Drug intelligence / Profile preview

talniflumate

Development stage
Phase 4
Lead developer
Genaera
Modality
Small Molecules
Administration
Oral
01

Overview

Talniflumate is an orally available small molecule prodrug of niflumic acid, classified as a nonsteroidal anti-inflammatory drug (NSAID). It exhibits potent analgesic and anti-inflammatory effects and has been used primarily for the treatment of inflammatory disorders such as rheumatoid arthritis and osteoarthritis. Talniflumate also acts as a mucin regulator, studied in cystic fibrosis, chronic obstructive pulmonary disease (COPD), asthma, and certain gastrointestinal disorders. Its mechanism involves selective inhibition of the core mucin-synthesizing enzyme GCNT3 (core 2 b-1,6 N-acetylglucosaminyltransferase), leading to decreased mucin production. Additionally, it blocks prostaglandin synthesis by inhibiting cyclooxygenases and acts as a strong calcium-activated chloride channel blocker. Talniflumate was originally developed by Laboratorios Bago and later pursued by Genaera[1][2][3][9].

Brand names
LOMUCIN
Other names
talniflumate2-[3-(trifluoromethyl)anilino]-3-pyridinecarboxylic acid (3-oxo-1H-isobenzofuran-1-yl) ester
02

Targets

CaCC (Calcium-activated chloride channel protein regulator 1)PGHS-1 (Prostaglandin G/H Synthase 1)C2GnT (Core 2 beta-1,6-N-acetylglucosaminyltransferase 1)

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