Title: Eptifibatide
CAS Registry Number: 188627-80-7
CAS Name: N6-(Aminoiminomethyl)-
N2-(3-mercapto-1-oxopropyl)-L-lysylglycyl-L-a-aspartyl-L-tryptophyl-L-prolyl-L-cysteinamide, cyclic (1?6)-disulfide
Trademarks: Integrilin (COR)
Molecular Formula: C35H49N11O9S2
Molecular Weight: 831.96
Percent Composition: C 50.53%, H 5.94%, N 18.52%, O 17.31%, S 7.71%
Literature References: Fibrinogen receptor antagonist. Specifically inhibits fibrinogen binding to the platelet integrin GPIIb-IIIa which prevents platelet aggregation and subsequent clot formation. Synthetic, disulfide-linked cyclic heptapeptide based on
barbourin, a specific GPIIb-IIIa antagonist isolated from venom of the southeastern pigmy rattlesnake,
Sistrurus m. barbouri. Contains the Lys-Gly-Asp (KGD) amino acid sequence, a modification of the Arg-Gly-Asp (RGD) recognition site which appears to confer specificity: R. M. Scarborough
et al., J. Biol. Chem. 266, 9359 (1991). Design and structure-activity study of integrin antagonists:
eidem, ibid. 268, 1066 (1993). Prepn: R. M. Scarborough
et al., US 5686570 (1997 to COR Therapeutics). Pharmacology: F. A. Nicolini
et al., Circulation 89, 1802 (1994); K. Uthoff
et al., ibid. 90, pt 2, II-269 (1994). Clinical trial in patients undergoing percutaneous cardiovascular intervention: IMPACT-II Investigators,
Lancet 349, 1422 (1997). Clinical trial in acute coronary syndromes: PURSUIT Trial Investigators,
N. Engl. J. Med. 339, 436 (1998).
Therap-Cat: Antithrombotic.
Keywords: Antithrombotic.
