Bivalirudin

Bivalirudin directly inhibits thrombin by specifically binding both to the catalytic site and to the anion-binding exosite of circulating and clot-bound thrombin. Thrombin is a serine proteinase that plays a central role in the thrombotic process, acting to cleave fibrinogen into fibrin monomers and to 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.

• Bivalirudin for injection is indicated for use as an anticoagulant for use in patients undergoing percutaneous coronary intervention (PCI) including patients with heparin-induced thrombocytopenia and heparin-induced thrombocytopenia and thrombosis syndrome.

• Bivalirudin is contraindicated in patients with: • Active major bleeding; • Hypersensitivity (e.g., anaphylaxis) to bivalirudin or its components [see Adverse Reactions (6.1) ] .contraindicated

• The recommended dosage is a 0.75 mg/kg intravenous bolus dose followed immediately by a 1.75 mg/kg/h intravenous infusion for the duration of the procedure. Five minutes after the bolus dose has been administered, an activated clotting time (ACT) should be performed and an additional bolus dose of 0.3 mg/kg should be given if needed. • Extending duration of infusion post-procedure up to 4 hours should be considered in patients with ST segment elevation MI (STEMI). ( 2.1 ) 2.1 Recommended Dosage Bivalirudin has been studied only in patients receiving concomitant aspirin. The recommended dose of bivalirudin is an intravenous bolus dose of 0.75 mg/kg, followed immediately by an infusion of 1.75 mg/kg/h for the duration of the procedure. Five minutes after the bolus dose has been administered, an activated clotting time (ACT) should be performed and an additional bolus of 0.3 mg/kg should be given if needed. Extended duration of infusion following PCI at 1.75 mg/kg/h for up to 4 hours post-procedure should be considered in patients with ST segment elevation MI (STEMI). 2.2 Dose Adjustment in Renal Impairment Bolus Dose No reduction in the bolus dose is needed for any degree of renal impairment. Maintenance Infusion In patients with creatinine clearance less than 30mL/min (by Cockcroft Gault equation), reduce the infusion rate to 1 mg/kg/h. Monitor anticoagulant status in patients with renal impairment. In patients on hemodialysis, reduce the infusion rate to 0.25 mg/kg/h [see Use in Specific Populations ( 8.6 ) , Clinical Pharmacology ( 12.3 )] .

• Bleeding Events: Bivalirudin increases the risk of bleeding. ( 5.1 , 6.1 , 12.2 ) • Acute Stent Thrombosis: Increased incidence of acute stent thrombosis in STEMI patients undergoing primary PCI. ( 2.1 , 5.2 ) • Thrombotic Risk with Coronary Artery Brachytherapy: An increased risk of thrombus formation, including fatal outcomes, in gamma brachytherapy. ( 5.3 ) 5.1 Bleeding Events Bivalirudin increases the risk of bleeding [see Adverse Reactions ( 6.1 )] . An unexplained fall in blood pressure or hematocrit should lead to serious consideration of a hemorrhagic event and cessation of bivalirudin administration. Monitor patients receiving bivalirudin for signs and symptoms of bleeding. Monitor patients with disease states associated with an increased risk of bleeding more frequently for bleeding. 5.2 Acute Stent Thrombosis in Patients with STEMI Undergoing PCI Acute stent thrombosis (AST) (less than 4 hours) has been observed at a greater frequency in bivalirudin treated patients (1.2%, 36/2889) compared to heparin treated patients (0.2%, 6/2911) with STEMI undergoing primary PCI. Among patients who experienced an AST, one fatality (0.03%) occurred in a bivalirudin treated patient and one fatality (0.03%) in a heparin treated patient. These patients have been managed by Target Vessel Revascularization (TVR). Patients should remain for at least 24 hours in a facility capable of managing ischemic complications and should be carefully monitored following primary PCI for signs and symptoms consistent with myocardial ischemia.

