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 |
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Target ID: P00734|||Q9UCA1 Gene ID: 2147.0 Gene Symbol: F2 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/11833835 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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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 |
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Thrombin-specific inhibition by and slow cleavage of hirulog-1. | 1992 May 1 |
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Direct thrombin inhibitors. | 1999 Dec |
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Clinical outcomes of bivalirudin for ischemic heart disease. | 1999 Nov 16 |
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Bivalirudin versus heparin during coronary angioplasty for unstable or postinfarction angina: Final report reanalysis of the Bivalirudin Angioplasty Study. | 2001 Dec |
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Thrombin-specific anticoagulation with bivalirudin versus heparin in patients receiving fibrinolytic therapy for acute myocardial infarction: the HERO-2 randomised trial. | 2001 Dec 1 |
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Direct and indirect antithrombins. Heparins, low molecular weight heparins, heparinoids, and hirudin. | 2001 Feb |
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Thrombin inhibitor approved for anticoagulation during angioplasty. | 2001 Mar 1 |
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Hirulog-like peptide reduces balloon catheter injury induced neointima formation in rat carotid artery without increase in bleeding tendency. | 2001 Mar-Apr |
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Laser-induced noninvasive vascular injury models in mice generate platelet- and coagulation-dependent thrombi. | 2001 May |
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Caspofungin acetate, bivalirudin. | 2001 Oct 1 |
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Optimal treatment and current situation in reperfusion after thrombolysis for acute myocardial infarction. | 2002 |
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Bivalirudin: a review of its potential place in the management of acute coronary syndromes. | 2002 |
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Direct thrombin inhibitors for percutaneous coronary intervention in the current era of platelet glycoprotein IIb/IIIa inhibition. | 2002 Apr |
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Pharmacodynamic profile of the direct thrombin antagonist bivalirudin given in combination with the glycoprotein IIb/IIIa antagonist eptifibatide. | 2002 Apr |
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Bivalirudin, a bivalent, thrombin specific anticoagulant as an alternative to heparin in interventional procedures as an alternative to heparin in interventional procedures. | 2002 Aug |
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Bivalirudin: a direct thrombin inhibitor for percutaneous transluminal coronary angioplasty. | 2002 Aug |
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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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Improved efficacy and less bleeding: further evidence of a unique uncoupling of benefit and risk with bivalirudin. | 2002 Feb |
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Publication policy, informed consent, and the randomized clinical trial. | 2002 Feb |
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Reversing anticoagulants both old and new. | 2002 Jun-Jul |
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Percutaneous coronary intervention with bivalirudin anticoagulation, immediate sheath removal, and early ambulation: a feasibility study with implications for day-stay procedures. | 2002 Mar |
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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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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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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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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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In-hospital complications of peripheral vascular interventions using unfractionated heparin as the primary anticoagulant. | 2003 May |
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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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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 |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Molecular Formula | CHEMICAL |
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MOL_WEIGHT:NUMBER(CALCULATED) | CHEMICAL |
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Volume of Distribution | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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