Preferred Label : Izorlisib;
NCIt synonyms : PI3Kalpha Inhibitor MEN1611; Alpha-selective PI3K Inhibitor MEN1611; 5-(7-Methylsulfonyl-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-amine; PI3K-alpha Inhibitor MEN1611;
NCIt definition : An orally bioavailable inhibitor of the class I phosphatidylinositol-4,5-bisphosphate
3-kinase (PI3K) catalytic subunit alpha (PIK3CA), with potential antineoplastic activity.
Upon administration, izorlisib selectively binds to and inhibits 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, izorlisib may be more efficacious and less toxic
than pan-PI3K inhibitors. In addition, izorlisib also targets mutated forms of PI3K
gamma (PI3Kg). It may also stimulate the immune system to restore CD8 T-cell activation
and cytotoxicity. 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. In most solid tumors,
the activation of the PI3K pathway is induced by mutations of PIK3CA.;
UNII : JCL936W835;
InChIKey : JEGHXKRHKHPBJD-UHFFFAOYSA-N;
CAS number : 1007207-67-1;
Molecule name : CH-5132799; MEN 1611; MEN-1611; CH 5132799; PA-799; PA 799;
NCI Metathesaurus CUI : CL938076;
Origin ID : C158603;
UMLS CUI : C5706649;
Semantic type(s)
- concept_is_in_subset
- has_target
