loading...| Preferred Name |
pimecrolimus cream |
|
| Synonyms |
Elidel 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 |
|
| Definitions |
A 33-epi-chloro-derivative of the ascomycin macrolactam with immunosuppressant properties. 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. Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C47671" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C47671" NCI Thesaurus) |
|
| ID |
http://purl.bioontology.org/ontology/PDQ/CDR0000711800 |
|
| altLabel |
Elidel 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 |
|
| CAS Registry |
137071-32-0 |
|
| cui |
C1099414 C0971833 |
|
| DATE FIRST PUBLISHED |
2011-09-12 |
|
| definition |
A 33-epi-chloro-derivative of the ascomycin macrolactam with immunosuppressant properties. 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. Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C47671" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C47671" NCI Thesaurus) |
|
| LT |
TRD |
|
| NCI ID |
C47671 |
|
| notation |
CDR0000711800 |
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| ORIG STY |
Drug/agent |
|
| prefLabel |
pimecrolimus cream |
|
| tui |
T109 T121 |