Preferred Label : Pan-mutant-selective PI3K-alpha Inhibitor RLY-2608;
NCIt synonyms : Pan-mutant PIK3CA-selective Inhibitor RLY-2608; Pan-mutant PI3Ka Inhibitor RLY-2608; Mutant-selective PI3Ka Inhibitor RLY-2608; PI3Ka Inhibitor RLY-2608;
NCIt 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.;
Molecule name : RLY 2608; RLY-2608;
NCI Metathesaurus CUI : CL1778828;
Origin ID : C186533;
UMLS CUI : C5576916;
Semantic type(s)
- concept_is_in_subset
- has_target
