Margetuximab: First Approval

The second-generation anti-human epidermal growth factor receptor2 protein (HER2) monoclonal antibody margetuximab (MARGENZA (TM), margetuximab-cmkb) is being developed for the treatment of HER2-positive breast cancer, gastric cancer and gastro-oesophageal junction cancer. The antibody has been engineered for increased binding to activating Fc gamma receptor IIIA (CD16A) and decreased binding to inhibitory Fc gamma receptor IIB (CD32B) relative to trastuzumab with the aim of improving response rates. Based on the results of the phase III SOPHIA trial margetuximab has been approved in the USA for use in combination with chemotherapy as treatment of previously-treated metastatic HER2-positive breast cancer. This article summarizes the milestones in the development of margetuximab leading to this first approval.

Automated summary

Margetuximab, a second-generation anti-HER2 monoclonal antibody, has been approved in the USA for the treatment of previously-treated metastatic HER2-positive breast cancer, based on its improved binding to activating Fc gamma receptor IIIA and reduced binding to inhibitory Fc gamma receptor IIB, aiming to enhance response rates.