Preferred Label : PI3K-alpha Inhibitor TOS-358;
NCIt synonyms : PI3Kalpha Inhibitor TOS-358;
NCIt 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.;
Molecule name : TOS 358; TOS-358;
NCI Metathesaurus CUI : CL1905844;
Origin ID : C198692;
concept_is_in_subset
- has_target
