Noninvasive imaging has played an increasing role in the process of cardiovascular drug development. This review focuses specifically on the use of molecular imaging, which has been increasingly applied to improve and accelerate certain preclinical steps in drug development, including the identification of appropriate therapeutic targets, evaluation of on-target and off-target effects of candidate therapies, assessment of dose response, and the evaluation of drug or biological biodistribution and pharmacodynamics. Unlike the case in cancer medicine, in cardiovascular medicine, molecular imaging has not been used as a primary surrogate clinical end point for drug approval. However, molecular imaging has been applied in early clinical trials, particularly in phase 0 studies, to demonstrate proof-of-concept or to explain variation in treatment effect. Many of these applications where molecular imaging has been used in drug development have involved the retasking of technologies that were originally intended as clinical diagnostics. With greater experience and recognition of the rich information provided by in vivo molecular imaging, it is anticipated that it will increasingly be used to address the enormous time and costs associated with bringing a new drug to clinical launch.