Evidence Grade A — Regulatory approved. 1069 published studies. 35 registered clinical trials.
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Eptifibatide (sold as Integrilin) is a hospital anti-clotting medication given through an IV during heart attacks and coronary stenting procedures. Derived from a protein found in pygmy rattlesnake venom, it blocks the final step in blood clot formation — the linking of platelets to each other. Its effects wear off within hours of stopping the infusion.
Eptifibatide is also known by these brand and alternate names:
1,069 published studies: 878 human, 45 animal, 94 in-vitro, 233 reviews
Eptifibatide is marketed as Integrilin (approved 1998). It is indicated for acute coronary syndrome and percutaneous coronary intervention (stenting). Administered as an intravenous bolus followed by continuous infusion for up to 72 hours.
In the PURSUIT trial involving nearly 11,000 patients with acute coronary syndrome, eptifibatide reduced the combined rate of death and heart attack. However, the use of GPIIb/IIIa inhibitors has declined significantly with the widespread adoption of newer oral anti-platelet agents like ticagrelor and prasugrel, and improvements in stent technology. Eptifibatide remains available and is still used selectively, particularly during complex coronary interventions where additional anti-platelet protection is needed.
When a blood vessel is damaged (or a stent is placed), platelets rush to the site and link together via a receptor on their surface called GPIIb/IIIa, which grabs fibrinogen molecules to form bridges between platelets — this is the final common step in clot formation. Eptifibatide blocks this receptor, preventing platelets from linking together regardless of what triggered them to activate. Because it blocks the very last step, it is one of the most powerful anti-platelet agents available. Its effects wear off within hours of stopping the infusion.
The PURSUIT trial, involving nearly 11,000 patients with acute coronary syndrome, showed eptifibatide reduced the combined rate of death and heart attack. During the era of bare-metal stents, drugs like eptifibatide were a transformative advance in interventional cardiology. However, clinical use has declined substantially. Newer oral anti-platelet drugs (ticagrelor, prasugrel) and improvements in stent technology (drug-eluting stents) have reduced the need for IV anti-platelet infusions in most situations. Eptifibatide is still available and used selectively during complex coronary interventions where extra anti-platelet protection is needed, but it is no longer a routine part of cardiac care. Generic versions are available.
PeptideTrace tracks 35 registered clinical trials for Eptifibatide sourced from ClinicalTrials.gov.
Eptifibatide for Extended Window Ischemic Stroke After Thrombolysis
Platelet Function in Patients With Ischemic Stroke Treated With Anti-thrombotic or Thrombolytic
Multi-arm Optimization of Stroke Thrombolysis
Eptifibatide in Endovascular Treatment of Acute Ischemic Stroke (EPOCH)
Pharmacologic Treatment of Myocardial Ischemia Detected by Intracoronary ECG
FDA ORIG 1
EMA Marketing Authorisation
FDA ORIG 1
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FDA ORIG 1
FDA SUPPL 1
FDA SUPPL 6
FDA SUPPL 4
FDA ORIG 1
Health Canada Market Authorisation
FDA SUPPL 2
FDA SUPPL 4
FDA SUPPL 1
Eptifibatide is a cyclic heptapeptide (6 amino acids plus a mercaptopropionyl group forming the ring) designed as a platelet glycoprotein IIb/IIIa receptor antagonist. It was derived from barbourin, a disintegrin peptide found in the venom of the southeastern pygmy rattlesnake (Sistrurus miliarius barbouri).
Eptifibatide reversibly binds the GPIIb/IIIa receptor (integrin αIIbβ3) on activated platelets, blocking the final common pathway of platelet aggregation by preventing fibrinogen binding and platelet cross-linking. The KGD (Lys-Gly-Asp) recognition sequence (rather than the more common RGD) provides selectivity for GPIIb/IIIa over other integrins. Half-life is approximately 2.5 hours. Administered IV only with rapid onset and offset.
Eptifibatide is marketed as Integrilin (approved 1998). Indicated for acute coronary syndrome (ACS) and percutaneous coronary intervention (PCI). The PURSUIT trial (N=10,948; ACS) showed a reduction in death/MI at 30 days: 14.2% versus 15.7% (P=0.04; 1.5% ARR). The ESPRIT trial (N=2,064; PCI/stenting) demonstrated a 37% RRR in the primary composite: 6.6% versus 10.5% (P=0.0015; stopped early for efficacy). Major bleeding is the primary safety concern.
Linaclotide is marketed as Linzess (approved August 2012). It is taken as a daily oral capsule on an empty stomach, at least 30 minutes before the first meal. The recommended dose is 290 mcg for IBS-C and 72 or 145 mcg for chronic constipation. In clinical trials, approximately 34% of IBS-C patients met the composite improvement endpoint compared to 17% on placebo. Diarrhoea is the most common side effect (approximately 20%) and the leading reason for discontinuation. Linaclotide has a boxed warning against use in children under 6 years due to deaths in young mice, though no such events have been reported in humans. It competes with plecanatide (which targets the same pathway) and other IBS-C treatments.
Elamipretide (Forzinity) was approved by the FDA for Barth syndrome based on the TAZPOWER trial. The randomised crossover phase (12 patients) did not meet its primary endpoints, but the open-label extension (168 weeks) demonstrated durable improvements in walking distance and muscle strength that formed the basis for approval. Barth syndrome affects approximately 1 in 300,000–400,000 births. A larger Phase III trial in primary mitochondrial myopathy (218 patients, MMPOWER-3) did not meet its primary endpoint, and the drug was not approved for that broader indication. Elamipretide remains approved exclusively for Barth syndrome. See also SS-31 (#158) for the research compound context.
Glucagon has been available as an emergency injection since the 1960s and remains the standard rescue treatment for severe hypoglycaemia. Recent innovation has focused on making it easier to administer in emergencies. Baqsimi, approved in 2019, was the first needle-free option as a nasal powder. Gvoke, also approved in 2019, eliminated the need to mix and reconstitute the medication before injection — a significant advance since severe hypoglycaemia often impairs the ability to follow complex preparation steps. Dasiglucagon (Zegalogue), a next-generation stable liquid glucagon approved in 2021, further improved on the convenience of rescue administration. Beyond emergency rescue, glucagon's receptor is now a major research target — dual and triple agonists combining glucagon receptor activity with GLP-1 (such as survodutide and retatrutide) are in advanced clinical trials for obesity and metabolic disease.
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