BIVALIRUDIN

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/20873lbl.pdf | https://www.ncbi.nlm.nih.gov/pubmed/11833835

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
Prothrombin 4 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	Inhibitor 8504

Conditions

Condition	Modality	Targets	Highest Phase	Product
unstable angina 2 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/20873lbl.pdf	Palliative		Approved 8583	ANGIOMAX Approved Use Angiomax™ 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 Date 2000

PubMed

Title	Date	PubMed
Thrombin-specific inhibition by and slow cleavage of hirulog-1.	1992 May 1	1290488
Direct thrombin inhibitors.	1999 Dec	10629409
Clinical outcomes of bivalirudin for ischemic heart disease.	1999 Nov 16	10562259
Bivalirudin versus heparin during coronary angioplasty for unstable or postinfarction angina: Final report reanalysis of the Bivalirudin Angioplasty Study.	2001 Dec	11717596
Thrombin-specific anticoagulation with bivalirudin versus heparin in patients receiving fibrinolytic therapy for acute myocardial infarction: the HERO-2 randomised trial.	2001 Dec 1	11741625
Direct and indirect antithrombins. Heparins, low molecular weight heparins, heparinoids, and hirudin.	2001 Feb	11270128
Thrombin inhibitor approved for anticoagulation during angioplasty.	2001 Mar 1	11258166
Hirulog-like peptide reduces balloon catheter injury induced neointima formation in rat carotid artery without increase in bleeding tendency.	2001 Mar-Apr	11316950
Laser-induced noninvasive vascular injury models in mice generate platelet- and coagulation-dependent thrombi.	2001 May	11337359
Caspofungin acetate, bivalirudin.	2001 Oct 1	11596694
Optimal treatment and current situation in reperfusion after thrombolysis for acute myocardial infarction.	2002	12553491
Bivalirudin: a review of its potential place in the management of acute coronary syndromes.	2002	11929334
Direct thrombin inhibitors for percutaneous coronary intervention in the current era of platelet glycoprotein IIb/IIIa inhibition.	2002 Apr	12063809
Pharmacodynamic profile of the direct thrombin antagonist bivalirudin given in combination with the glycoprotein IIb/IIIa antagonist eptifibatide.	2002 Apr	11923794
Bivalirudin, a bivalent, thrombin specific anticoagulant as an alternative to heparin in interventional procedures as an alternative to heparin in interventional procedures.	2002 Aug	12215763
Bivalirudin: a direct thrombin inhibitor for percutaneous transluminal coronary angioplasty.	2002 Aug	12173785
Anticoagulation with bivalirudin during cardiopulmonary bypass in cardiac surgery.	2002 Dec	12643418
Current anticoagulation options in percutaneous intervention: designing patient-specific strategies.	2002 Fall	12556751
Improved efficacy and less bleeding: further evidence of a unique uncoupling of benefit and risk with bivalirudin.	2002 Feb	11835018
Publication policy, informed consent, and the randomized clinical trial.	2002 Feb	11835017
Reversing anticoagulants both old and new.	2002 Jun-Jul	12557411
Percutaneous coronary intervention with bivalirudin anticoagulation, immediate sheath removal, and early ambulation: a feasibility study with implications for day-stay procedures.	2002 Mar	11870930
Gateways to clinical trials.	2002 Oct	12500432
A Bayesian ordinal model for heterogeneity in a multi-centre myocardial infarction clinical trial.	2002 Oct 30	12369078
Heparin-induced thrombocytopenia: pathophysiology and new treatment options.	2002 Sep-Dec	13679659
Heparin-induced thrombocytopenia and cardiac surgery.	2003 Aug	12902132
Contemporary use of antiplatelet therapies in percutaneous coronary interventions.	2003 Aug	12878902
Can bivalirudin and provisional GP IIb/IIIa blockade REPLACE heparin and planned glycoprotein IIb/IIIa blockade during percutaneous coronary intervention?	2003 Aug	12877649
Clinician update: direct thrombin inhibitors in acute coronary syndromes.	2003 Feb	14574076
Bivalirudin monitored with the ecarin clotting time for anticoagulation during cardiopulmonary bypass.	2003 Feb	12538181
The evolving role of direct thrombin inhibitors in acute coronary syndromes.	2003 Feb 19	12644344
Should bivalirudin replace heparin during percutaneous coronary interventions?	2003 Feb 19	12588276
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	12588269
Favorable outcome with bivalirudin anticoagulation during cardiopulmonary bypass.	2003 Jan	12537226
Alternative methods of anticoagulation for dialysis-dependent patients with heparin-induced thrombocytopenia.	2003 Jan-Feb	12535303
Hirulog-like peptide reduces restenosis and expression of tissue factor and transforming growth factor-beta in carotid artery of atherosclerotic rabbits.	2003 Jul	12860248
Economic impact of bleeding complications and the role of antithrombotic therapies in percutaneous coronary intervention.	2003 Jul 15	12908378
Current anticoagulant therapy--unmet clinical needs.	2003 Jul 15	12818628
Bivalirudin as a foundation anticoagulant in peripheral vascular disease: a safe and feasible alternative for renal and iliac interventions.	2003 Jun	12777673
Bivalirudin (Angiomax) use during intracoronary brachytherapy may predispose to acute closure.	2003 Mar	12652325
Informed consent during the clinical emergency of acute myocardial infarction (HERO-2 consent substudy): a prospective observational study.	2003 Mar 15	12648970
Safe and efficacious use of bivalirudin for percutaneous coronary intervention with adjunctive platelet glycoprotein IIb/IIIa receptor inhibition.	2003 Mar 15	12633814
Predicting the pharmacology of thrombin inhibitors.	2003 May	12871372
In-hospital complications of peripheral vascular interventions using unfractionated heparin as the primary anticoagulant.	2003 May	12730630
A 24-hour continuous infusion study of bivalirudin in the rat.	2003 May-Jun	12851152
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	14583359
Successful use of bivalirudin for cardiopulmonary bypass in a patient with heparin-induced thrombocytopenia.	2003 Oct	14579220
Direct thrombin inhibitors for non-ST-segment elevation acute coronary syndromes: what, when, and where?	2003 Oct	14564303
Argatroban for off-pump coronary artery bypass surgery.	2003 Oct	14500190
Antibodies against lepirudin are polyspecific and recognize epitopes on bivalirudin.	2004 Jan 15	14512301

