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188627-80-7NC(=O)[C@@H]1CSSCCC(=O)N[C@@H](CCCCN=C(N)N)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N2CCC[C@H]2C(=O)N1CZKPOZZJODAYPZ-LROMGURASA-N188627-80-7DTXSID7046673CHEMBL1174CHEBI:291902Sicherheitsangaben dienen nur zur Orientierung und ersetzen weder das Sicherheitsdatenblatt (SDB) des Lieferanten noch geltende Vorschriften oder eine fachliche Bewertung.
BeschreibungEptifibatide is a reversible antagonist of the glycoprotein llb/llla complex, a specific platelet adhesion receptor that plays a central role in the cascade of thrombus formation by allowing mediators such as fibrinogen or von Willbrand factor to cross-link adjacent platelets and to give rise to aggregation. In diverse animal experimental models of arterial thrombosis, treatment with Eptifibatide resulted in an enhanced lysis of occlusive thrombus and a restoration of arterial blood flow. In clinical trials involving patients with acute coronary syndromes, Eptifibatide demonstrated a significant decrease in the incidence of death or nonfatal myocardial infarction at 30 days. In other trials in patients undergoing percutaneous coronary intervention (PCI), it showed a positive trend. Eptifibatide has the advantage of being short acting, its antiplatelet effect being rapidly reversible.
VerwendenEptifibatide is a cyclical heptapeptide with anticoagulant activity. Eptifibatide selectively and reversibly binds to and blocks the platelet glycoprotein IIb/IIIa receptor. This prevents the binding of fibrinogen, von Willebrand factor, and other adhesive ligands and leads to an inhibition of platelet aggregation and prevents thrombus development. It is an efficient peptide drug to reduce the risk of cardiac ischemic events, however has a short half-life. Therefore, antithrombotic agents like eptifibatide are required to become improved with a protected and targeted delivery system such as using nano-liposomes to the site of thrombus.
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DefinitionChEBI: 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.