PM02734 + erlotinib

PM02734 (also known as elisidepsin or Kahalalide F) is a novel marine-derived cyclic peptide belonging to the Kahalalide family of compounds. It is under early clinical development for cancer therapy and has shown cytotoxic activity in non-small cell lung cancer (NSCLC) cell lines, particularly those with high ErbB3 expression. Erlotinib is an oral small molecule tyrosine kinase inhibitor that targets the epidermal growth factor receptor (EGFR), approved for use in non-small cell lung cancer and pancreatic cancer. The combination of PM02734 and erlotinib has demonstrated synergistic anti-tumor effects in preclinical NSCLC models, including those resistant to erlotinib alone. Mechanistically, this combination more effectively inhibits AKT signaling and induces necrosis-like cell death compared to either agent alone[3][4]. The rationale for combining these agents is based on their complementary mechanisms—PM02734 degrades ErbB3 while erlotinib inhibits EGFR—potentially overcoming resistance pathways in solid tumors.

Other names

Kahalalide F (for PM02734)elisidepsin (for PM02734)