P2Y12 Antagonists

Ticlopidine and clopidogrel (Figure 4) are prototypic antagonists of the platelet P2Y12 receptor that is involved in the inhibition of platelet function by selectively blocking ADP-induced platelet aggregation. These compounds were in clinical use long before the P2Y12 receptor was identified and cloned. In patients with unstable angina, ticlopidine reduced endpoints that included nonfatal and fatal myocardial infarction and any cause of cardiovascular death in events at 6 months (13.6% placebo, 7.3% ticlopidine) with a noted trend toward mortality benefit as well. Clopidogrel produces platelet inhibition in a shorter period than ticlopidine, has fewer severe adverse effects, requires only once per day dosing, and is cheaper than a twice per day regimen of ticlopidine. Newer P2Y12 receptor antagonists include CT-50547 and INS-50589 (Figure 4) both of which are in the preclinical stage.

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