Pharmacological Properties of Abciximab

Mary Ann Mascelli; Marian T. Nakada

doi:10.1055/s-0038-1660390

Hämostaseologie, Table of Contents

Hamostaseologie 1999; 19(03): 101-107
DOI: 10.1055/s-0038-1660390

Übersichts- und Originalarbeiten/Review and Original Articles

Schattauer GmbH

Pharmacological Properties of Abciximab

Mary Ann Mascelli

¹Clinical Pharmacology, Centocor, Malvern, PA, USA

,

Marian T. Nakada

¹Clinical Pharmacology, Centocor, Malvern, PA, USA

› Author Affiliations

Abstract

Abciximab is the first of a new class of therapeutic agents that specifically block the function of the platelet cell adhesion receptor, glycoprotein (GP) IIb/IIIa and the subsequent platelet aggregation that contributes to thrombosis. Abciximab displays high avidity for the GPIIb/IIIa receptor, which results in a prolonged platelet-bound half-life, and a sustained duration of platelet inhibition resulting from the redistribution and equilibration of abciximab molecules among circulating platelets at gradually diminishing levels of GPIIb/IIIa receptor occupancy. In contrast to its extended platelet bound life-span, unbound abciximab is cleared rapidly (half-life <10 min) after an intravenous bolus dose. Nevertheless, a subsequent continuous infusion that maintains relatively low concentrations of free abciximab (50 to 100 ng/ml) sustains the pharmacologic GPIIb/IIIa receptor blockade throughout the duration of treatment. In addition, abciximab also interacts with other potentially important biological targets. The agent binds with equal affinity to the other β₃ containing integrin, the vitronectin (α_vβ₃) receptor, and more weakly to the leukocyte Mac-1 receptor. The high avidity and multi-receptor specificity of abciximab are consistent both short- and long-term therapeutic benefits in patients with acute coronary syndromes.

Keywords

Abciximab - glycoprotein IIb/IIIa

Full Text

References

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