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European Heart Journal 1995 16(Supplement L):50-55; doi:10.1093/eurheartj/16.suppl_L.50
Copyright © 1995 by the European Society of Cardiology.
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© 1995 The European Scociety of Cardiology

Early clinical experience with integrelin, an inhibitor of the platelet glycoprotein IIb/IIIa integrin receptor

E. M. Ohman*,, R. A. Harrington*, A. M. Lincoff{dagger}, M. M. Kitt, N. S. Kleiman{ddagger} and J. E. Tcheng*

* Division of Cardiology, Duke University Medical Center Durham, North Carolina
{dagger} Department of Cardiology, Cleveland Clinic Foundation Cleveland, Ohio
{ddagger} COR Therapeutics, South San Francisco, California (MK), and Baylor College of Medicine Houston, Texas, U.S.A

Correspondence: E. Magnus Ohman, MD, Box 3151, Duke University Durham, NC 27707, U.S.A

Aggregation of platelets leading to thrombosis is one of the hallmarks of unstable angina, acute myocardial infarction, and ischaemic complications following coronary angioplasty. Activated platelets bind to fibrinogen through the glycoprotein IIb/IIIa integrin receptor. New agents have been developed to bind this receptor and thus prevent aggregation of platelets. One such compound (integrelin) is a cyclical peptide that has been shown to be a potent inhibitor of the glycoprotein IIb/IIIa receptor in man. A number of phase I and phase II clinical trials have been completed to evaluate this agent for the indications of unstable angina, acute myocardial infarction, as well as an adjunct to coronary angioplasty. This article will focus on the clinical investigation of integrelin with particular emphasis on its use during angioplasty.

It has been consistently shown across different trials that integrelin can inhibit between 70% and 95% of platelet aggregation responses to 20 µmol of ADP at a variety of dosages used in the phase II trials. Preliminaray data also suggest that a more clinically unstable patient may require a higher dose of integrelin to cause a near complete inhibition of the platelet aggregation response to ADP. Future studies will need to explore more definitely the relationship between dose of glycoprotein IIb/IIIa receptor blockers and clinical instability.

Key Words: Platelet function • angioplasty • complications


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