Synthetic inhibitors of platelet glycoprotein IIb/IIIa in clinical development

Authors
Citation
M. Verstraete, Synthetic inhibitors of platelet glycoprotein IIb/IIIa in clinical development, CIRCULATION, 101(6), 2000, pp. E76-E80
Citations number
30
Categorie Soggetti
Cardiovascular & Respiratory Systems","Cardiovascular & Hematology Research
Journal title
CIRCULATION
ISSN journal
00097322 → ACNP
Volume
101
Issue
6
Year of publication
2000
Pages
E76 - E80
Database
ISI
SICI code
0009-7322(20000215)101:6<E76:SIOPGI>2.0.ZU;2-E
Abstract
Activation of the platelet glycoprotein (GP IIb/IIIa) receptor on the plate let surface is the final pathway of platelet aggregation, regardless of the initiating stimulus. Inhibitors of GP IIb/IIIa receptors include monoclona l antibodies (abciximab) against this receptor and peptidic and nonpeptidic synthetic specific receptor blockers. Abciximab exchanges between and bind s to platelets for as long as 2 weeks, whereas synthetic GP IIb/IIIa inhibi tors inhibit ex vivo platelet aggregation for only a few hours after the en d of infusion, but some have the advantage of also being orally active. In the secondary prevention of atherothrombosis, large-scale trials were succe ssfully conducted with aspirin, dipyridamole, ticlopidine, and clopidogrel. In the first large-scale trials with GP IIb/IIIa inhibitors, abciximab was investigated. Tn aggregate, synthetic GP IIb/IIIa inhibitors, combined wit h aspirin and heparin, were shown to reduce ischemic events in patients wit h high- and low-risk coronary intervention, stents, unstable angina, and no n-Q-wave infarction. With short-term use of synthetic GP IIb/IIIa inhibitor s, there is no suppression of clinical evident restenosis 6 months after th e end of treatment. With the doses currently used, bleeding occurs more oft en with the synthetic GP IIb/IIIa inhibitors (used for 3 days) than with ab ciximab (used for 12 hours), but there are no direct comparisons between th ese drugs.