alpelisib + capecitabine

Alpelisib + capecitabine is an investigational oral combination therapy consisting of alpelisib, a selective phosphatidylinositol 3-kinase catalytic subunit alpha (PI3Kα) inhibitor, and capecitabine, an oral prodrug of 5-fluorouracil (5-FU). Alpelisib inhibits the PI3K/AKT/mTOR signaling pathway by selectively targeting the p110α isoform of PI3K, which is frequently mutated in various cancers and associated with tumor growth and resistance to therapy. Capecitabine is converted to 5-FU in tumor tissues, where it interferes with DNA synthesis by inhibiting thymidylate synthase. The combination aims to overcome chemotherapy resistance mediated by PI3K pathway activation and has shown tolerability and preliminary antitumor activity in phase I/II studies for advanced solid tumors including metastatic breast cancer (HER2-negative) and PIK3CA-mutant metastatic colorectal cancer[1][2][4][5].

Other names

alpelisib + capecitabineBYL719 + capecitabine