Eptifibatide

Integrilin, SB-1, Sch 60936

Cardiovascular & circulation

Awaiting medical reviewEN ES DE FR PT ZH+ Follow for updates

Note on this profile. Eptifibatide is an approved hospital-only antiplatelet medicine given by intravenous infusion in acute coronary syndromes and during stenting. It has no research-chemical or community use. This page explains the published science.

1What it is

Eptifibatide is a small ring-shaped peptide designed in the early 1990s by COR Therapeutics from barbourin, a disintegrin protein in the venom of the south-eastern pygmy rattlesnake (Sistrurus miliarius barbouri). Most disintegrins use an Arg-Gly-Asp (RGD) sequence to block integrins broadly; barbourin uses Lys-Gly-Asp (KGD), which is far more selective for the platelet integrin αIIbβ3 (glycoprotein IIb/IIIa). Eptifibatide packages that KGD motif into a seven-residue ring with a modified arginine-like residue (homoarginine) and a mercaptopropionyl cap, which makes it potent, selective and resistant to breakdown in plasma.

It was approved by the FDA in 1998 and is one of three "GP IIb/IIIa inhibitors" (with abciximab, an antibody fragment now largely withdrawn, and tirofiban, a non-peptide). Its use has declined since potent oral P2Y12 inhibitors became standard, but it remains in guidelines as a bail-out or bridging drug.

2How it's thought to work

Activated platelets expose about 50,000–80,000 copies of GP IIb/IIIa, which bind fibrinogen and von Willebrand factor to form the platelet plug. Eptifibatide binds the same site competitively and reversibly, blocking aggregation by more than 80% at approved doses regardless of what activated the platelet.

Because binding is reversible and the short, platelet function returns within hours of stopping — useful if urgent surgery is needed, and the reason bleeding is manageable.

It is cleared mainly by the kidneys (about 50%), so the infusion is reduced in renal impairment and the drug is contraindicated in patients on dialysis.

A cyclic peptide blocking the glycoprotein IIb/IIIa receptor on platelets — the final common step of aggregation. Fibrinogen can no longer bridge one platelet to the next, so a clot cannot build however the platelets were activated.Schematic — not to scale

3What the research shows

Non-ST-elevation acute coronary syndromes

PURSUIT (n=10,948) reported a reduction in death or MI at 30 days from 15.7% to 14.2% with eptifibatide added to aspirin and heparin, at the cost of more bleeding (PURSUIT Trial Investigators 1998, NEJM). This remains the largest trial of any GP IIb/IIIa inhibitor. [2]

Coronary stenting

ESPRIT (n=2,064) found the double-bolus regimen cut death, MI or urgent revascularisation at 48 h from 10.5% to 6.6% in planned stenting (ESPRIT Investigators 2000, Lancet). IMPACT-II (n=4,010) used a lower dose and showed a smaller, borderline effect (IMPACT-II Investigators 1997, Lancet), which is why the dose was raised. [3][4]

Graded A (negative for routine early use)

Early routine vs delayed provisional use

EARLY ACS (n=9,492) found no benefit from starting eptifibatide routinely before angiography versus giving it only when needed in the cath lab, with more bleeding in the early group (Giugliano 2009, NEJM). Guidelines since recommend selective rather than routine use. [5]

Comparison with bivalirudin

In ACUITY and REPLACE-2, heparin plus GP IIb/IIIa inhibitor (often eptifibatide) produced similar ischaemic outcomes but more bleeding than bivalirudin alone (see profile 131).

Graded B/A

Stroke thrombolysis adjunct

CLEAR-ER and related trials tested eptifibatide with low-dose alteplase in acute ischaemic stroke; safety was acceptable and efficacy signals modest (Pancioli 2013, Stroke). The MOST trial (2024) found no benefit from adding eptifibatide or argatroban to thrombolysis (Adeoye 2024, NEJM) †. [6]

Community / self-directed use

None documented.

4Reported side effects and interactions

Literature-reported

Bleeding (major bleeding roughly 1–3% above comparator in trials, mostly at vascular access sites); hypotension; thrombocytopenia, usually mild but occasionally acute and profound (<0.5%), far rarer than with abciximab; rare pseudothrombocytopenia (a laboratory artefact, which is why a repeat count in a citrate tube is recommended).

Community-reported

none; no community use.

