188627-80-7

Description

Eptifibatide is a synthetic cyclic heptapeptide composed of six amino acids and one mercaptopropionyl residue. It is designed to selectively and reversibly bind to the platelet receptor glycoprotein (GP) IIb/IIIa, inhibiting platelet aggregation by blocking the binding of fibrinogen, von Willebrand factor, and other adhesive ligands. This binding prevents thrombus development, making it effective in reducing the risk of acute cardiac ischemic events. Eptifibatide is used in the treatment of acute coronary syndrome (ACS) and percutaneous coronary intervention (PCI), often in combination with aspirin or clopidogrel and heparin.

Originator

Cor Therapeutics (US)

Uses

Manufactured through solution-phase peptide synthesis and purified by preparative reverse-phase liquid chromatography and lyophilization, eptifibatide is a cyclic heptapeptide with anticoagulant activity. Despite its efficacy, it has a short half-life, necessitating improvements in delivery systems. Nano-liposomes may be employed to enhance the protected and targeted delivery of antithrombotic agents like eptifibatide to the site of thrombus.

Definition

ChEBI: Eptifibatide is a synthetic homodetic cyclic peptide comprising N(alpha)-(3-sulfanylpropanoyl)homoarginyl, glycyl, aspartyl, tryptophyl, prolyl and cysteinamide residues connected in sequence and cyclised via a disulfide bond. Derived from a protein found in the venom of the southeastern pygmy rattlesnake, Sistrurus miliarus barbouri, eptifibatide is an anti-coagulant that inhibits platelet aggregation by selectively blocking the platelet glycoprotein IIb/IIIa receptor, so preventing the binding of fibrinogen, von Willebrand factor, and other adhesive ligands. It is used in the management of unstable angina and in patients undergoing coronary angioplasty and stenting procedures. It has a role as a platelet aggregation inhibitor and an anticoagulant. It is an organic disulfide, a macrocycle and a homodetic cyclic peptide.

Brand name

Integrilin

Clinical Use

As a GPIIb/IIIa receptor antagonist, eptifibatide is derived from the natural product barbourin, found in the venom of a pygmy rattlesnake. Its structure includes the RGD sequence, allowing it to bind to the RGD receptor on platelets, blocking their ability to bind with fibrinogen. This makes eptifibatide valuable in the treatment of unstable angina and angioplastic coronary interventions.