Most common adverse reaction (>2%) was bleeding. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Sandoz Inc. at 1-800-525-8747 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. In the BAT trials, 79 of the 2161 (3.7%) patients undergoing PCI for treatment of unstable angina and randomized to bivalirudin experienced major bleeding events, which consisted of intracranial bleeding, retroperitoneal bleeding, and clinically overt bleeding with a decrease in hemoglobin greater than 3 g/dL or leading to a transfusion of greater than 2 units of blood. 6.2 Immunogenicity As with all peptides, there is potential for immunogenicity. The detection of antibody formation is highly dependent on the sensitivity and specificity of the assay. Additionally, the observed incidence of antibody (including neutralizing antibody) positivity in an assay may be influenced by several factors including assay methodology, sample handling, timing of sample collection, concomitant medications, and underlying disease. For these reasons, comparison of the incidence of antibodies to bivalirudin in the studies described below with the incidence of antibodies in other studies or to other products may be misleading.

• Geriatric patients: Increased bleeding risk possible. ( 8.5 ) • Renal impairment: Reduce infusion dose and monitor ACT. ( 2.2 , 8.6 ) 8.1 Pregnancy Risk Summary There are no data available on use of bivalirudin in pregnant women to inform a drug-associated risk of adverse developmental outcomes. Reproduction studies in rats and rabbits administered subcutaneously doses up to 1.6 times and 3.2 times the maximum recommended human dose (MRHD) of 15 mg/kg/day based on body surface area (BSA) during organogenesis, respectively, revealed no evidence of fetal harm. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data Reproductive studies have been performed in rats at subcutaneous doses up to 150 mg/kg/day (1.6 times the maximum recommended human dose based on body surface area) and rabbits at subcutaneous doses up to 150 mg/kg/day (3.2 times the maximum recommended human dose based on body surface area). These studies revealed no harm to the fetus attributable to bivalirudin.

Metabolism

Bivalirudin exhibits linear pharmacokinetics following IV administration to patients undergoing PTCA. In these patients, a mean steady state bivalirudin concentration of 12.3 ± 1.7 mcg/mL is achieved following an IV bolus of 1 mg/kg and a 4-hour 2.5 mg/kg/h IV infusion.

Cases of overdose of up to 10 times the recommended bolus or continuous infusion dose of bivalirudin have been reported in clinical trials and in postmarketing reports. A number of the reported overdoses were due to failure to adjust the infusion dose of bivalirudin in persons with renal dysfunction including persons on hemodialysis [see Dosage and Administration (2.2) ] . Bleeding, as well as deaths due to hemorrhage, have been observed in some reports of overdose. In cases of suspected overdosage, discontinue bivalirudin immediately and monitor the patient closely for signs of bleeding. There is no known antidote to bivalirudin. Bivalirudin is hemodialyzable [see Clinical Pharmacology (12.3) ] .

• Dec 15, 2000NDANDA020873Sandoz
• Oct 28, 2016ANDAANDA090189Fresenius Kabi Usa
• May 26, 2017ANDAANDA201577Dr Reddys
• Nov 22, 2017ANDAANDA206551Accord Hlthcare
• Jun 1, 2018ANDAANDA202471Mylan Institutional
• Jul 16, 2018ANDAANDA091602Meitheal
• Jul 27, 2018ANDAANDA205962Eugia Pharma
• Jul 25, 2019NDANDA211215Maia Pharms Inc

1. 1Drug Ineffective17919%
2. 2Off Label Use10811%
3. 3Haemorrhage869.1%
4. 4Heparin-induced Thrombocytopenia717.5%
5. 5Gastrointestinal Haemorrhage434.6%
6. 6Thrombosis384.0%
7. 7Acute Myocardial Infarction353.7%
8. 8Vascular Stent Thrombosis353.7%
9. 9Thrombosis In Device333.5%
10. 10Hypotension323.4%
11. 11Cardiac Arrest242.5%
12. 12Thrombocytopenia242.5%
13. 13Haemorrhage Intracranial232.4%
14. 14Deep Vein Thrombosis222.3%
15. 15Pulmonary Embolism212.2%

