Preferred Label : Mutant-selective PI3K-alpha H1047X Inhibitor SNV4818;
NCIt synonyms : PIK3CA H1047X Mutant Inhibitor SNV4818; Mutation-selective PI3K-a Inhibitor SNV4818; PI3Ka-H1047X Mutant Inhibitor SNV4818; PIK3CA H1047X Mutation Inhibitor SNV4818;
NCIt definition : An orally bioavailable and selective inhibitor of the class I phosphatidylinositol-4,5-bisphosphate
3-kinase (PI3K) catalytic subunit alpha (phosphoinositide 3-kinase alpha; PIK3CA;
PI3K p110alpha) mutant H1047X, with potential antineoplastic activity. Upon oral administration,
mutant-selective PI3K-alpha H1047X inhibitor SNV4818 selectively targets and binds
to the PIK3CA mutated form PIK3CA H1047X, thereby preventing the activity of the H1047X
mutant. This prevents PIK3CA H1047X-mediated activation of the PI3K/Akt (protein kinase
B)/mammalian target of rapamycin (mTOR) pathway. This results in apoptosis and growth
inhibition in PIK3CA H1047X mutant-expressing tumor cells. By specifically targeting
the PIK3CA H1047X mutation, SNV4818 may be more efficacious and less toxic than other
PI3K-alpha inhibitors that are not mutant specific. 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. SNV4818 may also have selectivity over PIK3CA E542K, E545K and 542X mutant
forms.;
Molecule name : SNV-4818; SNV 4818;
Origin ID : C213670;
concept_is_in_subset
- has_target
