Ciclesonide-d7 is intended for use as an internal standard for the quantification of ciclesonide by GC- or LC-MS. Ciclesonide is a prodrug form of the glucocorticoid receptor agonist desisobutyryl-CIC (des-CIC).1 CIC binds to the glucocorticoid receptor with a Ki value of 37 nM.2 It is selective for the glucocorticoid receptor over the estrogen, progesterone, and testosterone receptors. CIC inhibits eosinophil influx into the lung (ED50 = 0.49 mg/kg) and reduces sephadex-induced lung edema (ED50 = 0.72 mg/kg) in a rat model of ovalbumin-sensitized and -challenged airway inflammation. Formulations containing CIC have been used in the maintenance treatment of asthma and in the treatment of allergic rhinitis.
References
1. Derendorf, H., Nave, R., Drollmann, A., et al. Relevance of pharmacokinetics and pharmacodynamics of inhaled corticosteroids to asthma. Eur. Respir. J. 28(5), 1042-1050 (2006).
2. Belvisi, M.G., Bundschuh, D.S., Stoeck, M., et al. Preclinical profile of ciclesonide, a novel corticosteroid for the treatment of asthma. J. PHarmacol. Exp. Ther. 314(2), 568-574 (2005).