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.
| Identifier | MLC-T-ONC-015375 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | PI3K-alpha inhibitor BPI-21668; PIK3CA inhibitor BPI-21668 |
| References | National 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.