A roadmap for drug discovery and its translation to small molecule agents in clinical development for tuberculosis treatment.

Drug discovery and development, from an initial disease treatment concept to a new drug application (NDA), is a complex, lengthy and expensive process. In this review we discuss the key stages of drug discovery and early development, including target identification and validation, assay development and screening, confirmed hits to leads, lead optimization, and progressing development candidates to an investigational new drug (IND) filing. We also provide particular examples of how this process is beginning to assist in the development of small molecule treatments for tuberculosis, by summarizing the status of the clinical development of several newer classes of drugs. These include the fluoroquinolones, oxazolidinones, diarylquinolines, and nitroimidazo-oxazoles and -oxazines.