Pimecrolimus CAS 137071-32-0 

Topical immunomodulators

Pimecrolimus is a topical immunomodulators and is a kind of semi-synthetic products of the

Streptomyces-produced ascomycin. It has a greater lipophilicity than tacrolimus with a stronger

affinity with the skin. It can effectively and safely control the signs and symptoms of facial seborrheic

dermatitis and can quickly relieve the itching symptoms of patients with dermatitis and eczema as well

as reduce the lesion area, clear atopic dermatitis (eczema) sign. Therefore, it is an effective treatment

method for the treatment of atopic dermatitis (eczema) for both early remission purpose and long-term

control purpose. 

Chemical Properties:White Solid

Usage: Pimecrolimus is a semi-synthetic, macrocyclic lactone derived from ascomycin by activation of the

32-hydroxy group with a triflate ester, and nucleophilic substitution with chloride under phase transfer conditions

to provide the chloro analogue. Pimecrolimus has been targeted for treatment of inflammatory skin disorders. Like

all tacrolimus analogues, pimecrolimus binds to receptor protein, FKBP12. The complex then binds to mTOR preventing

it from interacting with target proteins. Pimecrolimus is extensively cited in the literature with over 2,000 citations.

Pimecrolimus is an immunomodulating agent of the calcineurin inhibitor class used in the treatment of atopic dermatitis (eczema).

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.[citation needed] 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.