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National Cancer Institute Thesaurus
| Preferred Name | Cobimetinib | |
| Synonyms |
COBIMETINIB Cobimetinib MEK Inhibitor GDC-0973 Cotellic GDC-0973 XL518 |
|
| 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. |
|
| ID |
http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C68923 |
|
| 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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|
| Concept_In_Subset |
http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C176424 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C157711 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C157712 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C116978 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C201600 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C116977 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C128784 |
|
| Contributing_Source |
CTRP FDA GDC HemOnc
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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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|
| FULL_SYN |
COBIMETINIB Cobimetinib MEK Inhibitor GDC-0973 Cotellic GDC-0973 XL518
|
|
| Has_Salt_Form | ||
| Has_Target | ||
| 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 |
Thesaurus:C68923
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|
| Semantic_Type |
Pharmacologic Substance
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|
| UMLS_CUI |
C2346910
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| subClassOf |
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