Drug intelligence / Profile preview

ciclamilast

Development stage
Preclinical
Lead developer
JOINN Laboratories
Modality
Small Molecules
Administration
Oral
01

Overview

Ciclamilast is a **novel, selective phosphodiesterase 4 (PDE4) inhibitor** developed as a derivative of piclamilast, with enhanced potency and selectivity towards PDE4, particularly the PDE4B subtype[2][4][7]. It acts by *inhibiting PDE4*, which leads to an increase in intracellular cyclic adenosine monophosphate (cAMP) levels, resulting in broad **anti-inflammatory effects** including inhibition of proinflammatory cytokines (such as TNF-α, IL-1β, and IL-6), reduction of leukocyte and eosinophil infiltration, and suppression of lung and joint tissue inflammation[2][3][7][10]. Preclinical studies demonstrate efficacy in models of **asthma, allergic inflammation, and rheumatoid arthritis**, with evidence of improved bronchorelaxant and disease-modifying anti-rheumatic drug (DMARD) activity compared to related compounds[2][3][4][6][7][10][12]. Ciclamilast may also offer reduced gastrointestinal side effects relative to other PDE4 inhibitors[4]. It is primarily administered *orally* in research studies.

Brand names
ciclamilast
Other names
N-(3,5-dichloropyrid-4-yl)-3-cyclopentyloxy-4-methylbenzamide
02

Targets

PDE4B (3',5'-cyclic-AMP phosphodiesterase 4B)PDE4D (Phosphodiesterase 4D)

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