Drug intelligence / Profile preview

betamethasone + tacrolimus

Development stage
Unknown
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Topical
01

Overview

Betamethasone + tacrolimus refers to the concomitant or sequential use of the topical corticosteroid betamethasone and the topical calcineurin inhibitor tacrolimus. This therapeutic approach is primarily employed in the treatment of moderate-to-severe atopic dermatitis to achieve rapid anti-inflammatory control with the steroid while utilizing the steroid-sparing properties of tacrolimus for long-term maintenance. Betamethasone binds to the glucocorticoid receptor to modulate gene expression of inflammatory mediators, whereas tacrolimus binds to FKBP-12 to inhibit calcineurin, thereby preventing the dephosphorylation of NFAT and subsequent T-cell activation. Clinical trials, such as those conducted by Cairo University, have explored optimizing this regimen by adding antimicrobial agents like azithromycin to manage secondary infections and further reduce inflammation.

02

Targets

GR (Glucocorticoid receptor)CN (Calcineurin)FKBP1A

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