Definition of Pimecrolimus

A 33-epi-chloro-derivative of the ascomycin macrolactam with immunosuppressant property. Pimecrolimus binds to the receptor macrophilin-12 (FKBP-12) forming a complex that blocks the calcium-dependent signal transduction cascade mediated by calcineurin. Via dephosphorylation, calcineurin is the enzyme responsible for activating nuclear factor of activated T-cells (NF-AT), a T cell transcriptional regulatory factor. As a consequence, the synthesis and release of Th1- (T helper 1) and Th2- (T helper 2) type cytokines, and other inflammatory mediators from T-cells and mast cells are blocked and the expression of signals essential for the activation of inflammatory T-lymphocytes is inhibited. However, pimecrolimus mode of action is cell-selective and does not affect Langerhans’ cells/dendritic cells and primary fibroblasts.

Pimecrolimus is from the group

Immunosuppressant

Other Names for Pimecrolimus

Pimecrolimus
15,19-Epoxy-3H-pyrido(2,1-c)(1,4)oxaazacyclotricosine-1,7,20,21(4H,23H)-tetrone, 3-((1E)-2-((1R,3R,4S)-4-chloro-3-methoxycyclohexyl)-1-methylethenyl)-8-ethyl-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-14,16-dimethoxy-4,10,12,18-tetramethyl-,(3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS)-
33-epi-Chloro-33-desoxyascomycin
Elidel
PIMECROLIMUS

Source

NCI Thesaurus License

Topics #1-c)(1 #10 #11 #12 #12S #13 #14 #14S #15 #15R #16 #16-dimethoxy-4 #16S #17 #18 #18-tetramethyl- #18R #19 #19-dihydroxy-14 #19-epoxy-3H-pyrido[2 #19R #2:5 #20 #21(4H #23H)-tetrone #24 #26 #26a-hexadecahydro-5 #26aS)- 33-epi-Chloro-33-desoxyascomycin Elidel PIMECROLIMUS #3-((1E)-2-((1R #3R #3S*) #4]oxaazacyclotricosine-1 #4R #4S)-4-chloro-3-methoxycyclohexyl)-1-methylethenyl)-8-ethyl-5 #5S #6 #7 #8 #8R* #9E #Pimecrolimus 15