==== 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.====

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Primary information
ThPP IDTh1006
Therapeutic Peptide/Protein NameBivalirudin
SequenceFPRPGGGGNGDFEEIPEEYL view full sequnce in fasta
Functional ClassificationIa
Molecular Weight2180.2853
Chemical FormulaC98H138N24O33
Isoelectric Point3.91
Hydrophobicity-0.985
Melting Point (℃)N.A.
Half LifeCreatinine clearance 10-29mL/min: 0.95 hours
DescriptionBivalirudin is a synthetic 20 residue peptide which acts as a thrombin inhibitor. Once bound to the active site of the inhibitor, thrombin cannot activate fibrinogen into fibrin which is a crucial step in the formation of thrombus. As it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure. It is administered intravenously.
Indication/DiseaseFor treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is planned.
PharmacodynamicsBivalirudin directly and reversibly inhibits thrombin by specifically binding to both the catalytic site and the anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible as thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin.
Mechanism of ActionInhibits the action of thrombin by binding to both its catalytic site and to its anion-binding exosite. Thrombin, a serine proteinase that plays a central role in the thrombotic process, acts to cleave fibrinogen into fibrin monomers and activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.
ToxicityBased on a study by Gleason et al., the no observed adverse effect level (NOAEL) for bivalirudin administered to rats via Intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h.
Metabolism80% proteolytic cleavage
AbsorptionBivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 ± 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr Intravenous infusion given over 4 hours.
Volume of Distribution0.2L/kg
Clearance3.4 mL/min/kg [mild renal function]
CategoriesAntithrombins
Patents NumberUS5196404
Date of Issue23/05/93
Date of Expiry23/05/10
Drug InteractionGemcitabine, Gemcitabine may enhance the adverse/toxic effect of Bleomycin. The risk of pulmonary toxicity may be increased. Use extreme caution if using gemcitabine and bleomycin in combination. Monitor for the development of pulmonary toxicity
TargetN.A.
Information of corresponding available drug in the market
Brand NameAngiox
CompanyThe Medicines Company UK Ltd
Brand DiscriptionN.A.
Prescribed forUsed as an anticoagulant in adult patients undergoing percutaneous coronary intervention (PCI), including patients with ST-segment elevation myocardial infarction (STEMI) undergoing primary PCI. Angiox is also indicated for the treatment of adult patients
Chemical NameN.A.
FormulationEach vial contains 250 mg bivalirudin.
Physcial AppearncePowder for concentrated solution
Route of AdministrationInjection
Recommended Dosage0.75 mg/kg IV bolus, initially, followed by continuous infusion at rate of 1.75 mg/kg/hr for duration of procedure
ContraindicationHypersensitivity, active bleeding or increased risk of bleeding because of haemostasis disorder or irreversible coagulation disorder, uncontrolled hypertension, subacute bacterial endocarditis, severe renal impairment and in dialysis dependent pateints,
Side EffectsN.A.
Useful Linkhttp://www.rxlist.com/angiomax-drug.htm
PubMed ID17381384, 16553503, 16466327, 12851152, 11156732
3-D StructureTh1006 (View) or (Download)