The 10 most recently updated of 92 ClinicalTrials.gov registrations naming Bivalirudin as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• BivaLirudin versUS Heparin in Extracorporeal Membrane Oxygenation
  Recruiting · Phase 2 · Interventional · 80 enrolled · Sydney Local Health District
  NCT05959252updated 2026-05-08
• Pharmacokinetics, Pharmacodynamics, and Safety Profile of Understudied Drugs Administered to Children Per Standard of Care (POPS)
  Recruiting · Observational · 5,000 enrolled · Duke University
  NCT04278404updated 2026-04-06
• Use of Bivalirudin for Anticoagulation in Patients With Extracorporeal Membrane Oxygenation
  Recruiting · Interventional · 154 enrolled · Xiaotong Hou
  NCT06275555updated 2026-04-06
• Bivalirudin Versus Heparin During PCI in High Bleeding Risk Patients With Acute Coronary Syndromes
  Not yet recruiting · Phase 4 · Interventional · 5,270 enrolled · Shenyang Northern Hospital
  NCT07383155updated 2026-02-03
• Multicenter Trial of ECMO in Children With Severe Cardiac Failure Using the Cardiohelp System
  Recruiting · Phase 2 · Interventional · 50 enrolled · Stanford University
  NCT06080074updated 2026-01-29
• A Single Center Diagnostic, Cross-sectional Study of Coronary Microvascular Dysfunction
  Active not recruiting · Interventional · 206 enrolled · NYU Langone Health
  NCT03537586updated 2025-11-28
• Bivalirudin With Prolonged Full Dose Infusion Versus Heparin Alone During Emergency PCI
  Completed · Interventional · 6,016 enrolled · Shenyang Northern Hospital
  NCT03822975updated 2025-08-27
• A Study on the Impact of Bivalirudin Usage During PCI for High-risk Plaques on Post-PCI Coronary Microcirculation.
  Recruiting · Phase 4 · Interventional · 70 enrolled · Peking University First Hospital
  NCT05984537updated 2025-08-12
• Pharmacokinetics of Bivalirudin for Pediatric Anticoagulation
  Recruiting · Observational · 30 enrolled · Boston Children's Hospital
  NCT03532399updated 2025-07-02
• Bivalirudin with Prolonged Infusion During PCI Versus Heparin After Fibrinolytic Therapy
  Not yet recruiting · Interventional · 2,400 enrolled · First Affiliated Hospital Xi'an Jiaotong University
  NCT06861374updated 2025-03-06

Frequently asked questions

How does Bivalirudin work?

Bivalirudin directly inhibits thrombin by specifically binding both to the catalytic site and to the anion-binding exosite of circulating and clot-bound thrombin. Thrombin is a serine proteinase that plays a central role in the thrombotic process, acting to cleave fibrinogen into fibrin monomers and to 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.

What is Bivalirudin used for?

According to FDA labeling, Bivalirudin carries indications including: Bivalirudin for injection is indicated for use as an anticoagulant for use in patients undergoing percutaneous coronary intervention (PCI) including patients with heparin-induced thrombocytopenia and heparin-induced thrombocytopenia and thrombosis syndrome.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Bivalirudin?

Bivalirudin is classified as Direct thrombin inhibitors, Anti-coagulant, Direct Thrombin Inhibitor, Antithrombins, Thrombin Inhibitors, Decreased Coagulation Factor Activity, Hemorrheologic Alteration.

What are the brand names for Bivalirudin?

Bivalirudin is marketed under brand names including Angiomax.

What are the contraindications for Bivalirudin?

Bivalirudin labeling lists contraindications including: Bivalirudin is contraindicated in patients with: • Active major bleeding; • Hypersensitivity (e.g., anaphylaxis) to bivalirudin or its components [see Adverse Reactions (6.1) ] .. Always consult the full prescribing information and a clinician.