Chapter Imaging in Drug Discovery and Development
Kristian Stromgaard, Povl Krogsgaard-Larsen, Ulf Madsen · 2009
The genomics/proteomics revolution has led to an explosion in the number of potential targets for therapeutic interventions to something in the order of 5000-10,000. This requires extensive change in strategies for drug discovery and development (DDD) involving high-throughput approaches for target validation and compound screening. The individual phases in the modern DDD process comprise the selection of a potential drug target (D0), which may be based on clinical observations, genetic linkage maps, or on a mechanistic hypothesis (Figure 7.1). The next two phases are related to high-throughput screening of large compound collections and comprise the development of the screening assay (D1) and the high-throughput screening procedure itself (D2), hopefully leading to chemical lead compounds, which are optimized by chemical derivatization during lead optimization (D3). Compounds are compared with regard to ef cacy and potency in relevant animal models of human disease to identify an optimized drug candidate(s) for further characterization including extensive safety assessment (D4). Thereafter, the drug candidate enters the clinical development phases (Phases I-III).