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ISSX Webinar: Physicochemistry and ADMET
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Thank you for your interest in attending the ISSX Webinar. This webinar is now full and registration is closed. A recording will be made available to ISSX Members later this month.

ISSX Members are invited to attend a free one-hour webinar on Wednesday, January 18 at 10:00 am ET US.

Lipoidal or lipid permeability has been used to define the disposition characteristics of molecules (BDDCS) and these relationships can be extended through biopharmaceutics to actual pharmacological and toxicological outcome (pharmacodynamics). Moreover the same guiding principles can be used to understand the likely outcomes of metabolism. The relationship between lipoidal permeability and lipophilicity is due to the alkyl chain interior of the bilayer. Compounds have to have positive lipophilicity. Hydrogen bonding groups have to undergo desolvation when they move from an aqueous extracellular environment to the lipophilic interior of membranes. Hydrogen bonding and the removal of solvent thus represents, a large part, of the energy cost involved in membrane permeability. Lipophilic functions in contrast readily de-solvate and are therefore favourable energy wise to membrane permeability. The same basic factors can be related to interations with proteins that trigger pharmacodynamic effects. Lipophilicity and hydrogen bonding can be quantified and calculated. The session will describe the use of log P, log D and pKa, PSA and TPSA and the limitations of each. The relationship to pharmacokinetic parameters will be discussed, particularly Vd (drug binding), free drug concentration and target interactions. The discussion will extend the concepts to metabolites in terms of the impact of metabolism on physicochemical characteristics, the effect on disposition and likely pharmacological properties.


About the Speaker:

Dr. Dennis Smith worked in the pharmaceutical industry for 32 years after gaining his Ph.D. from the University of Manchester. During this period, he directly helped in the Discovery and Development of eight marketed NCEs. For the last nine years he has taken on a number of roles. Academic appointments include Honary Professor at the University of Capetown, where he is closely involved with H3D, the leading academic drug discovery unit in Africa. He is a member of a number of Expert Panels working within organisations such as Medicines for Malaria Venture and Cancer Research UK as well as serving on Scientific Advisory Boards for a number of Research Institutions. His research interests and publications span all aspects of Drug Discovery and Development particularly where drug metabolism knowledge can impact on the design of more efficacious and safer drugs. He has co-authored over 170 publications. He was recently elected as the first Fellow of the Drug Metabolism Discussion Group.

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