Drug intelligence / Profile preview

L-745,337

Development stage
Discontinued
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

L-745,337 is a potent and highly selective inhibitor of cyclooxygenase-2 (COX-2), originally developed by Merck Frosst. It was designed as a non-steroidal anti-inflammatory drug (NSAID) candidate that could provide therapeutic benefits for inflammation and pain while avoiding the gastrointestinal toxicity typically associated with non-selective COX inhibitors like indomethacin. Research has demonstrated that L-745,337 effectively inhibits the production of pro-inflammatory prostanoids, such as PGE2 and PGI2, in human colonic mucosal biopsies from patients with inflammatory bowel disease (IBD). Although it served as a significant research tool in the development of the coxib class of drugs, it was not commercialized, as Merck ultimately prioritized other candidates such as rofecoxib (Vioxx).

Other names
5-methanesulfonamido-6-(2,4-difluorophenylthio)-1-indanone
02

Targets

PTGS2 (Prostaglandin-Endoperoxide Synthase 2)

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