cobimetinib fumarate
Term · Oncology and biomedicine · MLC-T-ONC-001871
A drug used alone to treat adults with a group of blood disorders called histiocytic neoplasms and with vemurafenib to treat adults with melanoma that has spread or cannot be removed by surgery and has a certain mutation (change) in the BRAF gene. It is also being studied in the treatment of other types of cancer. Cobimetinib fumarate blocks proteins called MEK1 and MEK2, which may help keep tumor cells from growing. It is a type of kinase inhibitor. Also called Cotellic.
The fumarate salt of 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.
| Identifier | MLC-T-ONC-001871 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | Cotellic |
| References | NCI Dictionary of Cancer Terms; National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-001871",
"term": "cobimetinib fumarate",
"field": "Oncology and biomedicine",
"definitions": [
"A drug used alone to treat adults with a group of blood disorders called histiocytic neoplasms and with vemurafenib to treat adults with melanoma that has spread or cannot be removed by surgery and has a certain mutation (change) in the BRAF gene. It is also being studied in the treatment of other types of cancer. Cobimetinib fumarate blocks proteins called MEK1 and MEK2, which may help keep tumor cells from growing. It is a type of kinase inhibitor. Also called Cotellic.",
"The fumarate salt of 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."
],
"synonyms": [
"Cotellic"
],
"references": [
"NCI Dictionary of Cancer Terms",
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/cobimetinib-fumarate/"
}
Record 5,049 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.