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 8146

Conditions

Condition	Modality	Targets	Highest Phase	Product
unstable angina 2 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/20873lbl.pdf	Palliative		Approved 8307	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 9.7683839E11

PubMed

Title	Date	PubMed
Thrombin-specific inhibition by and slow cleavage of hirulog-1.	1992 May 1	1290488
Development and current applications of thrombin-specific inhibitors.	2001 Jun	12769663
Bivalirudin: a new approach to anticoagulation.	2001 Mar-Apr	11975781
Current developments in antithrombotic therapy: the role of antithrombin agents.	2002	12811005
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
New drugs 2002. Part II.	2002 Apr	11969021
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
Direct thrombin inhibitors in acute coronary syndromes.	2002 Aug 10	12241752
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
Bivalirudin as a replacement for unfractionated heparin in unstable angina/non-ST-elevation myocardial infarction: observations from the TIMI 8 trial. The Thrombolysis in Myocardial Infarction.	2002 Feb	11835024
Bivalirudin pharmacokinetics and pharmacodynamics: effect of renal function, dose, and gender.	2002 Jun	12087346
The role of thrombin inhibition during percutaneous coronary intervention.	2002 Jun	12064571
A practical cost analysis of bivalirudin.	2002 Jun	12064569
Bivalirudin: an anticoagulant for acute coronary syndromes and coronary interventions.	2002 Jun	12036417
Absolute and relative truth in clinical trials.	2002 Jun 1	12057577
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
[What is new in antithrombotic treatment?].	2002 Mar-Apr	11937438
Bivalirudin with planned or provisional abciximab versus low-dose heparin and abciximab during percutaneous coronary revascularization: results of the Comparison of Abciximab Complications with Hirulog for Ischemic Events Trial (CACHET).	2002 May	12040347
Gateways to clinical trials.	2002 Oct	12500432
Slowed ST segment recovery despite early infarct artery patency in patients with Q waves at presentation with a first acute myocardial infarction. Implications of initial Q waves on myocyte reperfusion.	2002 Sep	12208225
Effect of non-heparin thrombin antagonists on thrombin generation, platelet function, and clot structure in whole blood.	2003	14515016
Direct thrombin inhibitors in cardiac disease.	2003	12668887
Management of thrombotic and cardiovascular disorders in the new millenium.	2003 Apr	12812377
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
The evolving role of direct thrombin inhibitors in acute coronary syndromes.	2003 Feb 19	12644344
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
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
Bivalirudin use in off-pump myocardial revascularization in patients with heparin-induced thrombocytopenia [corrected].	2003 Jul	12842558
Bivalirudin in peripheral vascular interventions: a single center experience.	2003 Jul	12840239
Evolving role of bivalirudin in percutaneous coronary interventions; impact of the REPLACE-2 study.	2003 Jun	12783606
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
Direct thrombin inhibitors.	2003 May	12739991
Correlation of point-of-care ecarin clotting time versus activated clotting time with bivalirudin concentrations.	2003 May 1	12714157
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
Bivalirudin provides increasing benefit with decreasing renal function: a meta-analysis of randomized trials.	2003 Oct 15	14556866
Bivalirudin in percutaneous coronary intervention.	2003 Sep 15	14521034

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 `Sun Dec 18 19:34:36 UTC 2022` Edited by `admin` on `Sun Dec 18 19:34:36 UTC 2022`
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

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

BG-8967

Code

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