MLchartDataset catalogue

mutant-selective PI3K-alpha inhibitor BPI-21668

Term · Oncology and biomedicine · MLC-T-ONC-015375

An orally bioavailable, small molecule inhibitor of the class I phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K) catalytic subunit alpha (PIK3CA; PI3K p110alpha) mutant(s), with potential antineoplastic activity. Upon oral administration, PI3K-alpha inhibitor BPI-21668 selectively targets, binds to and inhibits the activity of PIK3CA mutant(s), in the PI3K/Akt (protein kinase B)/mammalian target of rapamycin (mTOR) pathway. This results in both apoptosis and growth inhibition in PIK3CA mutant-expressing tumor cells. Dysregulation of the PI3K/Akt/mTOR pathway is often found in solid tumors and results in the promotion of tumor cell growth, survival, and resistance to chemo- and radio-therapy. PIK3CA, one of the most frequently mutated oncogenes, encodes the p110-alpha catalytic subunit of the class I PI3K.

Table 1. Record
IdentifierMLC-T-ONC-015375
FieldOncology and biomedicine
SynonymsPI3K-alpha inhibitor BPI-21668; PIK3CA inhibitor BPI-21668
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-015375",
  "term": "mutant-selective PI3K-alpha inhibitor BPI-21668",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable, small molecule inhibitor of the class I phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K) catalytic subunit alpha (PIK3CA; PI3K p110alpha) mutant(s), with potential antineoplastic activity. Upon oral administration, PI3K-alpha inhibitor BPI-21668 selectively targets, binds to and inhibits the activity of PIK3CA mutant(s), in the PI3K/Akt (protein kinase B)/mammalian target of rapamycin (mTOR) pathway. This results in both apoptosis and growth inhibition in PIK3CA mutant-expressing tumor cells. Dysregulation of the PI3K/Akt/mTOR pathway is often found in solid tumors and results in the promotion of tumor cell growth, survival, and resistance to chemo- and radio-therapy. PIK3CA, one of the most frequently mutated oncogenes, encodes the p110-alpha catalytic subunit of the class I PI3K.",
  "synonyms": [
    "PI3K-alpha inhibitor BPI-21668",
    "PIK3CA inhibitor BPI-21668"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/mutant-selective-pi3k-alpha-inhibitor-bpi-21668/"
}

Record 11,465 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.