Source: FDA label
| Molecular formula | C98H138N24O33 |
|---|---|
| Molecular weight | 2180.3 g/mol |
| Registered trials | 105 |
| PubChem CID | 16129704 |
| Drug class | Anti-coagulant [EPC] |
| Brand names | bivalirudin |
Mechanism of Action
12.1 Mechanism of Action 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
Patients undergoing a coronary procedure often need an anticoagulant that acts quickly and predictably. Bivalirudin is one option doctors use to manage clotting risk during these interventions.
Key takeaways
- Bivalirudin is a direct thrombin inhibitor approved as an anticoagulant during percutaneous coronary intervention (PCI).
- It works even in patients with heparin-induced thrombocytopenia (HIT) or HIT with thrombosis syndrome (HITTS).
- More than 100 clinical trials have registered bivalirudin, spanning phases from early testing to phase 3.
- FAERS reports for bivalirudin most frequently mention drug ineffectiveness and bleeding-related events.
- The label does not carry a boxed warning.
What Bivalirudin Is
Bivalirudin belongs to the anticoagulant class, specifically the direct thrombin inhibitors. It works by binding directly to thrombin, an enzyme central to clot formation. By attaching to both the catalytic site and the anion-binding exosite of thrombin, bivalirudin blocks thrombin's ability to convert fibrinogen into fibrin, the protein mesh that stabilizes blood clots. This action targets thrombin whether it is circulating freely or already bound within a forming clot.
What Bivalirudin Is Approved For
Bivalirudin is approved as an anticoagulant for patients undergoing percutaneous coronary intervention (PCI). This includes patients who have heparin-induced thrombocytopenia (HIT) or heparin-induced thrombocytopenia and thrombosis syndrome (HITTS), conditions that make standard heparin therapy unsuitable. It is marketed under the brand name Bivalirudin. The label for this drug does not include a boxed warning.
What the Evidence Shows
More than 100 clinical trials have registered bivalirudin as a study drug. One completed phase 3 trial, the CHOOSE study, examined bivalirudin in patients with HIT or HITTS undergoing off-pump coronary artery bypass grafting. A separate completed phase 1 trial, the UNBLOCK study, looked at bivalirudin's use for clots in pediatric patients.
Reported Side Effects
Reports submitted to the FDA Adverse Event Reporting System reflect counts of reported events, not confirmed incidence or proven causation. The most frequently reported issues for bivalirudin involve treatment failure and bleeding: drug ineffectiveness (185 reports), off-label use (108), and haemorrhage (87). Other reports describe heparin-induced thrombocytopenia (74), gastrointestinal haemorrhage (43), and clotting events such as vascular stent thrombosis (39), thrombosis (38), and acute myocardial infarction (35).
FAQ
What is bivalirudin used for?
Bivalirudin is approved as an anticoagulant for patients undergoing percutaneous coronary intervention (PCI). It is also used in PCI patients who have heparin-induced thrombocytopenia (HIT) or HIT with thrombosis syndrome (HITTS), conditions where heparin cannot be used safely.
How does bivalirudin work?
Bivalirudin is a direct thrombin inhibitor. It binds directly to thrombin, both the catalytic site and the anion-binding exosite, blocking thrombin's role in converting fibrinogen into the fibrin that stabilizes blood clots.
Does bivalirudin have a boxed warning?
No, the bivalirudin label does not carry a boxed warning.
What are the most commonly reported side effects of bivalirudin?
Reports to the FDA Adverse Event Reporting System most often mention drug ineffectiveness, off-label use, and haemorrhage, along with heparin-induced thrombocytopenia and gastrointestinal bleeding. These are counts of submitted reports, not confirmed rates or proof that the drug caused the event.
Has bivalirudin been studied in clinical trials?
Yes, bivalirudin has been registered in more than 100 clinical trials. Examples include the completed phase 3 CHOOSE study in HIT/HITTS patients undergoing bypass surgery and the completed phase 1 UNBLOCK study evaluating its use for clots in pediatric patients.
This page is an editorial information resource. It does not sell, prescribe, or recommend any medication.
Content is editorial information, not medical advice. Talk to your doctor before any treatment decision.
Sources: FDA drug label (DailyMed) FDA Adverse Event Reporting System (FAERS) ClinicalTrials.gov PubChem
Updated 2026-08-10