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Trust Your Gut: Strategies and Tactics for Intestinally Restricted Drugs

Ruth Dorel, Alice R. Wong, James J. Crawford

2023ACS Medicinal Chemistry Letters17 citationsDOIOpen Access PDF

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.

Topics & Concepts

Gastrointestinal tractDosingPharmacologyMedicineIntestinal permeabilityComputational biologyBiologyInternal medicineDrug Transport and Resistance MechanismsDrug Solubulity and Delivery SystemsPharmaceutical studies and practices
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