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Biological and Environmental Research Ontology
| Preferred Name | Cobimetinib | |
| Synonyms |
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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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| CAS_Registry |
934660-93-2
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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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| in_subset |
http://purl.obolibrary.org/obo/NCIT_C63923 http://purl.obolibrary.org/obo/NCIT_C177537 http://purl.obolibrary.org/obo/NCIT_C176424 http://purl.obolibrary.org/obo/NCIT_C116977 http://purl.obolibrary.org/obo/NCIT_C116978 http://purl.obolibrary.org/obo/NCIT_C128784 |
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| Is_Value_For_GDC_Property | ||
| label |
Cobimetinib
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| Legacy Concept Name |
MEK_Inhibitor_XL518
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|
| Maps_To |
Cobimetinib
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| NCI_Drug_Dictionary_ID |
551654
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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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