Potential of doxofylline in the treatment of chronic obstructive airway diseases (Review)

Doxofylline, a xanthine derivative introduced in 1987, was developed as an alternative to theophylline for the treatment of chronic respiratory disease, including chronic obstructive pulmonary disease and bronchial asthma, but also a promising agent with therapeutic potential, unique pharmacological profile, improved safety and tolerability, potential to decrease corticosteroid dependence and applicability in diverse healthcare settings, including resource-limited environments. The present review examines the utility of doxofylline as an effective bronchodilator, highlighting its improved tolerability profile, minimal drug interactions and distinct pharmacological activities, including its roles as a phosphodiesterase inhibitor, adenosine receptor antagonist and β-adrenergic receptor agonist, alongside its bronchodilator, antitussive and anti-inflammatory properties. The present review performed a comprehensive analysis of literature and a comparative evaluation of relevant clinical trials. By contrast with theophylline, whose clinical use has diminished due to its narrow therapeutic window and notable side effects, doxofylline demonstrates a more favorable safety profile and wider therapeutic range. Doxofylline not only enhances spirometric values and reduces the need for salbutamol administration but also exhibits fewer adverse effects, contributing to improved patient tolerance and adherence to treatment. Clinical findings further suggest significant improvements in lung function, exercise capacity and quality of life among patients treated with doxofylline. These results underscore its potential as a viable long-term therapeutic option, particularly in resource-limited settings, where it may reduce corticosteroid dependency and provide an effective, affordable and safer alternative to theophylline.

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Publication Details

Journal
Biomedical Reports
Published
2025-09-22
DOI
https://doi.org/10.3892/br.2025.2060
Primary Topic
Respiratory and Cough-Related Research
Type
article
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article

Potential of doxofylline in the treatment of chronic obstructive airway diseases (Review)

Vasiliki Georgakopoulou, Alexandr Ceasovschih, Serghei Covanţev, Demetrios�� Spandidos et al.
Biomedical Reports
Respiratory and Cough-Related Research
article

Potential of doxofylline in the treatment of chronic obstructive airway diseases (Review)

Vasiliki Georgakopoulou, Alexandr Ceasovschih, Serghei Covanţev, Demetrios�� Spandidos, Alexandru Corlăteanu, Anna Bumbu, Diana Poparcea
article en

Abstract

Doxofylline, a xanthine derivative introduced in 1987, was developed as an alternative to theophylline for the treatment of chronic respiratory disease, including chronic obstructive pulmonary disease and bronchial asthma, but also a promising agent with therapeutic potential, unique pharmacological profile, improved safety and tolerability, potential to decrease corticosteroid dependence and applicability in diverse healthcare settings, including resource-limited environments. The present review examines the utility of doxofylline as an effective bronchodilator, highlighting its improved tolerability profile, minimal drug interactions and distinct pharmacological activities, including its roles as a phosphodiesterase inhibitor, adenosine receptor antagonist and β-adrenergic receptor agonist, alongside its bronchodilator, antitussive and anti-inflammatory properties. The present review performed a comprehensive analysis of literature and a comparative evaluation of relevant clinical trials. By contrast with theophylline, whose clinical use has diminished due to its narrow therapeutic window and notable side effects, doxofylline demonstrates a more favorable safety profile and wider therapeutic range. Doxofylline not only enhances spirometric values and reduces the need for salbutamol administration but also exhibits fewer adverse effects, contributing to improved patient tolerance and adherence to treatment. Clinical findings further suggest significant improvements in lung function, exercise capacity and quality of life among patients treated with doxofylline. These results underscore its potential as a viable long-term therapeutic option, particularly in resource-limited settings, where it may reduce corticosteroid dependency and provide an effective, affordable and safer alternative to theophylline.

Biomedical ReportsVol. 23(5)
University of Crete (GR), National and Kapodistrian University of Athens (GR), Grigore T. Popa University of Medicine and Pharmacy (RO), Laiko General Hospital of Athens (GR), Botkin Hospital (RU), Nicolae Testemițanu State University of Medicine and Pharmacy (MD), Ministry of Health (MN)
Openalex Percentile: Top 63%
Respiratory and Cough-Related Research
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