Pimecrolimus

Pimecrolimus is an immunomodulating agent used in the treatment of atopic dermatitis (eczema). It is currently available as a topical cream, once marketed by Novartis (however Galderma is promoting the compound in Canada since early 2007) under the trade name Elidel. Pimecrolimus is an ascomycin macrolactam derivative. It has been shown in vitro that pimecrolimus binds to macrophilin-12(also referred to as FKBP-12) and inhibits calcineurin. Thus pimecrolimus inhibits T-cell activation by inhibiting the synthesis and release of cytokines from T-cells. Pimecrolimus also prevents the release of inflammatory cytokines and mediators from mast cells.

Properties:

Appearance & Physical State: white crystalline powder

Density: 1.19

Boiling Point: 866.1ºC at 760 mmHg

Flash Point: 477.6ºC

Refractive Index: 1.543

Vapor Pressure: 5.44E-35mmHg at 25°C

Immunology & Inflammation related Inhibitors Related Prodcuts:

Cyclosporin A; Bestatin; GI254023X; Bindarit; TAPI-1; Avadomide; Thymopentin; Pranlukast; Laquinimod; VGX-1027; Y-320; Imiquimod; Levamisole hydrochloride; Halcinonide; Sodium gualenate; Aceclofenac; Fenoprofen calcium; Pidotimod; Etofenamate; Tenoxicam

[1]. Nghiem, P., G. Pearson, and R.G. Langley, Tacrolimus and pimecrolimus: from clever prokaryotes to inhibiting calcineurin and treating atopic dermatitis. J Am Acad Dermatol, 2002. 46(2): p. 228-41.

[2]. Gupta, A.K. and M. Chow, Pimecrolimus: a review. J Eur Acad Dermatol Venereol, 2003. 17(5): p. 493-503.

[3]. Stuetz, A., M. Grassberger, and J.G. Meingassner, Pimecrolimus (Elidel, SDZ ASM 981)--preclinical pharmacologic profile and skin selectivity. Semin Cutan Med Surg, 2001. 20(4): p. 233-41.