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Margetuximab (HER2)


Margetuximab is an Fc-optimized monoclonal antibody that targets the human epidermal growth factor receptor 2, or HER2. HER2 is expressed on tumor cells in breast, gastric and other types of solid tumors, making it a key target for biologic therapy. Margetuximab is currently being studied as a potential treatment for metastatic breast cancer and advanced gastric cancer. In November 2018, Zai Lab obtained regional development and commercialization rights of margetuximab in mainland China, Hong Kong (China), Macau (China) and Taiwan region from MacroGenics Inc. In February 2019, our partner MacroGenics announced positive results from its pivotal Phase 3 SOPHIA study of margetuximab which improved progression-free survial (PFS) compared to HERCEPTIN, when used in combination with chemotherapy in patients with advanced HER2+ metastatic breast cancer. MacroGenics expects a BLA submission in 2H 2019.

Mechanism of Action

Margetuximab is believed to mediate its therapeutic activity against HER2+ tumors by acombination of mechanisms including:

  • Modulation of HER2 signaling, resultingin growth retardation or the induction of apoptosis, or cell death;
  • Enhanced ADCC through increased binding of margetuximab to immune cells that bear type III Fcgreceptors leading to destruction of HER2+ tumor cells.