Pimecrolimus

Pimecrolimus, like all ascomycins, is an immunophilin ligand, which binds specifically to the cytosolic receptor, immunophilin macrophilin-12.(In Vitro):Pimecrolimus (SDZ-ASM 981) (100 nM) targets T-cells and mast cells and inhibits the production and release of cytokines and other inflammatory mediators, as well as the expression of signals essential for the activation of inflammatory T-lymphocytes.Pimecrolimus acts specifically on cells that are crucial for the effector phase of an inflammatory reaction.Pimecrolimus (10 nM; 3 days) inhibits the polyclonal growth of peripheral blood T cells in murine and human mixed lymphocyte reactions.Pimecrolimus inhibits cytokine IL-2, IL-4, IL-10 and interferon-γ release from T-cell clone CFTS4:3.1 with IC50s of 0.28, 0.3, 0.2 and 0.42 nM, respectively after antigen-specific stimulation.(In Vivo):Pimecrolimus (SDZ-ASM 981) (0-0.4%; topical; 10 μL once) inhibits allergic contact dermatitis in mice and pigs.Pimecrolimus (0-90 mg/kg; p.o. or s.c.; twice or once) potently inhibits allergic contact dermatitis in mice and rats.