Overview
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In plain language
Bivalirudin is a hospital medicine that prevents blood clots. It is a lab-made chain of 20 amino acids modeled on hirudin, the natural anti-clotting substance in leech saliva.
Doctors give it through an IV during heart procedures such as angioplasty and stenting. It works quickly and wears off quickly once stopped, which helps doctors control bleeding risk. Bleeding is its main side effect.
For students
Bivalirudin is a 20-residue synthetic peptide (about 2,180 Da) and a direct thrombin inhibitor. Its N-terminal D-Phe-Pro-Arg-Pro segment binds thrombin's active site, a glycine linker spans the enzyme, and a C-terminal segment from hirudin binds exosite 1, the fibrinogen-binding site.
Unlike heparin, it does not need antithrombin and can inhibit thrombin that is already bound to clots. Thrombin slowly cleaves bivalirudin's Arg3–Pro4 bond, so inhibition is reversible. Its half-life is about 25 minutes in people with normal kidney function, and it is used as an anticoagulant during percutaneous coronary intervention.
For researchers and instructors
Design. A rational-design "hirulog": bivalent binding (active site plus exosite 1) gives high affinity in a much smaller molecule than 65-residue hirudin.
Pharmacokinetics. Cleared by proteolysis and renal excretion; dose adjustment is needed in renal impairment. Monitored by ACT during PCI.
Clinical evidence. Large randomized PCI trials compared bivalirudin with heparin plus or minus glycoprotein IIb/IIIa inhibitors, generally showing less bleeding, with debated effects on stent thrombosis depending on post-procedure infusion.
Status. FDA-approved (Angiomax and generics) for use as an anticoagulant during PCI.
Molecular identity
- Amino acids
- 20
- Molecular weight
- ~2,180.3 Da
- Formula
- C₉₈H₁₃₈N₂₄O₃₃
- Sequence
- D-Phe–Pro–Arg–Pro–Gly–Gly–Gly–Gly–Asn–Gly–Asp–Phe–Glu–Glu–Ile–Pro–Glu–Glu–Tyr–Leu
Origin and history
In 1884 John Haycraft found that leech saliva stops blood from clotting. In the 1950s Fritz Markwardt in Germany isolated the substance responsible, hirudin.
In about 1990, John Maraganore at Biogen designed a 20-amino-acid version, then called hirulog. Developed by The Medicines Company, it was approved as Angiomax in 2000 to prevent clots during heart procedures.
Key people
- John HaycraftDiscovered leech anticoagulant (1884)
- Fritz MarkwardtIsolated hirudin
- John MaraganoreDesigned bivalirudin
Timeline
- 1884
Leech saliva anticoagulant discovered
- 1950s
Hirudin isolated
- 1990
Bivalirudin designed
- 2000
Angiomax approved
See every peptide on one history timeline.
Human evidence
Large randomized trials compared it with heparin during percutaneous coronary intervention.
Registration and enrollment are not proof of benefit; check study results directly.
Explore original publications and distinguish preclinical findings from controlled human evidence.
Safety and regulatory status
See every compound on the regulatory tracker.
FDA-approved for hospital use.
This profile is educational and does not provide treatment, dosing or sourcing guidance.
Sources
- PubMed literature search: Bivalirudin
- PubChem compound search: Bivalirudin
- DailyMed (FDA label search): Bivalirudin
- PubMed: Maraganore hirulog
- ClinicalTrials.gov search: Bivalirudin
Hernandez Gener, E. (2026, November 7). Bivalirudin: molecular data, research history and evidence. VALREXA Biosciences. https://valrexa.com/peptides/bivalirudin.html
APA style · Last reviewed November 7, 2026 · Our editorial standardsLast reviewed November 7, 2026. Trial and regulatory status can change; confirm in the linked registries. This profile is educational and is not medical advice, a treatment recommendation, or dosing or sourcing guidance. Report an error · Corrections policy