The Drug Discovery Process: from Lead Optimization to the Clinical Candidate

This course will give an overview of the approaches characterizing a crucial stage of the drug discovery process, i.e. the optimization of lead compounds towards the selection of drug candidates for clinical phases. The goal of this stage is to extensively optimize, in parallel, both the biological activity and the properties of the lead series, through a dedicated screening funnel of both in vitro and in vivo assays. Colleagues from companies, with consolidated expertise in the field, will illustrate the relavant steps of lead optimization, including medicinal chemistry, in vivo analysis, pharmacodynamics and toxicologival assessment, solid state characterization and preformulation studies. Selected case examples will also be presented and discussed.