Drug intelligence / Profile preview

tetomilast

Development stage
Phase 3
Lead developer
Otsuka Holdings
Modality
Small Molecules
Administration
Oral
01

Overview

Tetomilast is a small molecule thiazole derivative that acts as a selective phosphodiesterase‐4 (PDE‐4) inhibitor. By inhibiting PDE‐4, tetomilast increases intracellular cyclic adenosine monophosphate (cAMP), leading to anti-inflammatory effects. This includes suppression of pro-inflammatory mediators such as TNF-alpha and IL‐12 and stimulation of anti-inflammatory mediators like IL‐10 and prostaglandin E2. It was developed primarily for the treatment of inflammatory bowel diseases (including Crohn's disease and ulcerative colitis) and chronic obstructive pulmonary disease (COPD). Clinical trials in ulcerative colitis did not demonstrate significant efficacy over placebo for primary endpoints but suggested some potential activity in subgroups with higher baseline inflammation[1][3][5][6].

Other names
Tetomilast [INN]6-(2-(3,4-diethoxyphenyl)thiazol-4-yl)picolinic acid6-[2-(3,4-diethoxyphenyl)-1,3-thiazol-4-yl]pyridine-2-carboxylic acid145739-56-6
02

Targets

PDE4 (Phosphodiesterase 4A1)

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