Drug intelligence / Profile preview

tacrolimus + methylprednisolone aceponate

Development stage
Unknown
Lead developer
Astellas Pharma
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Topical
01

Overview

Tacrolimus + methylprednisolone aceponate is a topical combination therapy consisting of tacrolimus, a calcineurin inhibitor immunosuppressant, and methylprednisolone aceponate, a synthetic glucocorticoid corticosteroid. Tacrolimus acts by inhibiting calcineurin-dependent T-cell activation and cytokine release, thereby reducing inflammation. Methylprednisolone aceponate exerts anti-inflammatory effects through glucocorticoid receptor agonism, suppressing multiple inflammatory genes involved in immune response. This combination has been studied for the treatment of chronic plaque-type psoriasis and atopic dermatitis; however, clinical studies indicate that the combination does not provide significant additive benefit over monotherapy with methylprednisolone aceponate alone[1][2][9]. Both agents are well-established as topical treatments for inflammatory skin diseases.

Other names
tacrolimus and methylprednisolone aceponateFK506 + MPA
02

Targets

GR (Glucocorticoid receptor)CN (Calcineurin)

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