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Clinical Pharmacokinetic and Pharmacodynamic Profile of Inhaled Ciclesonide

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Abstract

Asthma is a chronic inflammatory disease of the airways, and inhaled corticosteroids (ICSs) are recommended as first-line therapy for persistent asthma of all severities. Ciclesonide is a novel ICS, which is administered as an aerosol solution in a metered-dose inhaler, using hydrofluoroalkane-134a as a propellant. Because of the high respirable particle fraction, high pulmonary deposition is obtained in patients, which constitutes the basis of effective therapeutic action. The parent compound, ciclesonide, is pharmacologically inactive and is activated in the target organ, the lung, to form its only pharmacologically active metabolite, desisobutyryl-ciclesonide (des-CIC). Low oral deposition combined with minimal formation of des-CIC in the oropharynx may minimize the typical oropharyngeal adverse events associated with ICSs. Low oral bioavailability, rapid clearance and high protein binding reduce pharmacologically relevant systemic exposure.

The unique pharmacokinetic and pharmacodynamic profile of ciclesonide offers a rationale that supports the favourable risk-benefit profile observed in clinical trials in patients with persistent asthma.

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Acknowledgments

The author acknowledges Gezim Lahu of Pharmacometrics/Pharmacokinetics, Nycomed GmbH, for helpful discussions during the preparation of this review.

All studies were sponsored by Nycomed GmbH (formerly ALTANA Pharma AG), Konstanz, Germany. The author is an employee of Nycomed GmbH and has been involved in the pharmaceutical development of ciclesonide.

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  1. Department of Pharmacometrics/Pharmacokinetics, Nycomed GmbH, Byk-Gulden-Str. 2, 78467, Konstanz, Germany

    Rüdiger Nave

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Nave, R. Clinical Pharmacokinetic and Pharmacodynamic Profile of Inhaled Ciclesonide. Clin Pharmacokinet 48, 243–252 (2009). https://doi.org/10.2165/00003088-200948040-00002

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