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Roflumilast

In Chronic Obstructive Pulmonary Disease

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Abstract

Roflumilast is an orally administered, selective phosphodiesterase 4 inhibitor that is a novel treatment for patients with severe chronic obstructive pulmonary disease (COPD).

Across four randomized, double-blind, multinational trials in patients with moderate to severe or severe COPD, roflumilast 500 μg/day produced significantly greater improvements from baseline than placebo in pre- and post-bronchodilator forced expiratory volume in 1 second (FEV1). While mean increases in FEV1 in roflumilast groups were small, they were in marked contrast to the decreases or negligible increase in FEV1 in the placebo groups. In three of four trials, roflumilast significantly reduced the COPD exacerbation rate; in a pooled analysis of two 52-week trials, roflumilast was associated with a 17% reduction over placebo.

Further randomized, double-blind, multinational trials compared roflumilast 500 μg plus salmeterol with placebo plus salmeterol and roflumilast 500 μg plus tiotropium bromide with placebo plus tiotropium bromide. In both trials, roflumilast plus long-acting bronchodilator produced significantly greater increases in pre- and post-bronchodilator FEV1 than placebo plus long-acting bronchodilator.

Roflumilast had an acceptable tolerability profile. In a pooled analysis of two trials, 19% and 22% of roflumilast and placebo recipients had serious adverse events; in the corresponding groups, 14% and 11% discontinued medications because of adverse events.

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Acknowledgements and Disclosures

The manuscript was reviewed by: A.D. D’Urzo, Department of Family and Community Medicine, University of Toronto, Toronto, Ontario, Canada; O.E. Della Pasqua, Leiden/Amsterdam Centre for Drug Research, Leiden, the Netherlands, and GlaxoSmithKline Research and Development, Stockley Park, Uxbridge, UK; J.A. Falk, Division of Pulmonary and Critical Care Medicine, Department of Medicine, Cedars-Sinai Medical Center, Los Angeles, California, USA; A.F. Gelb, Pulmonary Division, Department of Medicine, Lakewood Regional Medical Center, Lakewood, California, USA; J. Walters, Menzies Research Institute, University of Tasmania, Hobart, Tasmania, Australia.

The preparation of this review was not supported by any external funding. During the peer review process, the manufacturer of the agent under review was offered an opportunity to comment on this article. Changes resulting from any comments were made on the basis of scientific and editorial merit.

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    Mark Sanford

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Sanford, M. Roflumilast. Drugs 70, 1615–1627 (2010). https://doi.org/10.2165/11205930-000000000-00000

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