ACT-281959

ACT-281959 is a novel, potent, and selective oral P2Y12 receptor antagonist developed as a di-ester prodrug of ACT-246475 to improve absorption after oral dosing. It is rapidly converted in vivo by esterases to its active form (ACT-246475) via the intermediate mono-ester prodrug (ACT-409100). The drug acts as a reversible antagonist of the P2Y12 receptor, which plays a central role in platelet activation and aggregation. Preclinical studies demonstrated antithrombotic efficacy in animal models. Clinical development reached phase I trials for thrombosis and cardiovascular diseases but has not progressed further or reported recent activity. The original developer was Actelion Pharmaceuticals; following acquisition, Janssen Pharmaceuticals (a Johnson & Johnson company) became responsible for further development[1][3][4][5].