Abstract

Optimisation of P2Y12 Receptor Antagonists for the Treatment of Arterial Thrombosis: Receptor Kinetics and Pharmacodynamic Relevance

Fabrizio Giordanetto, Director, Taros Chemicals GmbH & Co KG

Antagonism of the P2Y12 receptor results in successful anti-platelet aggregation therapies. The lead optimisation of a series of P2Y12 antagonists with respect to anticoagulation effects, physicochemical and absorption profiles is presented. The observed in vivo effects and pharmacodynamic-pharmacokinetic profiles are discussed in light of the recorded P2Y12 receptor kinetic and the emerging structure-kinetic-relationships.