loading...| 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://purl.obolibrary.org/obo/NCIT_C68923 |
|
| Accepted_Therapeutic_Use_For |
unresectable or metastatic melanoma with BRAF V600E or V600K mutation |
|
| code |
C68923 |
|
| Contributing_Source |
CTRP FDA |
|
| 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. |
|
| Display_Name |
Cobimetinib |
|
| FDA_UNII_Code |
ER29L26N1X |
|
| has exact synonym |
COBIMETINIB Cobimetinib MEK Inhibitor GDC-0973 Cotellic GDC-0973 XL518 |
|
| 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 |
|
| label |
Cobimetinib |
|
| Legacy_Concept_Name |
MEK_Inhibitor_XL518 |
|
| PDQ_Closed_Trial_Search_ID |
551654 |
|
| PDQ_Open_Trial_Search_ID |
551654 |
|
| Preferred_Name |
Cobimetinib |
|
| prefixIRI |
NCIT:C68923 |
|
| prefLabel |
Cobimetinib |
|
| Semantic_Type |
Pharmacologic Substance |
|
| UMLS_CUI |
C2346910 |
|
| subClassOf |