title: Ciclesonide: a closer look at its systemic and oropharyngeal safety profile.
abstract: Inhaled corticosteroids (ICS) are recommended first-line therapy for patients with asthma of all severities. Prolonged exposure to high-dose ICS can cause systemic and oropharyngeal adverse events. Minimizing ICS-related adverse events by selecting an ICS with an improved safety profile may increase patients' adherence to their asthma treatment. Ciclesonide, a novel ICS currently under development, is a parent compound that is converted in the lungs by endogenous esterases to its active metabolite, desisobutyryl-ciclesonide. Reported data suggest that ciclesonide is well tolerated, with no observed effect on hypothalamic-pituitary-adrenal (HPA)-axis function and a low incidence of oropharyngeal adverse events (comparable with placebo). These safety benefits, observed in children and adults with asthma, may be due to ciclesonide's favorable pharmacokinetic/pharmacodynamic properties. The lack of HPA-axis function suppression may be due to the low oral bioavailability, high serum protein binding and rapid apparent systemic clearance reported with desisobutyryl-ciclesonide. The low incidence of oropharyngeal adverse events may be attributed to the low oral deposition of ciclesonide in the oropharynx and its limited conversion to desisobutyryl-ciclesonide. The favorable safety profile of ciclesonide suggests a conferred benefit to asthma patients treated with this novel ICS.
authors.affiliation: Allergy and Asthma Associates, 27800 Medical Center Road, Mission Viejo, CA 92691, USA. weberger@uci.edu
authors.forename: William E
authors.initials: WE
authors.lastname: Berger
mesh_terms: D000280:Administration, Inhalation; D000328:Adult; D018927:Anti-Asthmatic Agents / Q000008:administration & dosage / Q000009:adverse effects* / Q000627:therapeutic use; D001249:Asthma / Q000150:complications / Q000188:drug therapy; D002648:Child; D006130:Growth Disorders / Q000139:chemically induced / Q000453:epidemiology; D006801:Humans; D007030:Hypothalamo-Hypophyseal System / Q000187:drug effects; D009059:Mouth Diseases / Q000139:chemically induced* / Q000453:epidemiology / Q000473:pathology; D010608:Pharyngeal Diseases / Q000139:chemically induced* / Q000453:epidemiology / Q000473:pathology; D010913:Pituitary-Adrenal System / Q000187:drug effects; D011282:Pregnenediones / Q000008:administration & dosage / Q000009:adverse effects* / Q000627:therapeutic use
chemical_list: D018927:Anti-Asthmatic Agents; D011282:Pregnenediones; C120481:ciclesonide