BEZ235 + everolimus

BEZ235 (dactolisib) is a dual inhibitor of phosphatidylinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR), developed as an oral small molecule for cancer therapy. Everolimus is an mTOR inhibitor that blocks the activity of mTOR, a key protein involved in cell growth and proliferation. The combination of BEZ235 and everolimus targets both PI3K and mTOR pathways to inhibit tumor cell growth more effectively than either agent alone. Preclinical studies showed synergistic antitumor effects with this combination, particularly in overcoming resistance to single-agent mTOR inhibition. Clinical trials have evaluated the safety, tolerability, pharmacokinetics, and preliminary efficacy of this combination in patients with advanced solid tumors such as breast cancer, kidney cancer, non-small cell lung cancer, colon cancer, glioblastoma multiforme, hepatocellular carcinoma (HCC), pancreatic neuroendocrine tumors (pNETs), esophageal cancer, adenoid cystic carcinoma of the larynx, and appendiceal carcinoma[1][3][4]. Both drugs are administered orally.

Brand names

DactolisibAfinitor

Other names

dactolisib + everolimusNVP-BEZ235 + everolimus