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Trust Your Gut: Strategies and Tactics for Intestinally Restricted Drugs
Ruth Dorel1, Alice R Wong1, James J Crawford1
1Genentech, Inc., South San Francisco, California 94080, United States.
Abstract:
Non-absorbable small-molecule drugs targeted to the gut represent an alternative approach to safe, non-systemic therapeutics. Such drugs remain confined to the gastrointestinal tract upon oral dosing by virtue of their limited passive permeability, increasing the local concentration at the site of action while minimizing exposure elsewhere in the body. Herein we review the latest advances in the field of gut-restricted therapeutics, highlighting the different strategies and tactics that medicinal chemists have employed in pursuit of drugs with minimal intestinal absorption.
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