Heart & blood Direct thrombin inhibitor
Bivalirudin
Regulatory status
Status at a glance
503A compounding status
Not nominated
We found no pending nomination for the 503A bulks list. Unless the substance has another legal pathway (for example, a USP monograph or use in an FDA-approved drug), 503A pharmacies generally may not compound with it.
- FDA approval
- An FDA-approved product contains this peptide
- 503B outsourcing
- Not determined
- Anti-doping (WADA)
- Not on the WADA Prohibited List
- DEA schedule
- Not a controlled substance
About peptide status
Most peptides discussed here are not FDA-approved for any use, and products labeled “research use only” are not for human use. Removal from Category 2 does not authorize compounding. PCAC votes are non-binding recommendations; FDA and HHS make the final decisions.
This is not medical or legal advice, and we do not publish dosing, sourcing or reconstitution information. Talk with a licensed clinician before using any peptide.
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Key takeaway
Bivalirudin is a synthetic 20-amino acid peptide anticoagulant, derived in design from the leech protein hirudin, that directly and reversibly blocks thrombin, the central enzyme in blood clotting. Sold as Angiomax, it is given intravenously during coronary procedures such as angioplasty and stenting to prevent clots, including in people who cannot receive heparin. In a large trial of heart-attack patients, using it instead of heparin plus a second blood thinner reduced major bleeding and lowered 30-day death rates.
At a glance
- FDA status
- FDA-approved peptide anticoagulant, sold as Angiomax, given intravenously in the hospital
- How it works
- Direct thrombin inhibitor, blocking the key clotting enzyme without needing a cofactor
- Main uses
- Percutaneous coronary intervention (PCI), including in patients with or at risk of heparin-induced thrombocytopenia (HIT)
- Key trial
- In a major heart-attack trial, reduced major bleeding and 30-day mortality compared with heparin plus a glycoprotein IIb/IIIa inhibitor
- Evidence strength
- FDA approved
Summary
Bivalirudin (Angiomax) is an FDA-approved peptide anticoagulant used during heart procedures. Learn how it works, when it is used, and what trials found.
What is bivalirudin?
Bivalirudin is a synthetic peptide of 20 amino acids that works as an anticoagulant, or blood thinner. It belongs to a class called direct thrombin inhibitors, meaning it blocks thrombin, the enzyme that drives the final step of clot formation, by binding to it directly. It is made by chemical synthesis and sold under the brand name Angiomax (and as Angiox outside the United States).
It is given only by intravenous infusion in a hospital, typically in a cardiac catheterization lab, and is not an oral or at-home medication.
The history of bivalirudin
Bivalirudin traces back to the leech. The medicinal leech makes a natural anticoagulant protein called hirudin, which is why a leech can feed without the blood clotting, and hirudin became the template for a family of direct thrombin inhibitors. Bivalirudin is a short synthetic analog built from that model, engineered to bind thrombin at two sites at once, which makes it a bivalent inhibitor.
It was developed as a more predictable, shorter-acting alternative to heparin for use during heart procedures, and the FDA approved it in 2000. Unlike the leech protein it was modeled on, its effect is reversible and brief, which suited the controlled setting of angioplasty.
How does bivalirudin work?
Bivalirudin works by directly binding and blocking thrombin, the enzyme at the center of blood clotting. Thrombin converts fibrinogen into the fibrin mesh that holds a clot together and also activates platelets, and by occupying thrombin, bivalirudin stops both. It is a bivalent inhibitor: one end binds thrombin's active (catalytic) site, and the other binds a separate docking region, called exosite 1, that normally grips fibrinogen. Because it latches on at two points, it blocks thrombin that is free in the blood as well as thrombin already bound inside a clot, which heparin does less well.
Its action is also reversible and short-lived. Thrombin slowly cleaves the bound drug and recovers its function, so the effect fades within roughly 25 minutes of stopping the infusion, which makes it predictable to use during a procedure.
In the HORIZONS-AMI trial of 3,602 heart-attack patients undergoing angioplasty, bivalirudin alone reduced 30-day major bleeding and lowered death from cardiac causes compared with heparin plus a glycoprotein IIb/IIIa inhibitor.
| Outcome in HORIZONS-AMI | Bivalirudin alone | Heparin plus a glycoprotein IIb/IIIa inhibitor |
|---|---|---|
| 30-day major bleeding | 4.9% | 8.3% |
| Death from cardiac causes | 1.8% | 2.9% |
Is it FDA-approved?
Editor’s note
Status: FDA-approved peptide anticoagulant, sold as Angiomax, given intravenously in the hospital
Category: FDA-approved · Primary body area: Heart & blood
Yes. The FDA approved bivalirudin (Angiomax) in 2000 as an anticoagulant for use during coronary angioplasty, and its labeling later covered patients with or at risk of heparin-induced thrombocytopenia undergoing PCI. It is an established, guideline-recognized option for anticoagulation during these procedures.
What is bivalirudin prescribed for?
Bivalirudin is used as the anticoagulant during percutaneous coronary intervention (PCI), the catheter-based procedures (angioplasty and stent placement) that open blocked heart arteries. It is given to prevent clots from forming on the catheter and the freshly treated artery during the procedure. It is especially valuable for patients with heparin-induced thrombocytopenia (HIT), a serious immune reaction to heparin, because it provides anticoagulation without using heparin at all. It is administered and monitored by the medical team, not self-administered.
What are the side effects?
The main risk of bivalirudin, as with any anticoagulant, is bleeding, though in trials it caused less major bleeding than heparin-based regimens. Other effects reported during treatment include:
- Back pain
- Nausea
- Low blood pressure
- Headache
One specific signal from the HORIZONS-AMI trial was a higher rate of acute stent thrombosis, a clot forming on the new stent, in the first 24 hours; this did not persist at 30 days and is managed by ensuring adequate antiplatelet therapy. Because it is used only in monitored hospital settings, its dosing is carefully controlled.
Sources: mechanism, pharmacology, and regulatory details from the Drugs.com bivalirudin monograph; the HORIZONS-AMI randomized controlled trial in the New England Journal of Medicine (Stone et al., 2008, DOI: 10.1056/NEJMoa0708191), indexed on PubMed; and published reviews of bivalirudin's development from hirudin. This document is educational and does not constitute medical advice.
Registered human trials
0 registered human trials on ClinicalTrials.gov that we reviewed
Sources
- [1]
- [2]
- [3]
- [4]
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