pan-mutant-selective PI3K-alpha inhibitor RLY-2608

{
  "id": "MLC-T-ONC-015801",
  "term": "pan-mutant-selective PI3K-alpha inhibitor RLY-2608",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable, pan-mutant selective inhibitor of the class I phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K) catalytic subunit alpha (phosphoinositide 3-kinase alpha; PIK3CA; PI3K p110alpha), with potential antineoplastic activity. Upon oral administration, pan-mutant selective PI3K-alpha inhibitor RLY-2608 selectively targets and allosterically binds to PIK3CA mutated forms, thereby preventing the activity of PIK3CA mutants. This prevents mutant PIK3CA-mediated activation of 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. By specifically targeting PIK3CA mutants, RLY-2608 may be more efficacious and less toxic than PI3K-alpha inhibitors that also inhibit the wild-type (WT) form. 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": [
    "mutant-selective PI3Ka inhibitor RLY-2608",
    "pan-mutant PI3Ka inhibitor RLY-2608",
    "pan-mutant PIK3CA-selective inhibitor RLY-2608",
    "PI3Ka inhibitor RLY-2608"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/pan-mutant-selective-pi3k-alpha-inhibitor-rly-2608/"
}