Drug intelligence / Profile preview

theophylline

Development stage
Approved
Lead developer
Fleming & Co
Modality
Small Molecules
Administration
Oral
01

Overview

Theophylline is a methylxanthine derivative and bronchodilator used to manage symptoms of asthma and chronic obstructive pulmonary disease (COPD), as well as other lung conditions characterized by reversible airflow obstruction. It works primarily by relaxing bronchial smooth muscle to improve airflow. Mechanistically it acts as a nonselective phosphodiesterase inhibitor (leading to increased intracellular cAMP), an adenosine receptor antagonist (blocking bronchoconstrictive effects of adenosine), and a histone deacetylase activator. The drug also has mild diuretic properties and central nervous system stimulant effects. The primary indications are asthma and COPD; it is considered a second-line agent due to its narrow therapeutic window and potential for toxicity.

Brand names
ElixophyllinNorphylPhyllocontinQuibron-TQuibron-T/SRTheo-24Theo24Theo 24TheoCapTheochronTheo-DurTheo-TimeTruxophyllinUniphylElixophyllinePulmophylline
Other names
1,3-dimethylxanthine
02

Targets

HDAC (HDAC family)ADOR (Adenosine receptors)PDE (Phosphodiesterase family)

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