Imaging in Drug Discovery and Early Clinical Trials

Efficient tools for the selection and validation of drug targets both at the preclinical and clinical level are required. Non-invasive imaging and in particular molecular imaging methods are becoming essential technologies to support drug discovery and dvelopment. Imaging provides structural, functional, metabolic and molecular readouts that are being applied to characterize a disease phenotype (diagnosis), to elucidate molecular mechanisms involved, to evaluate drug efficacy and safety, and to identify potential biomarkers of the drug's mechanism-of-action, efficacy and safety. Non-invasive imaging techniques constitute a bridge between preclinical and clinical drug evaluation. In this monograph the contribution of imaging modalities to the various stages of drug discovery and development, from early target validation to their use in clinical development programs, is described. Chapters are devoted to the description of the drug discovery process as such, to the various imaging modalities being used both preclinically and clinically, to applications of imaging during the optimization of a lead compound (addressing issues such as bioavailability and efficacy) and during the drug safety evaluation.