Drug intelligence / Profile preview

tetomilast + 5-aminosalicylic acid

Development stage
Discontinued
Lead developer
Otsuka Holdings
Modality
Small Molecules
Administration
Oral
01

Overview

Combination drug of **tetomilast** (a selective phosphodiesterase-4 inhibitor with anti-inflammatory activity) and **5-aminosalicylic acid** (5-ASA, a local anti-inflammatory agent frequently used for inflammatory bowel disease). Tetomilast works by inhibiting phosphodiesterase-4 (PDE4), resulting in reduced production of pro-inflammatory cytokines and superoxide by leukocytes[1][3]. 5-aminosalicylic acid exerts topical anti-inflammatory effects on the colonic epithelium, primarily by binding to and activating PPAR-gamma, leading to transcriptional regulation that downregulates NF-kappaB, MAPKs, and reduces COX-2-mediated prostaglandin production, thereby reducing inflammation[2][4][6]. This drug combination is being considered primarily for the treatment of ulcerative colitis.

Other names
5-ASAmesalaminemesalazine
02

Targets

PPARG (Peroxisome proliferator-activated receptor gamma)PDE4D (Phosphodiesterase 4D)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)MEKNF-κBPDE4 (Phosphodiesterase 4A1)

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