7
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)>100
Half LifePlasma half life: 150 minutes, Elimination half life: 10hrs
DescriptionAprotinin, also known as bovine pancreatic trypsin inhibitor, BPTI (Trasylol, Bayer) is a protein, that is used as medication administered by injection to reduce bleeding during complex surgery, such as heart and liver surgery. Its main effect is the slowing down of fibrinolysis, the process that leads to the breakdown of blood clots. The aim in its use is to decrease the need for blood transfusions during surgery, as well as end-organ damage due to hypotension (low blood pressure) as a result of marked blood loss.
Indication/DiseaseFor prophylactic use to reduce perioperative blood loss and the need for blood transfusion in patients undergoing cardiopulmonary bypass in the course of coronary artery bypass graft surgery who are at an increased risk for blood loss and blood transfusion.
PharmacodynamicsAprotinin is a broad spectrum protease inhibitor which modulates the systemic inflammatory response (SIR) associated with cardiopulmonary bypass (CPB) surgery. SIR results in the interrelated activation of the hemostatic, fibrinolytic, cellular and humoral inflammatory systems. Aprotinin, through its inhibition of multiple mediators [e.g., kallikrein, plasmin] results in the attenuation of inflammatory responses, fibrinolysis, and thrombin generation. Aprotinin inhibits pro-inflammatory cytokine release and maintains glycoprotein homeostasis. In platelets, aprotinin reduces glycoprotein loss (e.g., GpIb, GpIIb/IIIa), while in granulocytes it prevents the expression of pro-inflammatory adhesive glycoproteins.
Mechanism of ActionAprotinin inhibits several serine proteases, specifically trypsin, chymotrypsin and plasmin at a concentration of about 125,000 IU/ml, and kallikrein at 300,000 IU/ml. Its action on kallikrein leads to the inhibition of the formation of factor XIIa. As a result, both the intrinsic pathway of coagulation and fibrinolysis are inhibited. Its action on plasmin independently slows fibrinolysis.
ToxicityN.A.
MetabolismAprotinin is slowly degraded by lysosomal enzymes.
Absorption100%(IV)
Volume of DistributionN.A.
ClearanceN.A.
CategoriesN.A.
Patents NumberUS5198534
Date of Issue30/03/93
Date of ExpiryN.A.
Drug InteractionCaptopril- aprotinin infused intravenously in a dose of 2 million KIU over two hours blocked the acute hypotensive effect of 100mg of captopril.
TargetTrypsin-1, Chymotrypsinogen B, Plasminogen, Kallikrein-!
Information of corresponding available drug in the market
Brand NameTrasylol
CompanyBayer Pharmaceuticals
Brand DiscriptionTrasylol (aprotinin injection), C284H432N84O79S7, is a natural proteinase inhibitor obtained from bovine lung. Aprotinin (molecular weight of 6512 daltons), consists of 58 amino acid residues that are arranged in a single polypeptide chain, cross-linked by three disulfide bridges.
Prescribed forTrasylol (aprotinin) is indicated for prophylactic use to reduce perioperative blood loss and the need for blood transfusion in patients undergoing cardiopulmonary bypass in the course of coronary artery bypass graft surgery who are at an increased risk for blood loss and blood transfusion.
Chemical NameN.A.
FormulationEach milliliter contains 10,000 KIU (Kallikrein Inhibitor Units) (1.4 mg/mL) and 9 mg sodium chloride in water for injection. Hydrochloric acid and/or sodium hydroxide is used to adjust the pH to 4.5-6.5.
Physcial AppearanceIt is supplied as a clear, colorless, sterile isotonic solution
Route of AdministrationIntravenous administration
Recommended Dosagedosage is given as two regimens: Regimen A and Regimen B intial dose is same 1ml (1.4mg or 10000 KIU) but loading dose and PumpPrime dose is 200ml in case of regimen A and 100ml in case of regimen B, and constant infusion rate is 50ml/hr in A and 25ml/hr in B.
ContraindicationAdministration of Trasylol (aprotinin) to patients with a known or suspected previous aprotinin exposure during the last 12 months is contraindicated. For patients with known or suspected history of exposure to aprotinin greater than 12 months previously.
Side EffectsVentricular fibrillation, heart arrest, bradycardia, congestive heart failure, hemorrhage, bundle branch block, myocardial ischemia, ventricular tachycardia, heart block, pericardial effusion, ventricular arrhythmia, shock, pulmonary hypertension. Hyperglycemia, hypokalemia, hypervolemia, acidosis. Arthralgia. Agitation, dizziness, anxiety, convulsion. Pneumonia, apnea, increased cough, lung edema.
Useful Linkhttp://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8a5982c6-825f-4d05-90f5-1519a7291d15
PubMed ID16301226
3-D StructureTh1158 (View) or (Download)


Entry 2
(2) Primary information
ID1668
ThPP IDTh1158
Therapeutic Peptide/Protein NameAprotinin
SequenceRPDFCLEPPYTGPCKARIIRYFYNAKAGLCQTFVYGGCRAKRNNFKSAED view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight6511.439
Chemical FormulaC284H432N84O79S7
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)>100
Half LifePlasma half life: 150 minutes, Elimination half life: 10hrs
DescriptionN.A.
Indication/DiseaseN.A.
PharmacodynamicsN.A.
Mechanism of ActionN.A.
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of DistributionN.A.
ClearanceN.A.
CategoriesN.A.
Patents NumberCA2030783
Date of Issue13/10/90
Date of ExpiryN.A.
Drug InteractionHeparin- Aprotinin, in the presence of heparin, has been found to prolong the activated clotting time (ACT) as measured by a celite surface activation method
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 Linkhttp://www.rxlist.com/trasylol-drug.htm
PubMed ID16301226
3-D StructureTh1158 (View) or (Download)


Entry 3
(3) Primary information
ID1669
ThPP IDTh1158
Therapeutic Peptide/Protein NameAprotinin
SequenceRPDFCLEPPYTGPCKARIIRYFYNAKAGLCQTFVYGGCRAKRNNFKSAED view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight6511.439
Chemical FormulaC284H432N84O79S7
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)>100
Half LifePlasma half life: 150 minutes, Elimination half life: 10hrs
DescriptionN.A.
Indication/DiseaseN.A.
PharmacodynamicsN.A.
Mechanism of ActionN.A.
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 InteractionTenecteplase- Aprotonin may antagonize the effect of Tenecteplase
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 Linkhttp://www.drugs.com/cdi/aprotinin.html
PubMed ID16301226
3-D StructureTh1158 (View) or (Download)


Entry 4
(4) Primary information
ID1670
ThPP IDTh1158
Therapeutic Peptide/Protein NameAprotinin
SequenceRPDFCLEPPYTGPCKARIIRYFYNAKAGLCQTFVYGGCRAKRNNFKSAED view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight6511.439
Chemical FormulaC284H432N84O79S7
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)>100
Half LifePlasma half life: 150 minutes, Elimination half life: 10hrs
DescriptionN.A.
Indication/DiseaseN.A.
PharmacodynamicsN.A.
Mechanism of ActionN.A.
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 InteractionUrokinase- Aprotonin may antagonize the effect of Urokinase
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 ID16301226
3-D StructureTh1158 (View) or (Download)