RAS/PI3K-alpha Interaction Inhibitor BBO-10203

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable covalent small molecule inhibitor of RAS-driven phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PI3K-alpha; PI3Ka; PIK3CA) activity, with potential antineoplastic activity. Upon oral administration, RAS/PI3Ka interaction inhibitor BBO-10203 disrupts the interaction between RAS and PIK3CA, thereby inhibiting PIK3CA in the PI3K/Akt (protein kinase B)/mammalian target of rapamycin (mTOR) pathway. This results in apoptosis and growth inhibition in PIK3CA-expressing tumor cells. By specifically targeting RAS-mediated activation of the PI3K/Akt/mTOR pathway, BBO-10203 may not cause hyperglycemia associated with direct PIK3CA kinase inhibition. 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:** - BBO 10203 - BBO-10203 - BBO10203 - PI3K-alpha:RAS Breaker BBO-10203 - PI3Ka:RAS Breaker BBO-10203 - RAS-driven PI3K-alpha Inhibitor BBO-10203 - RAS/PI3Ka Interaction Inhibitor BBO-10203