pimecrolimus

Modality

small molecule

Mechanism

12.1 Mechanism of Action The mechanism of action of pimecrolimus in atopic dermatitis is not known. While the following have been observed, the clinical significance of these observations in atopic dermatitis is not known. It has been demonstrated that pimecrolimus binds with high affinity to macrophilin-12 (FKBP-12) and inhibits the calcium-dependent phosphatase, calcineurin. As a consequence, it inhibits T-cell activation by blocking the transcription of early cytokines. In particular, pimecrolimus inhibits at nanomolar concentrations Interleukin-2 and interferon gamma (Th1-type) and Interleukin-4 and Interleukin-10 (Th2-type) cytokine synthesis in human T-cells. In addition, pimecrolimus prevents the release of inflammatory cytokines and mediators from mast cells in vitro after stimulation by antigen/IgE.

Targets

Calcineurin, Serine/threonine-protein kinase mTOR

Storage

—

Approved

atopic dermatitis — FDA

In trial

prurigo nodularis, atopic dermatitis, vitiligo

Sources

DailyMed (FDA label)DrugBank ClinicalTrials.gov

Last verified

2026-04-23

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Formulations

1% cream (≥2 y)