Drug intelligence / Profile preview

tacrolimus + pimecrolimus

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

Overview

Tacrolimus and pimecrolimus are topical calcineurin inhibitors used primarily as second-line agents for the treatment of atopic dermatitis, especially when traditional therapies such as emollients and low-dose corticosteroids are ineffective or contraindicated. Both drugs act by binding to immunophilins (FKBP12), inhibiting the calcium-dependent phosphatase calcineurin, which leads to suppression of T-cell activation and reduced production of pro-inflammatory cytokines. Tacrolimus is generally indicated for moderate-to-severe eczema, while pimecrolimus is used for mild-to-moderate cases. These agents help control inflammation without causing skin atrophy associated with long-term steroid use[1][4][5][6][8].

Brand names
Protopic (tacrolimus)Elidel (pimecrolimus)
Other names
topical calcineurin inhibitors
02

Targets

PPP3CA (Protein phosphatase 3 catalytic subunit alpha)FKBP1A

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