Pimecrolimus

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Background

Pimecrolimus is a cell-selective inhibitor of inflammatory cytokines secretion in T cells and mast cells [1].
Inflammatory cytokines are cytokines which promote systemic inflammation. Pimecrolimus can be used for the treatment of inflammatory skin diseases, such as plaque-type psoriasis, atopic dermatitis, irritant contact dermatitis and allergic contact dermatitis [1].
Pimecrolimus is a cell-selective inflammatory cytokines secretion inhibitor. Pimecrolimus inhibited the secretion of inflammatory cytokines in mast cells and T cells and also inhibited the release of preformed inflammatory mediators from mast cells. Pimecrolimus exhibited a low potential to impair systemic immune reactions in the skin [1]. In peripheral blood leukocytes contained basophil or mast cells, pimecrolimus inhibited histamine release induced by anti-IgE from basophils and mast cells by 82% and 73%, respectively. Also, pimecrolimus inhibited tryptase, LTC4 and TNF-alpha release [2]. In CD4+ T cells stimulated by dendritic cells (DC), pimecrolimus inhibited the up-regulation of CD25 and CD54 and surface expression of OX40. Pimecrolimus inhibited T cell proliferation with IC50 value of 0.55 nM and inhibited the synthesis of IFN-γ and TNF-α [3].
In treatment of allergic contact dermatitis (ACD) mice and rats, pimecrolimus exhibited a higher potency. In atopic dermatitis rats, pimecrolimus effectively reduced pruritus and skin inflammation [1].

[1]. Stuetz A, Grassberger M, Meingassner JG. Pimecrolimus (Elidel, SDZ ASM 981)--preclinical pharmacologic profile and skin selectivity. Semin Cutan Med Surg, 2001, 20(4): 233-241.
[2]. Zuberbier T, Chong SU, Grunow K, et al. The ascomycin macrolactam pimecrolimus (Elidel, SDZ ASM 981) is a potent inhibitor of mediator release from human dermal mast cells and peripheral blood basophils. J Allergy Clin Immunol, 2001, 108(2): 275-280.
[3]. Kalthoff FS, Chung J, Stuetz A. Pimecrolimus inhibits up-regulation of OX40 and synthesis of inflammatory cytokines upon secondary T cell activation by allogeneic dendritic cells. Clin Exp Immunol, 2002, 130(1): 85-92.