Maintenance of asthma control by once‐daily inhaled ciclesonide in adults with persistent asthma

Chapman, Kenneth R.; Patel, Piyush M.; D’Urzo, Anthony; Alexander, Michael; Mehra, Sunil; Oedekoven, C.; Engelstätter, Renate; Lp, Boulet

doi:10.1111/j.1398-9995.2004.00750.x

Cited by 101 publications

(64 citation statements)

References 22 publications

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“…However, the experience from corticosterone suggests that formation of esters alone may not be sufficient to affect the tissue kinetics of the GCs. There is no information on the role of CIC-AM esterification on the retention of CIC-AM in the airways, and once daily efficacy of CIC (Chapman et al, 2005;Pearlman et al, 2005) may be due to other CIC and CIC-AM features, such as high lipophilicity. For example, MF is reported to be effective at once daily inhalation (Nayak et al, 2000;Karpel et al, 2005), although it does not form esters.…”

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confidence: 99%

Differences in Endogenous Esterification and Retention in the Rat Trachea between Budesonide and Ciclesonide Active Metabolite

Lexmuller

Gullstrand²,

Axelsson³

et al. 2007

Drug Metab Dispos

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ABSTRACT:The airway retention of inhaled glucocorticosteroids (GCs) depends largely on their lipophilicity. Inhaled budesonide (BUD) becomes highly lipophilic reversibly by the formation of esters acting as a reservoir of active BUD. Ciclesonide (CIC) was also reported to form esters after hydrolysis to active metabolite (CIC-AM). We have investigated lipophilicity and airway retention of BUD, CIC/ CIC-AM, fluticasone propionate (FP), and mometasone furoate (MF), and compared esterification of BUD and CIC-AM and its contribution to GC airway retention. Rat tracheas were preincubated with the esterification inhibitor cyclandelate or vehicle. A 3 H-GC (ϳ10 ؊7 M: BUD, CIC, CIC-AM, FP, MF) was added for 20 min.After incubation, one half of the trachea was used for analysis of GC uptake and the other to analyze GC release during 3 h in drug-free medium. GC species in trachea halves were analyzed by radiochromatography. At 20 min, the uptake of BUD was similar to that of CIC/CIC-AM; however, the BUD-ester pool was 9-fold greater (p < 0.01). BUD overall retention in trachea at 3 h was greater than that of other GCs (p < 0.01), and the BUD-ester pool was 3-fold greater than the CIC-AM-ester pool (p < 0.01). Cyclandelate decreased the initial BUD-and CIC-AM-ester pools (p < 0.01), and reduced the overall retention of BUD at 3 h (p < 0.01) but not of CIC-AM. Thus, BUD becomes esterified in the airways more promptly and to a greater extent than CIC-AM, and BUD esterification prolongs BUD airway retention. In contrast, airway retention of CIC-AM and CIC seems to be determined mainly by their lipophilicity, similar to FP and MF, which are not esterified.

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confidence: 99%

Differences in Endogenous Esterification and Retention in the Rat Trachea between Budesonide and Ciclesonide Active Metabolite

Lexmuller

Gullstrand²,

Axelsson³

et al. 2007

Drug Metab Dispos

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“…Level 2 evidence from fully published studies investigating the efficacy and safety of ciclesonide is available, including placebocontrolled studies (Chapman et al 2005;Langdon et al 2005;Pearlman et al 2005;Bateman et al 2006b;Gelfand et al 2006) and trials with active comparator (Buhl et al 2005a;Niphadkar et al 2005;Boulet et al 2006a;Hansel et al 2006). Further evidence is also currently available in abstract form only, hindering full critical appraisal.…”

Section: Clinical Evidence With Ciclesonide In Asthmamentioning

confidence: 99%

Ciclesonide in persistent asthma: the evidence of its therapeutic value

Journal¹

2006

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Introduction: Asthma, a respiratory disease associated with airway inflammation and hyperresponsiveness, is one of the most prevalent chronic diseases worldwide affecting both children and adults. Inhaled corticosteroids are considered to be the cornerstone of asthma management. Ciclesonide, an airway-activated inhaled corticosteroid, has been developed for the management of persistent asthma. Its once-daily administration and airway activation may be advantageous in the treatment of asthma.

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“…[29,30]. Mit der einmal täglichen Applikation verbindet sich die Hoffnung auf eine deut− liche Verbesserung der Therapieadhärenz einer ICS−Therapie.…”

Section: Antiinflammatorische/antiasthmatische Wirksamkeitunclassified

Ciclesonid - ein neues inhalatives Kortikosteroid

Ukena

2005

Pneumologie

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Maintenance of asthma control by once‐daily inhaled ciclesonide in adults with persistent asthma

Abstract: Ciclesonide (160 or 640 microg) once daily in the morning effectively maintains asthma control, does not affect cortisol levels, and has an adverse event profile comparable with placebo in adults with primarily mild to moderate asthma.

Cited by 101 publications

References 22 publications

Differences in Endogenous Esterification and Retention in the Rat Trachea between Budesonide and Ciclesonide Active Metabolite

Differences in Endogenous Esterification and Retention in the Rat Trachea between Budesonide and Ciclesonide Active Metabolite

Ciclesonide in persistent asthma: the evidence of its therapeutic value

Ciclesonid - ein neues inhalatives Kortikosteroid

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