alpelisib + cetuximab

A combination of the **small molecule** PI3Kα inhibitor **alpelisib** and the **monoclonal antibody** **cetuximab** is under investigation, primarily for recurrent or metastatic squamous cell carcinoma of the head and neck (HNSCC), especially in patients with resistance to prior cetuximab therapy. Alpelisib inhibits the PI3K/AKT/mTOR pathway, which is often activated in cancers that develop resistance to EGFR inhibitors such as cetuximab. Cetuximab is a monoclonal antibody targeting the epidermal growth factor receptor (EGFR), blocking downstream growth and survival signaling. The combination is being tested for possible synergistic activity to overcome resistance to cetuximab through dual pathway inhibition[2][3][5]. Primary indications: investigational therapy for recurrent/metastatic, platinum-resistant, and/or cetuximab-resistant HNSCC, with doses studied up to 300 mg alpelisib daily plus standard cetuximab[2][4]. Key mechanisms: inhibition of EGFR and PI3Kα signaling pathways.

Other names

alpelisib and cetuximab combination