Polfermetinib
Term · Oncology and biomedicine · MLC-T-ONC-016138
An orally bioavailable, brain penetrating inhibitor of mitogen-activated protein kinase kinase (MAP2K; MAPKK; MEK), with potential antineoplastic activity. Upon oral administration, polfermetinib specifically targets, binds to and inhibits the catalytic activity of MEK, thereby inhibiting the activation of MEK-dependent effector proteins, including extracellular signal-regulated kinase (ERK), and inhibits the proliferation of tumor cells in which the RAS/RAF/MEK/ERK signaling pathway is overactivated. The threonine/tyrosine protein kinase MEK plays a key role in the RAS/RAF/MEK/ERK signaling pathway, which is frequently upregulated in a variety of tumor cell types and regulates key cellular activities including cell growth, proliferation, survival, differentiation and apoptosis.
| Identifier | MLC-T-ONC-016138 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | MEK inhibitor PF-07799544 |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-016138",
"term": "Polfermetinib",
"field": "Oncology and biomedicine",
"definition": "An orally bioavailable, brain penetrating inhibitor of mitogen-activated protein kinase kinase (MAP2K; MAPKK; MEK), with potential antineoplastic activity. Upon oral administration, polfermetinib specifically targets, binds to and inhibits the catalytic activity of MEK, thereby inhibiting the activation of MEK-dependent effector proteins, including extracellular signal-regulated kinase (ERK), and inhibits the proliferation of tumor cells in which the RAS/RAF/MEK/ERK signaling pathway is overactivated. The threonine/tyrosine protein kinase MEK plays a key role in the RAS/RAF/MEK/ERK signaling pathway, which is frequently upregulated in a variety of tumor cell types and regulates key cellular activities including cell growth, proliferation, survival, differentiation and apoptosis.",
"synonyms": [
"MEK inhibitor PF-07799544"
],
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/polfermetinib/"
}
Record 13,407 of 17,717 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.