Resumen de Chapter Seven - Recent Advances in the Development of P2Y12 Receptor Antagonists as Antiplatelet Agents
Allorie T. Caldwell, E. Blake Watkins
Abstract P2Y12 receptor antagonists are now the primary mode of treatment for acute coronary syndromes and for patients undergoing percutaneous coronary intervention with stenting. Antagonism of the receptor inhibits ADP-mediated platelet aggregation and results in a reduction in occlusive thrombotic events. Four FDA-approved agents are currently in use. Of these, clopidogrel has seen significant use in the clinic but suffers from inter-individual variation due to genetic differences in patient populations. Additionally, P2Y12 antagonists have demonstrated bleeding risks in certain patient populations. A number of structural analogs have been synthesized in an attempt to circumvent this issue while maintaining strong antiplatelet activity. Improved pharmacokinetic properties as well as potent antiplatelet activity of several of these agents warranted further examination.
