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Titolo:
CLINICAL-PHARMACOLOGY OF EPTIFIBATIDE
Autore:
PHILLIPS DR; SCARBOROUGH RM;
Indirizzi:
COR THERAPEUT INC,256 E GRAND AVE S SAN FRANCISCO CA 94080
Titolo Testata:
The American journal of cardiology
fascicolo: 4A, volume: 80, anno: 1997,
pagine: 11 - 20
SICI:
0002-9149(1997)80:4A<11:COE>2.0.ZU;2-L
Fonte:
ISI
Lingua:
ENG
Soggetto:
PLATELET GLYCOPROTEIN IIB/IIIA; ISCHEMIC-HEART-DISEASE; IIB-IIIA COMPLEX; ARG-GLY-ASP; CORONARY INTERVENTION; UNSTABLE ANGINA; GPIIB-IIIA; MEMBRANE-GLYCOPROTEINS; MYOCARDIAL-INFARCTION; INTEGRIN RECEPTOR;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
70
Recensione:
Indirizzi per estratti:
Citazione:
D.R. Phillips e R.M. Scarborough, "CLINICAL-PHARMACOLOGY OF EPTIFIBATIDE", The American journal of cardiology, 80(4A), 1997, pp. 11-20

Abstract

Activation of receptor function of platelet membrane glycoprotein (GP) IIb-IIIa leads to the binding of fibrinogen and is the final common pathway to platelet aggregation. Platelet aggregates provide the structural basis tor coronary thrombosis, a major cause of ischemic heart disease. GP IIb-IIIa has a narrow tissue distribution, being found onlyon platelets and their progenitors, and inhibition of its receptor function has emerged as a promising new therapeutic strategy for management of acute ischemic coronary syndromes and acute ischemic complications of percutaneous coronary interventions. Eptifibatide (INTEGRILIN) is a cyclic heptapeptide inhibitor of GP IIb-IIIa, with an active pharmacophore that is derived from the structure of barbourin, a GP IIb-IIIa inhibitor from the venom of the southeastern pigmy rattlesnake. Like barbourin, eptifibatide is a specific and robust inhibitor of the GPIIb-IIIa receptor function, having a low affinity for other integrinsand strongly preventing platelet aggregation. Preclinical pharmacologic studies have established that eptifibatide can inhibit thrombosis effectively, with only modest effects on bleeding time measurements. Pharmacokinetic and pharmacodynamic studies in both animal models and humans have shown that the antiplatelet effect of eptifibatide has a rapid onset of action and that the drug has a short plasma half-life. Furthermore, the rapid reversibility of action of eptifibatide, exemplified by an anti-hemostatic effect limited to the period of drug administration, was apparent in both healthy volunteers and patients with ischemic heart disease. In clinical trials, eptifibatide has not been found to be immunogenic or to induce thrombocytopenia. These studies have led to the evaluation of eptifibatide in the pivotal Integrilin to Minimize Platelet Aggregation and Coronary Thrombosis (IMPACT II) trial, which enrolled 4,010 patients undergoing coronary angioplasty. The combination of a bolus plus either of 2 infusion doses of eptifibatide reduced the incidence of ischemic complications without increasing the risk of bleeding or other complications. Recent pharmacodynamic studieshave established that more aggressive dosing of eptifibatide providesgreater inhibition of ex vivo platelet aggregation and more robust antithrombotic activity. Higher doses of eptifibatide were therefore selected for the Platelet GP IIb-IIIa in Unstable Angina: Receptor Suppression Using Integrilin Therapy (PURSUIT) trial, which enrolled patients with unstable angina or non-Q-wave myocardial infarction. The available data suggest that eptifibatide may represent a useful clinical alternative to existing antiplatelet therapies. (C) 1997 by Excerpta Medico, Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 02/12/20 alle ore 05:34:46