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Physician Data Query
| Preferred Name | cobimetinib | |
| Synonyms |
Cotellic XL518 GDC-0973 MEK inhibitor GDC-0973 |
|
| 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. Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C68923" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C68923" NCI Thesaurus) |
|
| ID |
http://purl.bioontology.org/ontology/PDQ/CDR0000551654 |
|
| altLabel |
Cotellic XL518 GDC-0973 MEK inhibitor GDC-0973
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|
| cui |
C4059049 C4049146 C2346910
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|
| DATE FIRST PUBLISHED |
2007-05-21
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| Date last modified |
2015-11-11
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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. Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C68923" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C68923" NCI Thesaurus)
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|
| LT |
TRD
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| NCI ID |
C68923
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|
| notation |
CDR0000551654
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| ORIG STY |
Drug/agent
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|
| prefLabel |
cobimetinib
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|
| tui |
T109 T121
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