Eptifibatide_Dosage, benefits & legal status
Also known as Integrilin
A hospital antiplatelet drug that blocks the platelet fibrinogen receptor. FDA-approved since 1998; the Integrilin brand is gone, generics remain.
Common vial size is what vendors typically sell, not a recommendation. Enter your own vial in the calculator.
What is Eptifibatide?
Plain language first. The technical label stays, but it never stands alone.Overview
During a heart attack or a stent procedure, platelets pile onto the damaged artery. Given as a bolus then a drip, eptifibatide blocks more than 90% of platelet clumping and largely wears off within about 4 hours of stopping. In trials it cut death or heart attack modestly (14.2% against 15.7% in PURSUIT) at the cost of more bleeding, and it failed in stroke. The main trials predate today's antiplatelet tablets.
Eptifibatide is a cyclic heptapeptide (six amino acids plus a mercaptopropionyl unit) closed by a disulfide, with homoarginine-glycine-aspartate as its binding motif. It reversibly blocks the platelet receptor glycoprotein IIb/IIIa (integrin alphaIIb-beta3), the receptor fibrinogen uses to link platelets together. COR Therapeutics designed it from the lysine-glycine-aspartate motif of barbourin, a protein in the venom of the southeastern pygmy rattlesnake; no venom is used to make it.
What it's used for
A hospital-only intravenous drug for unstable angina or non-ST-elevation heart attack, and during angioplasty and stenting, given with aspirin and heparin.
How does Eptifibatide work?
What it does in the body, and where.Eptifibatide blocks the receptor platelets use to grab fibrinogen and stick together.
- 01The bridgeActivated platelets switch their glycoprotein IIb/IIIa receptors on. Fibrinogen binds them and bridges one platelet to the next, building a clot in a damaged artery.
- 02The decoyEptifibatide's homoarginine-glycine-aspartate loop mimics the sequence the receptor recognises, so it sits in the receptor instead. The lysine-like homoarginine, copied from barbourin, makes it selective for this platelet receptor.
- 03Quick offPlatelet clumping is inhibited by more than 90% at steady state. The block is reversible, the half-life is about 2.5 hours, and inhibition falls below 50% within 4 hours of stopping.
A schematic of the compound's mechanism, not a diagnostic image.
What else is it used for?
Each group carries its own evidence level.Approved means regulators have cleared it for that purpose. Investigational means it is in trials. Early research means it is being studied and is not established.
Unstable angina and heart attack
FDA-approved- Human trialPURSUIT, 10,948 patients: death or heart attack at 30 days 14.2% against 15.7%.
- No dataThe benefit was seen in men (odds ratio 0.8) but not in women (1.1).
Stenting
FDA-approved- Human trialESPRIT, 2,064 patients: death, heart attack or urgent repeat procedure at 48 hours 6.6% against 10.5%, and 7.5% against 11.7% at 30 days.
Timing
FDA-approved- Human trialEARLY-ACS, 9,492 patients: routine use before angiography was no better than use when needed (odds ratio 0.92) and caused more bleeding.
Stroke
tested-and-failed- Human trialMOST, 514 patients: added to clot-dissolving treatment it gave no benefit (posterior probability 0.04), with deaths at 90 days 12% against 8%.
It is not made from rattlesnake venom: it is fully synthetic, designed from the lysine-glycine-aspartate motif of the venom protein barbourin. 'Heptapeptide' means six amino acids plus a mercaptopropionyl unit, not seven amino acids. Its motif is homoarginine-glycine-aspartate, modelled on KGD rather than RGD. The Integrilin brand has been discontinued in the US, Canada and the EU; the drug survives as generics. IMPACT-II did not test today's dose, and neither of its doses was significant by intention to treat (only the lower one was, among treated patients); the current double-bolus regimen comes from ESPRIT. PURSUIT's benefit was modest (1.5 percentage points) and not seen in women. EARLY-ACS randomised 9,492, though the registry lists 9,406.
The published record
Papers and trials about Eptifibatide
373 papers tagged human · 258 not reviews or lab · 103 clinical trial publications
35 registered trials · 14 with posted results
Furthest stage reached: Approved in the US
Counted from Europe PMC indexing, not read by a person; a human tag can land on reviews, commentary or lab papers; clinical trial publications is the narrower count. 488 papers and 35 trials indexed in detail.
At a glance
Four things to know about Eptifibatide
Evidence
FDA-approved
Category
Healing and recovery
Common vial
Varies
Half-life
About 2.5 hours
How much, and do you cycle it?
The range, and whether you take breaks.180 mcg/kg bolus, then 2 mcg/kg/min (label), continuous infusion for up to 72 to 96 hours. One course per hospital episode FDA label
A bolus and infusion lasting hours to a few days around a heart attack or stent procedure, then stopped.
