Medicinal Chemistry Lecture Series: Dr. Nicholas Carruthers, Day 2

Lecture #3 – Modern Drug Discovery: Lead Optimization through Candidate Selection

Following the identification of a working SAR template, the focus will move to selectivity, target engagement, in vivo assessment in animal models, pharmacokinetics (plasmaconcentration/time curves), pharmacodynamics and ADME (absorption, distribution, metabolism and excretion). This will include the relevance of animal models to human disease and the progression to a clinical candidate. The importance of being able to relate dose (plasma concentration) to target engagement in healthy volunteers and patients will be discussed and how this allows for the identification of improved clinical candidates.

Lecture #4 – Case Studies
P2X7 Antagonist (Depression) Solving Drug Metabolism Issues, Orexin-1 Antagonist (Anxiety) Exploiting the Kinetic Isotope Effect, AMPA-g8 Modulator (Seizure Disorders) Targeting Protein-Protein Interactions. The three case studies will build on the concepts described in Lectures 2 and 3 and demonstrate how optimal structures can be obtained for clinical evaluation. The emphasis will be on how deficiencies in promising pre-clinical candidates can be addressed via thoughtful structural modifications.

Please kindly note that there are limited seats for each talk, therefore you will be contacted directly if there is a seat for you. 

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