[The discovery process in the pharmaceutical industry]

Abstract

This paper reviews the process used in the pharmaceutical industry to discover new innovative drugs originating from medicinal chemistry or biotherapeutics. After a rapid description of the global Research and Development process (preclinical and clinical studies), the different steps involved specifically in the Discovery Research phase (from the initiation of the research program to the proposal of a candidate for development) are analysed in detail. As far as compounds originating from medicinal chemistry are concerned, we discuss the choice of the biological target (molecular or cellular) and its functional validation, the process used for the screening of chemical libraries and the generation of chemical hits, the hit-to-lead process and finally the chemical optimisation of the leads into drug candidates which will be proposed for preclinical and clinical development. As far as biotherapeutics are concerned, the process used for the generation and manufacturing of humanized naked or conjugated monoclonal antibodies and recombinant therapeutic proteins is discussed in detail.