J Clin Pharmacol
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DRUG INTERACTIONS

The Targeted Oral, Once-Daily Phosphodiesterase 4 Inhibitor Roflumilast and the Leukotriene Receptor Antagonist Montelukast Do Not Exhibit Significant Pharmacokinetic Interactions

Gabriele M. Böhmer, MD, Nassr Nassr, MD, Marcus Wenger, Andreas Hünnemeyer, MD, Gezim Lahu, Silke Templin, MD, Christoph H. Gleiter, MD, FCP and Robert Hermann, MD, FCP

From the Department of Clinical Pharmacology, University Hospital of Tübingen, Tübingen, Germany (Dr Böhmer; Marcus Wenger, Dr Templin, Dr Gleiter); Department of Exploratory Clinical Development, Nycomed GmbH, Konstanz, Germany (Dr Nassr, Dr Hünnemeyer, Gezim Lahu); Institute for Toxicology, Pharmacy and Chemistry, University of Tuebingen, Germany (Gezim Lahu); and Clinical Research Appliance, Radolfzell, Germany (Dr Hermann).

This nonrandomized, fixed-sequence, 3-period study investigated potential pharmacokinetic interactions between the leukotriene receptor antagonist montelukast, approved for the treatment of asthma, and roflumilast, an oral, once-daily phosphodiesterase 4 inhibitor in clinical development for asthma and chronic obstructive pulmonary disease. Pharmacokinetic interactions are of interest because both drugs may be coadministered and share a common metabolic pathway via cytochrome P450 3A. Single-dose montelukast (10 mg, po) was administered alone in period 1, followed by repeated once-daily roflumilast alone (500 µg, po) for 12 days (period 2). In period 3, 500 µg qd roflumilast was coadministered with 10 mg qd montelukast for 8 days. Different pharmacokinetic parameters were evaluated for montelukast alone, for steady-state roflumilast and its pharmacologically active metabolite roflumilast N-oxide alone, for single-dose montelukast when coadministered with steady-state roflumilast, and for steady-state roflumilast and its N-oxide metabolite when coadministered with steady-state montelukast. The AUC and Cmax of montelukast were modestly increased by 9% and 8%, respectively, when single-dose montelukast was coadministered with steady-state roflumilast. The pharmacokinetics of roflumilast and roflumilast N-oxide in steady state remained unchanged when repeat-dose montelukast was coadministered at steady-state. Concomitant administration of both drugs was well tolerated. These findings suggest that no dose adjustment is warranted for either drug when roflumilast and montelukast are coadministered.

Key Words: Drug interaction • roflumilast • montelukast

Address for reprints: Gabriele M. Böhmer, Abteilung Klinische Pharmakologie, Universitätsklinikum Tübingen, Otfried-Müller-Str 45, D-72076 Tübingen, Germany; e-mail: gabriele.boehmer{at}med.uni-tuebingen.de.


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