A New Inhaled Corticosteroid: Ciclesonide

摘要

On January of this year Sanofi-Aventis received an approval letter from the U.S. Food and Drug Administration signifying the approval of ciclesonide (Alvesco~R) 80 and 160 mug/puff by hydrofluoroalkane (HFA) propelled metered dose inhaler (MDI) for the long-term treatment of asthma in children >= 12 years and adults. The drug will be marketed by Sepracor Inc. (Marlborough, MA, USA). The MDIs have dose counters so that patients will know when they need to refill them. It has not yet received approval for use in younger children. Ciclesonide is a prodrug that is hydrolyzed by lung esterases to its more active metabolite (more than 100 times binding affinity for the glucocorticoid receptor in vitro) desisobutyryl-ciclesonide that is frequently abbreviated to des-ciclesonide. The relative glucocorticoid receptor binding affinity of des-ciclesonide would indicate that it is less potent than mometasone furoate and fluticasone propionate,similar to beclomethasone monopropionate (the more active metabolite of beclomethasone dipropionate) and slightly more potent than budesonide.