Drug intelligence / Profile preview

tebufelone

Development stage
Discontinued
Lead developer
Procter & Gamble
Modality
Small Molecules
Administration
Oral
01

Overview

Tebufelone is a small molecule nonsteroidal anti-inflammatory drug (NSAID) of the di-tert-butyl-phenol class, developed as a dual cyclooxygenase (COX)/5-lipoxygenase (5-LOX) inhibitor. It exhibits potent analgesic, antipyretic, and anti-inflammatory activities in preclinical and clinical models. Its mechanism of action involves reversible inhibition of both cyclooxygenase and 5-lipoxygenase enzymes, leading to decreased synthesis of prostaglandins and leukotrienes, respectively. Tebufelone was studied primarily for rheumatic disorders and pain but its development was discontinued after phase II clinical trials, likely due to safety or efficacy concerns[1][3][4][6][7][10].

Other names
TebufeloneTebufelonumTebufelonaNE 11740NE11740NE-117401-(3,5-ditert-butyl-4-hydroxyphenyl)hex-5-yn-1-one3',5'-Di-tert-butyl-4'-hydroxy-5-hexynophenone112018-00-5O048K9ZFHOO-048K9ZFHOO 048K9ZFHO5-Hexyn-1-one, 1-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-Tebufelone [USAN:INN]Tebufelone (USAN/INN)Tebufelona [INN-Spanish]
02

Targets

PTGS2 (Prostaglandin-Endoperoxide Synthase 2)ALOX5 (Arachidonate 5-lipoxygenase)PGHS-1 (Prostaglandin G/H Synthase 1)

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