The extensive clinical study of antiplatelet and anticoagulant therapy in PCI documented in this review has not only justified the standard of care but also provided the framework for the introduction of novel therapeutic agents such as those discussed previously. Although the evolution to this current standard has been relatively rapid and there have been substantial advancements made in this arena, there remains a clinically relevant rate of ischemic and bleeding complications. This fact, coupled with ongoing advancements in the understanding of mechanisms of vascular injury and thrombosis with ACS and PCI, continues to drive researchers and clinicians to develop new classes of agents with improved pharmacokinetic, efficacy, and safety profiles. Currently, patient- and lesion-specific characteristics guide the interventionalist in deciding which specific antithrombotic and antiplatelet agents to use before, during, and after PCI. In the future, pharmacogenomics, the science of examining genetic variations that dictate response to drug therapy, may play a role in the choice of anticoagulation for any given patient. Until that time, however, the continued execution of well-designed clinical trials of existing and novel pharmacotherapeutic agents and adherence to the findings of such trials is necessary to optimize the outcomes in the growing population of patients undergoing PCI.