Theoretical. no antidote; platelet transfusion is of limited use while drug circulates because transfused platelets are also blocked, but the short limits the problem.

Interactions. additive bleeding with heparin, bivalirudin, thrombolytics, oral anticoagulants, NSAIDs and antiplatelets. No metabolic (CYP) interactions. Contraindicated in dialysis-dependent patients, platelets <100,000/µL, recent major bleeding or stroke, and severe uncontrolled hypertension.

Markers researchers commonly monitor

These follow the label:

Marker	Why it's watched
Platelet count	baseline, within 6 h of starting, then at least daily; an acute fall is the signal to stop the drug and repeat the count in a citrate tube to exclude clumping artefact.
Haemoglobin / haematocrit	bleeding surveillance, especially at access sites.
Creatinine / creatinine clearance	determines the infusion rate; dialysis is a contraindication.
aPTT or ACT	for the heparin given alongside; eptifibatide itself does not change them, but the target ACT during PCI is lowered when a GP IIb/IIIa inhibitor is on board.
Blood pressure	hypotension is reported.

Free for everyone. Safety information is never behind a paywall.

5Reconstitution and handling

Supplied as ready-to-use solution (2 mg/mL vial for bolus; 0.75 mg/mL vial for infusion); no . Given undiluted by weight-based bolus and infusion pump. Hospital use only; the calculator is not applicable.

6Commonly studied alongside

Aspirin, unfractionated heparin or enoxaparin, clopidogrel/ticagrelor/prasugrel as background in every trial; bivalirudin (profile 131) as the main comparator strategy; alteplase in stroke trials; tirofiban and abciximab as class comparators.

Informational cross-links. Not stack recommendations.

7Regulatory status by region

Region	Status (checked —)
United States	FDA-approved (Integrilin, 1998) for ACS and PCI; generics available
European Union	Authorised (Integrilin, 1999, centralised procedure) for non-ST-elevation ACS in patients with chest pain within 24 h; generics authorised †
United Kingdom	MHRA-licensed (Integrilin and generics); hospital only
Australia	TGA-registered (Integrilin) †
South Africa	Registered with SAHPRA †
Sport	Not prohibited by WADA

8Open questions

What role remains for GP IIb/IIIa inhibitors now that ticagrelor, prasugrel and cangrelor are available? Most current use is bail-out for thrombotic complications.
Whether intracoronary or shortened-infusion regimens preserve efficacy with less bleeding.
Role as a thrombolysis adjunct in stroke after the neutral MOST result.

9References

1Scarborough RM et al. (1993). Design of potent and specific integrin antagonists: peptide antagonists with high specificity for glycoprotein IIb-IIIa. J Biol Chem. PubMed
2PURSUIT Trial Investigators (1998). Inhibition of platelet glycoprotein IIb/IIIa with eptifibatide in patients with acute coronary syndromes. NEJM. PubMed
3ESPRIT Investigators (2000). Novel dosing regimen of eptifibatide in planned coronary stent implantation (ESPRIT): a randomised, placebo-controlled trial. Lancet. PubMed
4IMPACT-II Investigators (1997). Randomised placebo-controlled trial of effect of eptifibatide on complications of percutaneous coronary intervention. Lancet. PubMed
5Giugliano RP et al. (2009). Early versus delayed, provisional eptifibatide in acute coronary syndromes (EARLY ACS). NEJM. PubMed · DOI
6Pancioli AM et al. (2013). Combined approach to lysis utilizing eptifibatide and recombinant tissue plasminogen activator in acute ischemic stroke — enhanced regimen (CLEAR-ER). Stroke. PubMed · DOI
7Integrilin (eptifibatide) prescribing information / Summary of Product Characteristics (current). PubMed

References are being resolved to PubMed/DOI identifiers; links search PubMed for the citation until then.

† Being confirmed by our reviewers against current sources.

10Community

forum threads →

community protocols include this →

Threads and protocols are visible to members. Joining is free.

Self-reported side effects Phase 2

Not enough data yet. 0 of the 50 members needed have logged this compound for 4+ weeks. We don't show anything below 50, so no one can be identified.

11Page history

30 Oct 2026Profile published — awaiting medical review

Licensed CC BY-NC-SA 4.0. Found an error? Report it · Editorial standards — corrections are logged here.