Bivalirudin is a synthetic 20 amino acid peptide rationally designed based on structural studies of hirudin, a naturally occurring anticoagulant. Bivalirudin is sold under the brand name Angiomax and is indicated for use as an anticoagulant in patients with unstable angina undergoing percutaneous transluminal coronary angioplasty (PTCA). It is intended for use with aspirin and has been studied only in patients receiving concomitant aspirin. Bivalirudin directly inhibits thrombin by binding simultaneously to its active catalytic site and its substrate recognition site.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: P00734|||Q9UCA1 Gene ID: 2147.0 Gene Symbol: F2 Target Organism: Homo sapiens (Human) |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Palliative | ANGIOMAX Approved UseAngiomax™ is indicated for use as an anticoagulant in patients with unstable angina undergoing percutaneous transluminal coronary angioplasty (PTCA). Angiomax is intended for use with aspirin and has been studied only in patients receiving concomitant aspirin. Launch Date2000 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Thrombin-specific inhibition by and slow cleavage of hirulog-1. | 1992 May 1 |
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| Development and current applications of thrombin-specific inhibitors. | 2001 Jun |
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| Current developments in antithrombotic therapy: the role of antithrombin agents. | 2002 |
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| Optimal treatment and current situation in reperfusion after thrombolysis for acute myocardial infarction. | 2002 |
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| Direct thrombin inhibitors in acute coronary syndromes. | 2002 Aug 10 |
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| Anticoagulation with bivalirudin during cardiopulmonary bypass in cardiac surgery. | 2002 Dec |
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| Current anticoagulation options in percutaneous intervention: designing patient-specific strategies. | 2002 Fall |
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| Decreased platelet reactivity in blood anticoagulated with bivalirudin or enoxaparin compared with unfractionated heparin: implications for coronary intervention. | 2002 Jun |
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| Reversing anticoagulants both old and new. | 2002 Jun-Jul |
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| Direct thrombin inhibitors. | 2002 May 1 |
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| Gateways to clinical trials. | 2002 Oct |
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| A Bayesian ordinal model for heterogeneity in a multi-centre myocardial infarction clinical trial. | 2002 Oct 30 |
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| Heparin-induced thrombocytopenia: pathophysiology and new treatment options. | 2002 Sep-Dec |
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| Effect of non-heparin thrombin antagonists on thrombin generation, platelet function, and clot structure in whole blood. | 2003 |
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| Direct thrombin inhibitors in cardiac disease. | 2003 |
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| Management of thrombotic and cardiovascular disorders in the new millenium. | 2003 Apr |
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| Anticoagulation in acute cardiac care in patients with chronic kidney disease. | 2003 Apr |
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| Heparin-induced thrombocytopenia and cardiac surgery. | 2003 Aug |
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| Contemporary use of antiplatelet therapies in percutaneous coronary interventions. | 2003 Aug |
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| Can bivalirudin and provisional GP IIb/IIIa blockade REPLACE heparin and planned glycoprotein IIb/IIIa blockade during percutaneous coronary intervention? | 2003 Aug |
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| Clinician update: direct thrombin inhibitors in acute coronary syndromes. | 2003 Feb |
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| Bivalirudin monitored with the ecarin clotting time for anticoagulation during cardiopulmonary bypass. | 2003 Feb |
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| The evolving role of direct thrombin inhibitors in acute coronary syndromes. | 2003 Feb 19 |
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| Should bivalirudin replace heparin during percutaneous coronary interventions? | 2003 Feb 19 |
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| Bivalirudin and provisional glycoprotein IIb/IIIa blockade compared with heparin and planned glycoprotein IIb/IIIa blockade during percutaneous coronary intervention: REPLACE-2 randomized trial. | 2003 Feb 19 |
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| Favorable outcome with bivalirudin anticoagulation during cardiopulmonary bypass. | 2003 Jan |
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| Alternative methods of anticoagulation for dialysis-dependent patients with heparin-induced thrombocytopenia. | 2003 Jan-Feb |
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| Hirulog-like peptide reduces restenosis and expression of tissue factor and transforming growth factor-beta in carotid artery of atherosclerotic rabbits. | 2003 Jul |
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| Bivalirudin use in off-pump myocardial revascularization in patients with heparin-induced thrombocytopenia [corrected]. | 2003 Jul |
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| Bivalirudin in peripheral vascular interventions: a single center experience. | 2003 Jul |
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| Economic impact of bleeding complications and the role of antithrombotic therapies in percutaneous coronary intervention. | 2003 Jul 15 |
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| Current anticoagulant therapy--unmet clinical needs. | 2003 Jul 15 |
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| Evolving role of bivalirudin in percutaneous coronary interventions; impact of the REPLACE-2 study. | 2003 Jun |
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| Bivalirudin as a foundation anticoagulant in peripheral vascular disease: a safe and feasible alternative for renal and iliac interventions. | 2003 Jun |
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| Bivalirudin (Angiomax) use during intracoronary brachytherapy may predispose to acute closure. | 2003 Mar |
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| Informed consent during the clinical emergency of acute myocardial infarction (HERO-2 consent substudy): a prospective observational study. | 2003 Mar 15 |
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| Safe and efficacious use of bivalirudin for percutaneous coronary intervention with adjunctive platelet glycoprotein IIb/IIIa receptor inhibition. | 2003 Mar 15 |
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| Predicting the pharmacology of thrombin inhibitors. | 2003 May |
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| Direct thrombin inhibitors. | 2003 May |
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| In-hospital complications of peripheral vascular interventions using unfractionated heparin as the primary anticoagulant. | 2003 May |
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| An assessment of different filter systems for extracorporeal elimination of bivalirudin: an in vitro study. | 2003 May |
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| Correlation of point-of-care ecarin clotting time versus activated clotting time with bivalirudin concentrations. | 2003 May 1 |
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| A 24-hour continuous infusion study of bivalirudin in the rat. | 2003 May-Jun |
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| Comparison of effectiveness and safety of three different antithrombotic regimens (bivalirudin, eptifibatide, and heparin) in preventing myocardial ischemia during percutaneous coronary intervention. | 2003 Nov 1 |
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| Successful use of bivalirudin for cardiopulmonary bypass in a patient with heparin-induced thrombocytopenia. | 2003 Oct |
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| Direct thrombin inhibitors for non-ST-segment elevation acute coronary syndromes: what, when, and where? | 2003 Oct |
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| Argatroban for off-pump coronary artery bypass surgery. | 2003 Oct |
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| Bivalirudin provides increasing benefit with decreasing renal function: a meta-analysis of randomized trials. | 2003 Oct 15 |
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| Bivalirudin in percutaneous coronary intervention. | 2003 Sep 15 |
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| Antibodies against lepirudin are polyspecific and recognize epitopes on bivalirudin. | 2004 Jan 15 |
Patents
Sample Use Guides
The recommended dosage of Angiomax (bivalirudin) is an intravenous (IV) bolus dose of 1.0 mg/kg followed by a 4-hour IV infusion at a rate of 2.5 mg/kg/h. After completion of the initial 4-hour infusion, an additional IV infusion of Angiomax may be initiated at a rate of 0.2 mg/kg/h for up to 20 hours if needed.
Route of Administration:
Intravenous
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ACTIVE MOIETY
SUBSTANCE RECORD