Advances in Chemical Biology

Tutorial Workshop

Topic: Small molecule drug discovery - an introductory course with a glance at cancer immunotherapy

Tuesday, 30 January 2018, 09.00-12.00hrs
Kurt Ritter,
Sanofi, D

The workshop will give a general introduction to the drug discovery process with a focus on small molecules. The process starts with the identification and selection of a disease target or pathway. After detection of first hit compounds in biological assays, iterative rounds of synthesis and testing are used to get to lead structures with clear structure-activity relationship and drug-like properties. Multi-parameter optimization results in compounds showing increased potency  and efficacy in animal disease models. Finally, a clinical candidate is nominated with sufficient efficacy and a tolerable side effect and toxicological profile as entry point to clinical development.

The second part of the workshop will focus on the new field of cancer immunotherapy. Monoclonal antibodies targeting "immune check points" such as pembrolizumab or nivolumab reactivate the silenced immune system to destroy tumor cells. Treatment with these antibodies lead to remarkable, prolonged survival in subsets of patients with difficult to treat cancers such as melanoma or lung cancer. New discovery efforts include also the development of immunomodulatory small molecules, particularly for synergistic combinations with checkpoint antibodies. The course will showcase first examples such as  IDO-inhibitors, adenosine antagonists, and mRNA-based therapies.



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