BYL719 + LEE011 + letrozole

This is a combination therapy consisting of three agents: BYL719 (alpelisib), an oral, α-selective phosphatidylinositol 3-kinase (PI3K) inhibitor; LEE011 (ribociclib), an oral cyclin-dependent kinase 4/6 (CDK4/6) inhibitor; and letrozole, a nonsteroidal aromatase inhibitor. The combination targets multiple pathways implicated in endocrine resistance in hormone receptor-positive, HER2-negative advanced or metastatic breast cancer. Alpelisib inhibits the PI3K pathway by selectively targeting the p110α isoform, ribociclib blocks cell cycle progression by inhibiting CDK4/6-mediated phosphorylation of retinoblastoma protein, and letrozole suppresses estrogen synthesis by inhibiting aromatase. This triplet regimen has been investigated for its potential to enhance antitumor activity compared to single-agent or doublet regimens in ER+ breast cancer[1][2][5].

Brand names

KisqaliPiqrayFemara

Other names

alpelisib + ribociclib + letrozole