Heart & blood GPIIb/IIIa inhibitor
Eptifibatide
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This is not medical or legal advice, and we do not publish dosing, sourcing or reconstitution information.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.
If you think you are having a medical emergency, call 911.
Key takeaway
Eptifibatide (sold as Integrilin) is a small cyclic peptide, modeled on a molecule from rattlesnake venom, that blocks the final step of platelet clumping to prevent dangerous clots during heart attacks and stenting. It is given intravenously in acute coronary syndrome and during coronary procedures. It has been FDA-approved in the U.S. since 1998, and its main risk is bleeding.
At a glance
- What it is
- A platelet glycoprotein IIb/IIIa receptor antagonist, a cyclic heptapeptide antiplatelet drug
- Approved for
- Acute coronary syndrome and patients undergoing percutaneous coronary intervention (PCI)
- Key fact
- In the PURSUIT trial it reduced death or heart attack at 30 days in acute coronary syndrome
- Route
- Intravenous (bolus plus infusion)
- Evidence strength
- FDA approved
Summary
Eptifibatide (Integrilin) is an intravenous peptide that blocks platelet clumping during heart attacks and stenting. Learn how it works and its bleeding risk.
What is eptifibatide?
Eptifibatide, sold under the brand Integrilin, is a cyclic seven-amino-acid peptide antiplatelet drug. Its design was inspired by a protein in the venom of the pygmy rattlesnake that interferes with platelet clumping, and it carries a specific sequence that lets it block the platelet receptor responsible for aggregation. It is used in heart attacks and during coronary stenting to prevent clots. It was approved in the United States in 1998.
How does eptifibatide work?
Eptifibatide blocks the glycoprotein IIb/IIIa receptor on platelets, the receptor that represents the final common step in platelet aggregation. Normally, when platelets are activated, this receptor binds fibrinogen and links platelets together into a clot. Eptifibatide occupies the receptor and prevents that cross-linking, so platelets cannot aggregate even if they have been activated. The effect is potent but rapidly reversible once the infusion stops, because the drug binds the receptor reversibly.
That makes it useful in the acute setting of a heart attack or a coronary stent procedure, where fresh clot formation on a disrupted plaque or a new stent is the danger. In the PURSUIT trial, eptifibatide reduced the combined rate of death or nonfatal heart attack at 30 days in acute coronary syndrome, at the cost of more bleeding. It is cleared by the kidneys, so dosing is reduced in kidney impairment.
Is it FDA-approved?
Editor’s note
Status: Yes. Eptifibatide was approved by the FDA in 1998 for acute coronary syndrome, including patients managed medically and those undergoing percutaneous coronary intervention. It is given intravenously as a bolus followed by an infusion.
Category: FDA-approved · Primary body area: Heart & blood
Yes. Eptifibatide was approved by the FDA in 1998 for acute coronary syndrome, including patients managed medically and those undergoing percutaneous coronary intervention. It is given intravenously as a bolus followed by an infusion.
What is eptifibatide prescribed for?
Eptifibatide is prescribed for acute coronary syndrome (unstable angina or non-ST-elevation heart attack) and for patients undergoing percutaneous coronary intervention, to reduce clot-related complications. It is used in the hospital alongside other antithrombotic therapy.
What are the side effects?
Common side effects include:
- Bleeding, especially at the vascular access site
- Low blood pressure
More serious considerations include:
- Major hemorrhage, the principal risk
- Low platelet count (thrombocytopenia)
The prescribing information lists these effects and also contraindicates eptifibatide in people with active or recent serious bleeding, severe uncontrolled high blood pressure, or dialysis-dependent kidney failure, among other conditions.
Sources: FDA prescribing information for Integrilin; the PURSUIT trial (New England Journal of Medicine, 1998, DOI: 10.1056/NEJM199808133390704); and the original description of the rattlesnake venom peptide barbourin (Scarborough et al., Journal of Biological Chemistry, 1991, PMID: 2033037), both indexed on PubMed. This document is educational and does not constitute medical advice.
Registered human trials
0 registered human trials on ClinicalTrials.gov that we reviewed
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