RAS/PI3K-alpha Inhibitor VVD-159642

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable 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 inhibitor VVD-159642 selectively disrupts the interaction between RAS and PIK3CA, thereby inhibiting RAS-mediated activation of PIK3CA. This results in apoptosis and growth inhibition in PIK3CA-expressing tumor cells. By specifically targeting RAS-mediated activation of the PI3K/Akt/mTOR pathway, VVD-159642 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:** - BAY 3674171 - BAY-3674171 - BAY3674171 - RAS/PI3K-alpha Inhibitor BAY 3674171 - RAS/PI3Ka Inhibitor VVD-159642 - RAS/PIK3CA Inhibitor VVD-159642 - VVD 159642 - VVD-159642 - VVD159642