Drug intelligence / Profile preview

doxofylline

Development stage
Phase 4
Lead developer
Alitair Pharmaceuticals
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Doxofylline is a methylxanthine derivative and bronchodilator used primarily for the treatment of chronic respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD). It is structurally related to theophylline but has a better safety profile with fewer side effects. The main mechanism of action involves inhibition of phosphodiesterase enzymes (notably PDE3 and PDE4), leading to increased cyclic AMP levels, which causes relaxation of bronchial smooth muscle and bronchodilation. Doxofylline also exhibits anti-inflammatory properties, partly by favoring interleukin-10 release through phosphodiesterase inhibition. Unlike theophylline, it does not significantly inhibit histone deacetylases or act as an antagonist at adenosine receptors except at very high concentrations. Additionally, it interacts with beta-2 adrenoceptors to induce airway smooth muscle relaxation[1][2][6][8].

Brand names
DoxofyllineDoxophylline
Other names
7-(1,3-dioxolan-2-ylmethyl)theophylline
02

Targets

ADORA2A (Adenosine A₂A Receptor)PDE2 (Phosphodiesterase 2)ADRB2 (β2)PDE3PDE4 (Phosphodiesterase 4A1)

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