molecules of the month


pM oral sEH epoxide hydrolase inhibitor

completed Ph. I HV study + in animal health

epoxide-opening transition-state mimic

J. Med. Chem., Feb. 7, 2021

EicOsis Human Health Inc., Davis, CA

1 min read

8. The EicOsis oral soluble epoxide hydrolase (sEH) inhibitor, EC5026, is a compound currently intended as a non-opioid analgesic and anti-inflammatory agent. It recently completed a Ph. I study in healthy volunteers without drug-related adverse events. Despite its small size, it has picomolar binding activity with the urea acting as an epoxide-opening transition-state mimic. The authors discuss a range of development considerations including their selection of a clinical path, IND-enabling studies, clinical findings, and even animal health development. This is a must-read for anyone interested in the overall drug discovery process beyond medicinal chemistry.

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