MLchartDataset catalogue

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.

Table 1. Record
IdentifierMLC-T-ONC-016138
FieldOncology and biomedicine
SynonymsMEK inhibitor PF-07799544
ReferencesNational 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.