How long does it stay in the body?
The half-life, and where the figure comes from.About 2.5 hoursFDA label
Steady state in 4 to 6 hours. About half is cleared by the kidneys, so clearance halves when creatinine clearance is below 50 mL/min. About 25% is protein-bound, with no major metabolites.
Source: Integrilin US prescribing information, section 12.3
You can compare this against the whole library to see where it sits.
How is it given?
Dosing context and source notes.Acute coronary syndrome: 180 mcg/kg intravenous bolus, then 2 mcg/kg/min for up to 72 hours (up to 96 hours in all if angioplasty follows). Angioplasty: 180 mcg/kg bolus just before the procedure, a second 180 mcg/kg bolus 10 minutes later, and 2 mcg/kg/min for 18 to 24 hours. Creatinine clearance below 50 mL/min: infusion halved to 1 mcg/kg/min. Given with aspirin and heparin, in hospital only. Supplied as ready-made solutions (20 mg/10 mL, 75 mg/100 mL, 200 mg/100 mL), so there is nothing to mix.
How do you store it?
Before mixing, and after.Given in hospital or a trial clinic, so the pharmacy stores it.
Eptifibatide goes into a vein and is prepared by hospital, clinic or trial pharmacy staff, following the product label or the trial protocol. Some products like this are ready-made solutions and others are powders mixed just before use, often with hours rather than weeks of shelf life once prepared. It is not a medicine people store at home.
What are the side effects and cautions?
Known cautions and warnings for this compound.Solubility, computed: 57% charged residues, 57% hydrophobic. Water usually sufficient.
A first-pass rule from peptide manufacturers' guidance. It does not account for disulfide bridges, salt form or how the powder was dried, and it predicts what should be easy rather than what will happen in your vial.
Who should avoid it
- Bleeding problems, or abnormal bleeding in the past 30 days
- Severely high blood pressure (above 200/110 mmHg) that is not controlled
- Major surgery in the past 6 weeks
- Stroke in the past 30 days, or any past bleeding stroke
- Dialysis, or use of another intravenous IIb/IIIa blocker
Stop and get help
- Any serious bleeding, including blood in urine or stool, vomiting blood or a sudden severe headache
- A sharp fall in platelet count (below 100,000 per microlitre): eptifibatide and heparin are stopped
Common effects
- Major bleeding 10.8% against 9.3% on placebo, and minor bleeding 13.1% against 7.6% (PURSUIT)
- In elective stenting (ESPRIT): major bleeding 1.3% against 0.4%, transfusion 1.5% against 1.1%
- Stopped because of bleeding in 8% against 1% (PURSUIT)
- Low platelets 1.2% against 0.6% (ESPRIT); low blood pressure 7% against 6% (PURSUIT)
Where this page says nothing is established, that means nobody has studied it, not that a compound is safe.
Is Eptifibatide approved?
And where the numbers on this page come from.Yes. Eptifibatide is FDA approved and available on prescription in the United States. It is also approved in the European Union.
- Approval statusFDA-approved
- RouteInto a vein (bolus, then infusion)
- Checked15 October 2026
- Approved outside the USEuropean Union: EU authorisation of Integrilin on 1 July 1999, withdrawn from 1 January 2026; the generic Eptifibatide Accord has been authorised since 11 January 2016. Canada's Integrilin infusion was discontinued in October 2022. Also approved in the US, where it is sold as generics.This does not change the United States position above.
- DoseFrom the drug label. The manufacturer tested this range and a regulator reviewed it.
- Vial sizeFrom what vendors typically list; not a recommendation.
- SourcesIntegrilin US prescribing information (2021)Drugs@FDA, NDA 020718FDA GSRS substance record, eptifibatide (UNII NA8320J834)EMA, Integrilin EPAREMA, Integrilin supply DHPC (2 Nov 2023)EMA, Eptifibatide Accord EPARPURSUIT Trial Investigators, New England Journal of Medicine 1998;339:436-443IMPACT-II Investigators, Lancet 1997;349:1422-1428ESPRIT Investigators, Lancet 2000;356:2037-2044Giugliano RP et al., New England Journal of Medicine 2009;360:2176-2190 (EARLY-ACS)Adeoye O et al., New England Journal of Medicine 2024;391:810-820 (MOST)Scarborough RM et al., Journal of Biological Chemistry 1991;266:9359-9362Drug Shortages Canada, Integrilin discontinuationDailyMed, eptifibatide labels
What has happened recently
FDA-approved on 18 May 1998 (NDA 020718, priority review) as Integrilin, for acute coronary syndrome and for angioplasty; the double-bolus regimen came from ESPRIT in 2001. Merck holds the application, and both Integrilin strengths are now listed as discontinued in the US, not for safety or effectiveness reasons. Generics have been sold since 2015, and at least 10 companies list it on DailyMed. In the EU, Integrilin was authorised on 1 July 1999 and withdrawn from 1 January 2026 at the holder's request for commercial reasons, after supply stopped in late 2023 because of a problem with the active ingredient; the generic Eptifibatide Accord, authorised in January 2016, remains. Canada's Integrilin infusion was discontinued in October 2022.
