loading...| Preferred Name |
Pimecrolimus |
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| Synonyms |
|
|
| Definitions |
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. |
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| ID |
http://purl.obolibrary.org/obo/NCIT_C47671 |
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| CAS_Registry |
137071-32-0 |
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| Chemical_Formula |
C43H68ClNO11 |
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| code |
C47671 |
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| Contributing_Source |
FDA |
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| definition |
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. |
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| FDA_UNII_Code |
7KYV510875 |
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| in_subset | ||
| label |
Pimecrolimus |
|
| Legacy Concept Name |
Pimecrolimus |
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| NCI_Drug_Dictionary_ID |
711800 |
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| PDQ_Closed_Trial_Search_ID |
711800 |
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| PDQ_Open_Trial_Search_ID |
711800 |
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| Preferred_Name |
Pimecrolimus |
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| prefixIRI |
NCIT:C47671 |
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| prefLabel |
Pimecrolimus |
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| Semantic_Type |
Pharmacologic Substance |
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| UMLS_CUI |
C1099414 |
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| subClassOf |