Overview

• Scientists at Duke, UT Health San Antonio, and University of Arkansas have developed a chemical endocytic medicinal chemistry (CEMC) strategy that uses the CD36 receptor to overcome the Rule of 5 barrier for drug absorption.
• The approach boosts cellular uptake of large-molecule drugs like PROTACs by up to 22.3 times, improving potency by as much as 23 times in preclinical studies.
• Mouse models demonstrated enhanced tumor suppression without compromising drug solubility or stability, with results independently reproduced across multiple institutions.
• The strategy holds potential for converting intravenous drugs into oral formulations and enabling them to cross the blood-brain barrier, broadening treatment options for conditions like Alzheimer’s and brain cancer.
• Researchers are engaging with the FDA to explore new approval frameworks for endocytic drugs and are advancing toward clinical trials to evaluate the approach in humans.