Patents

Sample Use Guides

In Vivo Use Guide

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

Substance Class	Protein Created by `admin` on `Wed Apr 02 08:41:11 GMT 2025` Edited by `admin` on `Wed Apr 02 08:41:11 GMT 2025`
Protein Sub Type
Sequence Type	COMPLETE
Record UNII	TN9BEX005G
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

BIVALIRUDIN

Official Name

English

BG-8967

Preferred Name

English

bivalirudin [INN]

Common Name

English

BIVALIRUDIN [ORANGE BOOK]

Common Name

English

BIVALIRUDIN [VANDF]

Common Name

English

BIVALIRUDIN [MART.]

Common Name

English

Bivalirudin [WHO-DD]

Common Name

English

BIVALIRUDIN [EMA EPAR]

Common Name

English

L-LEUCINE, D-PHENYLALANYL-L-PROLYL-L-ARGINYL-L-PROLYLGLYCYLGLYCYLGLYCYLGLYCYL-L-ASPARAGINYLGLYCYL-L-.ALPHA.-ASPARTYL-L-PHENYLALANYL-L-.ALPHA.-GLUTAMYL-L-.ALPHA.-GLUTAMYL-L-ISOLEUCYL-L-PROLYL-L-.ALPHA.-GLUTAMYL-L-.ALPHA.-GLUTAMYL-L-TYROSYL-

Systematic Name

English

BIVALIRUDIN [MI]

Common Name

English

BIVALIRUDIN [USP-RS]

Common Name

English

BG8967

Code

English

BIVALIRUDIN [USAN]

Common Name

English

Classification Tree Code System Code

WHO-ATC

B01AE06