Serabelisib

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable inhibitor of the class I phosphoinositide 3-kinase (PI3K) alpha isoform with potential antineoplastic activity. Serabelisib selectively inhibits PI3K alpha kinase, including mutations of PIK3CA, in the PI3K/Akt/mTOR pathway, which may result in tumor cell apoptosis and growth inhibition in PI3K alpha-expressing tumor cells. By specifically targeting class I PI3K alpha, this agent may be more efficacious and less toxic than pan PI3K inhibitors. Dysregulation of the PI3K/Akt/mTOR pathway is frequently found in solid tumors and results in promoting tumor cell growth, survival, and resistance to chemotherapy and radiotherapy; PIK3CA, one of the most highly mutated oncogenes, encodes the p110-alpha catalytic subunit of the class I PI3K.

**Synonyms:** - (6-(2-Amino-5-benzoxazolyl)imidazo(1,2-a)pyridin-3-yl)-4-morpholinylmethanone - INK1117 - MLN-1117 - MLN1117 - SERABELISIB - TAK 117 - TAK-117