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Doxofylline is not just another theophylline!

Authors Matera MG, Page C, Cazzola M

Received 5 September 2017

Accepted for publication 31 October 2017

Published 5 December 2017 Volume 2017:12 Pages 3487—3493


Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 3

Editor who approved publication: Dr Richard Russell

Maria Gabriella Matera,1 Clive Page,2 Mario Cazzola3

1Department of Experimental Medicine, Unit of Pharmacology, University of Campania ‘Luigi Vanvitelli’, Naples, Italy; 2Sackler Institute of Pulmonary Pharmacology, Institute of Pharmaceutical Science, King’s College London, London, UK; 3Department of Experimental Medicine and Surgery, Chair of Respiratory Medicine, University of Rome ‘Tor Vergata’, Rome, Italy

Abstract: Doxofylline, which differs from theophylline in containing the dioxalane group at position 7, has comparable efficacy to theophylline in the treatment of respiratory diseases, but with an improved tolerability profile and a favorable risk-to-benefit ratio. Furthermore, it does not have significant drug–drug interactions as exhibited with theophylline, which make using theophylline more challenging, especially in elderly patients with co-morbidities receiving multiple classes of drug. It is now clear that doxofylline also possesses a distinct pharmacological profile from theophylline (no significant effect on any of the known phosphodiesterase isoforms, no significant adenosine receptor antagonism, no direct effect on histone deacetylases, interaction with β2-adrenoceptors) and therefore, should not be considered as just a modified theophylline. Randomized clinical trials of doxofylline to investigate the use of this drug to reduce exacerbations and hospitalizations due to asthma or COPD as an alternative to expensive biologics, and certainly as an alternative to theophylline are to be encouraged.

Keywords: doxofylline, theophylline, mechanisms of action, therapeutic effects, adverse effects

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