Clopidogrel is an antithrombic compound whose active metabolite is a selective, irreversible antagonist of the platelet purinergic P2Y12 receptor (IC50 = 100 nM). Clopidogrel inhibits ADP-induced platelet aggregation ex vivo and functions as a prodrug whereupon biotransformation to its active metabolite via CYP2C19 in the liver enables its anti-aggregating activity. Marketed under the name Plavix , clopidogrel in combination with aspirin has been shown to be beneficial in the prevention of vascular ischemic events for patients without deficiencies in CYP2C19-related metabolism.
cis-Clopidogrel-MP derivative, also known as Clopidogrel-MP-AM, is a 3’-methoxyacetophenone derivative of Clopidogrel active metabolite. This compound is an orally-active platelet inhibitor specifically targeting the P2Y12 receptor.
Clopidogrel HCl is the salt form of Clopidogrel (free base), an inhibitor of ADP-induced platelet aggregation acting by direct inhibition of adenosine diphosphate (ADP) binding to its receptor and of the subsequent ADP-mediated activation of the glycoprotein GPIIb IIIa complex.
ACT-281959, a prodrug of ACT-246475, is a novel potent and selective P2Y12 Receptor Antagonist with a Wider Therapeutic Window in the Rat Than Clopidogrel. ACT-281959 showed antithrombotic efficacy after oral administration in the rat ferric chloride model. ACT-281959 entered clinical studies in healthy volunteers.