Drug Metabolism | Principles for Medicinal Chemists

One of the most difficult parts of discovering a drug is the optimization of pharmacokinetic properties.  Drug hunters must be mindful of ADME (absoprtion, distribution, metabolism and excretion) properties to insure that drug candidates have adequate drug exposures across preclinical species and ultimately humans.  Frequently, drug candidates are highly metabolized, limiting exposure to the drug target tissue.  Thus, mitigation of metabolism issues is one of the most impactful ways to improve the pharmacokinetic profile of a drug candidate.  This webinar described the most common drug metabolizing enzymes (DMEs) and metabolic pathways encountered in drug discovery.  Importantly, it also highlighted the assays and mitigation strategies in use to profile, understand and optimize the metabolism of drug candidates.  Other important principles, such as minimizing the formation of reactive metabolites and the impact of cytochrome p450 (CYP) inhibitors/activators on drug-drug interactions (DDIs) were described.

While the focus is on medicinal chemistry methods, the webinar will benefit all scientists who participate in the cross functional execution of drug discovery programs.

This FREE webinar was presented by Dr Bryan Norman. Bryan is the tutor on the 1.5 day course: Medicinal Chemistry Strategies to Mitigate Preclinical Safety Risks in Drug Discovery