Drug intelligence / Profile preview

halobetasol + tacrolimus

Development stage
Preclinical
Lead developer
Valeant Pharmaceuticals
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Topical
01

Overview

Halobetasol + tacrolimus is a topical combination therapy consisting of two active pharmaceutical ingredients: halobetasol propionate, a super-potent synthetic corticosteroid, and tacrolimus, a calcineurin inhibitor. Halobetasol acts by binding to the glucocorticoid receptor and modulating gene expression to suppress inflammation, immune responses, and pruritus in various dermatoses[2][10]. Tacrolimus inhibits calcineurin-dependent T-cell activation by blocking the transcription of pro-inflammatory cytokines such as interleukin-2. This dual mechanism targets both inflammatory pathways (via corticosteroid action) and immune-mediated components (via calcineurin inhibition), making the combination potentially useful for steroid-responsive dermatoses where long-term steroid use is limited or for areas prone to atrophy or sensitive skin. While each agent is approved individually for dermatological conditions such as psoriasis and atopic dermatitis, there are no widely recognized fixed-dose commercial products combining these two agents; however, they may be used together off-label in clinical practice.

02

Targets

FKBP1AGR (Glucocorticoid receptor)CN (Calcineurin)

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