PI3K-alpha inhibitor TOS-358

{
  "id": "MLC-T-ONC-016039",
  "term": "PI3K-alpha inhibitor TOS-358",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable, covalent inhibitor of class I phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K) catalytic subunit alpha (PIK3CA; PI3K p110alpha), with potential antineoplastic activity. Upon oral administration, PI3K-alpha inhibitor TOS-358 selectively targets, binds to and covalently inhibits wild-type PIK3CA and its mutated forms in the PI3K/Akt (protein kinase B)/mammalian target of rapamycin (mTOR) pathway. This results in both apoptosis and growth inhibition in PIK3CA-expressing tumor cells. By specifically targeting PIK3CA, this agent may be more efficacious and less toxic than pan-PI3K inhibitors. 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": [
    "PI3Kalpha inhibitor TOS-358"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/pi3k-alpha-inhibitor-tos-358/"
}