[2019 Pasteur Colloquium] Prof. Young G. Shin, College of Pharmacy, Chungnam National University
2019-10-01
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IPK Pasteur Colloquium
Date : Wed. Oct. 02, 2019 at 04:00pm
Venue : Monod Room (1F), Institut Pasteur Korea
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SPEAKER
Young G. Shin, Ph.D.
Professor, College of Pharmacy, Chungnam National Univ.
TALK TITLE
How to Overcome High Clearance and Poor Bioavailability of New Chemical Entities during Lead Optimization? Strategies and Case Study
ABSTRACT
Poor exposure following oral administration is a common challenge facing discovery programs and consequently a frequent focus for DMPK scientists. Frequently, potent compounds cannot be further developed due to less-than-ideal ADME (adsorption, distribution, metabolism and excretion) properties that prevent the compound to be available following oral administration. Beyond the discovery phase, the importance of understanding and optimizing oral exposure continues in the preclinical and ultimately clinical phase of drug development. Inadequate oral exposure could be due to suboptimal physicochemical properties, or problems in absorption from the gut, or first-pass metabolism in the gut and liver, or high intrinsic clearance of the compounds. The focus of this presentation is 1) to identify and learn about the issues that contribute to low oral exposure, and 2) to discuss approaches that one could use to overcome those challenges.
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