Bivalirudin is a synthetic 20-amino-acid peptide (MW ~2180.3 g/mol) that acts as a direct, reversible thrombin inhibitor. It was FDA-approved in 2000 (Angiomax) for use as an anticoagulant in patients with unstable angina undergoing percutaneous transluminal coronary angioplasty (PTCA), and for patients with or at risk of heparin-induced thrombocytopenia (HIT) undergoing PCI. Bivalirudin is a synthetic analog of hirudin that binds both the catalytic active site and the anion-binding exosite of thrombin.
Category: Cardiovascular / Antithrombotic. Evidence rating: A (strong human clinical data).
Clinical status: FDA-approved (Angiomax for PCI anticoagulation, 2000)
Bivalirudin is a bivalent direct thrombin inhibitor. Its N-terminal D-Phe-Pro-Arg-Pro sequence binds to the active (catalytic) site of thrombin, while its C-terminal dodecapeptide binds to the anion-binding exosite 1 (fibrinogen-binding site). This bivalent binding provides highly specific and…
Safety considerations: Common: bleeding is the primary adverse effect (major bleeding 2.4-4.9% in pivotal trials, significantly lower than heparin + GP IIb/IIIa comparator arms); Acute stent thrombosis: slightly increased risk in the first 24 hours compared to heparin-based regimens (1.3% vs 0.3% in HORIZONS-AMI); mitigated by concomitant dual antiplatelet therapy and adequate dosing; Back pain, nausea, headache, and hypotension reported in clinical trials.
Reviewed by the PeptideAtlas Editorial Team.
| Molecular weight | ~2180.3 g/mol |
|---|---|
| CAS number | 128270-60-0 |
| Half-life | ~25 minutes (normal renal function) |
| Bioavailability | 100% (intravenous) |
| Production method | synthetic |
| Anti-doping status | not-listed |
| US regulatory status | FDA-approved (Angiomax, 2000) for PCI anticoagulation in unstable angina and HIT/at risk for HIT. Generic versions available. |
Related peptides: Desirudin.
Bivalirudin directly inhibits thrombin (both free and clot-bound) without requiring antithrombin III as a cofactor, while heparin works indirectly by potentiating antithrombin III. Bivalirudin does not activate platelets, does not bind to plasma proteins (predictable dose-response), has a short half-life (25 min vs hours for heparin), and cannot cause HIT.
Patients with heparin-induced thrombocytopenia cannot receive heparin. Bivalirudin is a direct thrombin inhibitor with no structural similarity to heparin and does not cross-react with HIT antibodies. It is FDA-approved specifically for PCI in patients with or at risk for HIT.
Yes, bivalirudin remains an important anticoagulant option for PCI, particularly in bleeding-risk patients and HIT. However, its use varies by institution and has been influenced by the availability of generic versions, potent oral P2Y12 inhibitors, and evolving PCI anticoagulation protocols.
Coverage on this site: Common Misunderstandings in Peptide Synthesis Explained.