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Melanoma Ontology
Preferred Name | Cobimetinib | |
Synonyms |
COBIMETINIB Cobimetinib MEK Inhibitor GDC-0973 Cotellic GDC-0973 XL518 |
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Definitions |
An orally bioavailable small-molecule inhibitor of mitogen-activated protein kinase kinase 1 (MAP2K1 or MEK1), with potential antineoplastic activity. Cobimetinib specifically binds to and inhibits the catalytic activity of MEK1, resulting in inhibition of extracellular signal-related kinase 2 (ERK2) phosphorylation and activation and decreased tumor cell proliferation. Preclinical studies have demonstrated that this agent is effective in inhibiting the growth of tumor cells bearing a B-RAF mutation, which has been found to be associated with many tumor types. A threonine-tyrosine kinase and a key component of the RAS/RAF/MEK/ERK signaling pathway that is frequently activated in human tumors, MEK1 is required for the transmission of growth-promoting signals from numerous receptor tyrosine kinases. |
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ID |
http://purl.obolibrary.org/obo/NCIT_C68923 |
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Accepted_Therapeutic_Use_For |
unresectable or metastatic melanoma with BRAF V600E or V600K mutation
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code |
C68923
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Contributing_Source |
CTRP FDA
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definition |
An orally bioavailable small-molecule inhibitor of mitogen-activated protein kinase kinase 1 (MAP2K1 or MEK1), with potential antineoplastic activity. Cobimetinib specifically binds to and inhibits the catalytic activity of MEK1, resulting in inhibition of extracellular signal-related kinase 2 (ERK2) phosphorylation and activation and decreased tumor cell proliferation. Preclinical studies have demonstrated that this agent is effective in inhibiting the growth of tumor cells bearing a B-RAF mutation, which has been found to be associated with many tumor types. A threonine-tyrosine kinase and a key component of the RAS/RAF/MEK/ERK signaling pathway that is frequently activated in human tumors, MEK1 is required for the transmission of growth-promoting signals from numerous receptor tyrosine kinases.
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Display_Name |
Cobimetinib
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FDA_UNII_Code |
ER29L26N1X
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has exact synonym |
COBIMETINIB Cobimetinib MEK Inhibitor GDC-0973 Cotellic GDC-0973 XL518
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imported from | ||
in_subset |
http://purl.oboInOwllibrary.org/oboInOwl/NCIT_C116977 http://purl.oboInOwllibrary.org/oboInOwl/NCIT_C116978 http://purl.oboInOwllibrary.org/oboInOwl/NCIT_C63923 http://purl.oboInOwllibrary.org/oboInOwl/NCIT_C157711 |
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label |
Cobimetinib
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Legacy_Concept_Name |
MEK_Inhibitor_XL518
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PDQ_Closed_Trial_Search_ID |
551654
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PDQ_Open_Trial_Search_ID |
551654
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Preferred_Name |
Cobimetinib
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prefixIRI |
NCIT:C68923
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prefLabel |
Cobimetinib
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Semantic_Type |
Pharmacologic Substance
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UMLS_CUI |
C2346910
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subClassOf |
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