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fluticasone propionate + pimecrolimus

Development stage
Discontinued
Lead developer
GSK
Modality
Small Molecules
Administration
Topical
01

Overview

A combination therapy that pairs two distinct medications for treating inflammatory skin conditions, particularly atopic dermatitis (eczema). Fluticasone propionate is a synthetic fluorinated corticosteroid classified as a medium potency topical corticosteroid. It works through activation of glucocorticoid receptors to reduce inflammation, itching, and redness in skin conditions[3][7]. Pimecrolimus is a topical calcineurin inhibitor that works by binding to macrophilin-12 (FKBP-12) and inhibiting calcineurin, a calcium-dependent phosphatase. This inhibits T cell activation by blocking the transcription of early cytokines, particularly interleukin-2, interferon gamma, interleukin-4, and interleukin-10. It also prevents the release of inflammatory cytokines and mediators from mast cells[2][8]. When used in combination, these medications target different pathways in the inflammatory process. However, clinical studies have shown that adding pimecrolimus to once-daily fluticasone propionate treatment confers no short-term therapeutic benefit in the treatment of severe atopic dermatitis compared to fluticasone propionate alone[1].

02

Targets

GR (Glucocorticoid receptor)FKBP1ACN (Calcineurin)

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