You can compare this against the whole library, or read how to check a seller.
What else is like Eptifibatide?
Others in Healing and recovery, side by side.If you're weighing Eptifibatide, it's worth reading Linaclotide (Linzess), Nerinetide (NA-1), and Pentosan Polysulfate (PPS) in the same class.
A hospital antiplatelet drug that blocks the platelet fibrinogen receptor. FDA-approved since 1998; the Integrilin brand is gone, generics remain.
- Dose
- 180 mcg/kg bolus, then 2 mcg/kg/min (label)
- How often
- Continuous infusion for up to 72 to 96 hours
An approved oral peptide for constipation that works in the gut and barely reaches the blood.
- Dose
- 72, 145 or 290 mcg once daily (label)
- How often
- Once daily
A 20-residue peptide built to stop nerve cells dying during a stroke. Over 2,400 patients later, the main results are neutral.
- Dose
- 2.6 mg/kg once, up to 270 mg (trials)
- How often
- A single dose
A treatment for arthritis and painful bladder that acts like a joint lubricant.
- Dose
- 300 mg per day (100 mg three times a day)
- How often
- Three times a day (oral)
Guides for this compound
- How to Reconstitute a Peptide
Mix peptide powder with bacteriostatic water, step by step.
- How to Read an Insulin Syringe
Read the units, convert to millilitres, and draw the exact dose.
- mcg vs mg: The Peptide Dosing Mistake to Avoid
Your vial says mg and your protocol says mcg. Here is the conversion and how to check it.
Sources
- Integrilin US prescribing information (2021)(2021)Structure, dosing and kidney adjustment; half-life about 2.5 hours; PURSUIT, IMPACT-II and ESPRIT results and bleeding tables.
- Drugs@FDA, NDA 020718(2026)Approved 18 May 1998 with priority review; both Integrilin strengths discontinued; held by Merck.
- FDA GSRS substance record, eptifibatide (UNII NA8320J834)(2026)C35H49N11O9S2, MW 832; CAS 188627-80-7; structure with five L stereocentres.
- EMA, Integrilin EPAR(2026)EU authorisation 1 July 1999; withdrawn from 1 January 2026.
- EMA, Integrilin supply DHPC (2 Nov 2023)(2023)Supply stopped immediately because of a problem with the active ingredient, bringing forward a discontinuation planned for the end of 2024; not for safety or effectiveness reasons.
- EMA, Eptifibatide Accord EPAR(2026)EU generic authorised 11 January 2016 and still authorised.
- PURSUIT Trial Investigators, New England Journal of Medicine 1998;339:436-443(1998)10,948 patients: death or heart attack at 30 days 14.2% against 15.7% (P=0.04); no benefit seen in women.
- IMPACT-II Investigators, Lancet 1997;349:1422-1428(1997)4,010 angioplasty patients at lower doses than today: by intention to treat 9.2% and 9.9% against 11.4%, neither significant; among treated patients 9.1% (significant) and 10.0% against 11.6%.
- ESPRIT Investigators, Lancet 2000;356:2037-2044(2000)2,064 stent patients: 6.6% against 10.5% at 48 hours with the double-bolus regimen.
- Giugliano RP et al., New England Journal of Medicine 2009;360:2176-2190 (EARLY-ACS)(2009)9,492 patients: routine early use no better than delayed use as needed (9.3% against 10.0%), with more bleeding.
- Adeoye O et al., New England Journal of Medicine 2024;391:810-820 (MOST)(2024)514 stroke patients: no benefit added to thrombolysis; deaths 12% against 8%; stopped for futility.
- Scarborough RM et al., Journal of Biological Chemistry 1991;266:9359-9362(1991)Barbourin, a rattlesnake venom disintegrin with a KGD motif specific for glycoprotein IIb/IIIa.
- Drug Shortages Canada, Integrilin discontinuation(2022)Merck Canada discontinued the 0.75 mg/mL Integrilin infusion on 17 October 2022 for business reasons.
- DailyMed, eptifibatide labels(2026)Generic labels from about 10 companies; none under the Integrilin name.
Beyond these, 523 records are indexed. Browse the records