BKM120 + BYL719

**BKM120 + BYL719** is a combination of two small molecule PI3K inhibitors: **BKM120 (buparlisib)**, a pan-PI3K inhibitor targeting all class I PI3K isoforms (α, β, δ, γ), and **BYL719 (alpelisib)**, an α-specific PI3K inhibitor. Developed by **Novartis**, this pairing exploits complementary inhibition of the PI3K/AKT/mTOR pathway, frequently dysregulated in cancers like breast cancer due to PIK3CA mutations. It has been investigated in early-phase trials for advanced solid tumors, including metastatic breast cancer, triple-negative breast cancer (TNBC), and high-grade serous carcinoma (HGSC), often combined with chemotherapy (e.g., capecitabine), HER2-targeted agents (e.g., trastuzumab, lapatinib), hormone therapy (e.g., letrozole), or PARP inhibitors (e.g., olaparib), showing preliminary antitumor activity but limited by toxicities like hyperglycemia and rash.

Other names

buparlisib + alpelisib