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Bivalirudin (Angiomax): how it works, uses and side effects

Clinical review pending

Bivalirudin inhibits blood clotting during catheter-based procedures on coronary arteries. How it works, what HORIZONS-AMI found, and its bleeding and thrombosis risks.

Bivalirudin inhibits blood clotting during catheter-based procedures on the coronary arteries. It is intended to prevent clots from forming during treatment. The hospital team gives it directly into a vein and monitors its effect. Bleeding is the main risk.

What is bivalirudin?

Bivalirudin is a synthetic peptide: a chain of 20 amino acids. It inhibits blood clotting, making it an anticoagulant. More specifically, it is a direct thrombin inhibitor [1]. It binds to the enzyme thrombin and blocks its role in clot formation. The chemically manufactured medicine is known by the brand name Angiomax and, outside the US, also as Angiox. Which products are available depends on the country.

Bivalirudin is given only intravenously in a hospital, usually in a cardiac catheterization laboratory. It is not intended to be taken by mouth or used at home.

The history of bivalirudin

Bivalirudin’s inspiration came from the medicinal leech. The leech produces hirudin [2], a naturally occurring anticoagulant protein that prevents blood from clotting while it feeds. Hirudin became the model for a group of direct thrombin inhibitors. Bivalirudin is a short, synthetic version that binds to two sites on thrombin at once, a property described as “bivalent.”

Bivalirudin was developed as an alternative to heparin for cardiac procedures, with the aim of making its effect more predictable and shorter-lasting. The US Food and Drug Administration approved it in 2000. Unlike the leech protein on which it is based, bivalirudin produces inhibition that is reversible and short-lived. This makes it easier to use during angioplasty, a procedure that widens narrowed blood vessels.

How does bivalirudin work?

Thrombin converts fibrinogen into fibrin, forming a mesh that holds a blood clot together. It also activates platelets. Bivalirudin binds directly to the enzyme and inhibits both processes.

As a bivalent inhibitor [1], bivalirudin occupies two sites on thrombin. One end binds to the active site, where the enzyme does its chemical work. The other binds to exosite 1, a docking site for fibrinogen. Bivalirudin thereby inhibits both thrombin circulating freely in the blood and thrombin already bound within a clot. Heparin is less effective at inhibiting the latter.

Thrombin slowly cleaves the bound medicine and regains its function. Once the infusion stops, the anticoagulant effect wears off. This helps the treatment team control its effect during the procedure. The approximately 25 minutes [1] cited in this context should not, however, be taken as an established point at which anticoagulation has ended.

In the HORIZONS-AMI trial [3], 3,602 people underwent angioplasty for a heart attack. Within 30 days, those receiving bivalirudin alone had fewer major bleeds and fewer deaths from cardiac, or heart-related, causes than those receiving heparin together with a glycoprotein IIb/IIIa inhibitor. This inhibitor acts on platelets. The comparison therefore concerns that combination and cannot automatically be applied to every treatment involving heparin. At the same time, bivalirudin was associated with a higher risk of a clot forming at the stent within the first 24 hours. The side-effects section below explains more.

Outcome in HORIZONS-AMI Bivalirudin alone Heparin plus a glycoprotein IIb/IIIa inhibitor
Major bleeding within 30 days 4.9% 8.3%
Deaths from cardiac causes 1.8% 2.9%

Is bivalirudin FDA-approved?

Yes. The FDA approved bivalirudin (Angiomax) in 2000 [1] for anticoagulation during coronary angioplasty, which widens narrowed coronary arteries. The prescribing information later also covered people undergoing percutaneous coronary intervention (PCI), a catheter-based coronary procedure, who have or are at risk of heparin-induced thrombocytopenia. This is an immune reaction to heparin. These approval statements concern the US.

What is bivalirudin prescribed for?

Bivalirudin is intended to prevent clots from forming on the catheter or at the newly treated part of the vessel during percutaneous coronary intervention (PCI). These procedures include angioplasty and stent placement, used to open narrowed or blocked coronary arteries.

For people with heparin-induced thrombocytopenia (HIT) [1], a serious immune reaction to heparin, bivalirudin offers a way to provide anticoagulation without heparin. The medical team administers the medicine and monitors treatment. It is not intended for self-administration.

What side effects can occur?

Bleeding is the main risk of bivalirudin, as it is with other anticoagulants. In trials, major bleeding occurred less often with bivalirudin than with certain heparin-based treatments. In the HORIZONS-AMI trial described above, the specific comparison was with heparin plus a glycoprotein IIb/IIIa inhibitor.

The following symptoms were also reported during treatment:

In the HORIZONS-AMI trial [3], acute stent thrombosis occurred more often with bivalirudin during the first 24 hours. This means a clot forms at the newly implanted stent. No difference was reported over the 30-day period; the precise meaning of that finding remains unclear without establishing which endpoint was measured. Adequate treatment with medicines that inhibit platelets is part of managing this risk. This does not establish that such treatment completely prevents the increased early risk.

During treatment in the hospital, the medical team monitors the effect and controls the dose.