Ciclesonide is a glucocorticoid used in the relief of nasal symptoms associated with seasonal and perennial allergic rhinitis in adults and adolescents. It is also used to treat obstructive airway diseases like asthma, bronchoconstriction, and chronic obstructive pulmonary disease (COPD). Ciclesonide is a pro-drug so it is enzymatically hydrolyzed to C21-desisobutyryl-ciclesonide (des-ciclesonide or RM1), the active metabolite. Des-ciclesonide has anti-inflammatory activity with an affinity for the glucocorticoid receptor that is 120 times higher than ciclesonide. As des-ciclesonide is a glucocorticoid, its mechanism of action is that of the glucocorticoid response element (GRE) of influencing COX-2/prostaglandin G/H synthase 2 suppression and lipocortin/annexin induction. By binding to the glucocorticoid receptor, it influences transcription factors AP-1 and NF-kB to block the transcription of COX-2/prostaglandin G/H synthase 2 which reduces the amount of prostanoids being produced from arachidonic acid. Prostanoids such as PGI2 and thromboxane A2 influence the effects of inflammation through vasoconstriction/dilation, pain sensitivity, and platelet aggregation. Des-ciclesonide also affects the promoter of annexin-1, an important inflammatory protein as it affects leukocytes and blocks phospholipase A2 which reduces the amount of arachidonic acid being cleaved from the phospholipid bilayer. Reducing the amount of arachidonic acid formed further decreases the concentrations of prostanoids mentioned calming inflammation. Ciclesonide is administered as an inhaler or as a nasal spray.

Ciclesonide Pathway References