NCIt definition : An orally bioavailable inhibitor of the class I phosphatidylinositol 3-kinase (PI3K)
alpha isoform (PIK3CA), with potential antineoplastic activity. Taselisib selectively
inhibits PIK3CA and its mutant forms in the PI3K/Akt/mTOR pathway, which may result
in tumor cell apoptosis and growth inhibition in PIK3CA-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 causes increased tumor cell growth, survival,
and resistance to both chemotherapy and radiotherapy. PIK3CA, which encodes the p110-alpha
catalytic subunit of the class I PI3K, is mutated in a variety of cancer cell types
and plays a key role in cancer cell growth and invasion.;