Open Access

GPVI inhibition: Advancing antithrombotic therapy in cardiovascular disease

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Date: 7 March 2024
Journal: European Heart Journal - Cardiovascular Pharmacotherapy , Volume 10 , Issue 5 , Pages 465 - 473
Topic: CARDIOVASCULAR PHARMACOLOGY, BASIC SCIENCE
Authors: A. Slater , S. Khattak , M. Thomas

ESC Journals

Abstract

Glycoprotein (GP) VI (GPVI) plays a major role in thrombosis but not haemostasis, making it a promising antithrombotic target. The primary role of GPVI on the surface of platelets is a signalling receptor for collagen, which is one of the most potent thrombotic sub-endothelial components that is exposed by atherosclerotic plaque rupture. Inhibition of GPVI has therefore been investigated as a strategy for treatment and prevention of atherothrombosis, such as during stroke and acute coronary syndromes. A range of specific GPVI inhibitors have been characterized, and two of these inhibitors, glenzocimab and revacept, have completed Phase II clinical trials in ischaemic stroke. In this review, we summarize mechanisms of GPVI activation and the latest progress of clinically tested GPVI inhibitors, including their mechanisms of action. By focusing on what is known about GPVI activation, we also discuss whether alternate strategies could be used to target GPVI.

About the contributors

Alexandre Slater

Role: Author

Sophia Khattak

Role: Author

Mark R Thomas

Role: Author