Buparlisib

Buparlisib (INN, codenamed BKM120) is an investigational small molecule orally-available pan-class I phosphoinositide 3-kinase inhibitor. Buparlisib (INN, codenamed BKM120) is an investigational small molecule orally-available pan-class I phosphoinositide 3-kinase inhibitor. In December 2015 it is reporting results for the phase III BELLE-2 clinical trial for advanced HR+/HER2 endocrine-resistant breast cancer.Encouraging results are reported in some sub-populations — e.g., some PI3K mutations. A Phase Ib clinical trial combined buparlisib and letrozole in the treatment of estrogen receptor-positive/human epidermal growth factor receptor 2-negative metastatic cancer. Results indicated that the drug combination was safe on two different treatment schedules and the clinical benefit rate was 31%. Common toxicities included hyperglycemia, nausea, fatigue, transaminitis, and mood disorders, though the toxicities are reversible and well-tolerated.