margetuximab

Margetuximab is a chimeric IgG1κ monoclonal antibody engineered to target the extracellular domain of the human epidermal growth factor receptor 2 (HER2). It is derived from the same mouse 4D5 clone as trastuzumab but features an Fc-engineered region that increases its affinity for activating FcγRIIIA (CD16A) receptors and decreases binding to inhibitory FcγRIIB (CD32B) receptors. This modification enhances antibody-dependent cell-mediated cytotoxicity (ADCC), leading to improved immune-mediated killing of HER2-positive tumor cells, even in patients with low-affinity CD16A alleles or resistance to trastuzumab. Margetuximab inhibits tumor cell proliferation, reduces shedding of the HER2 extracellular domain, and prevents formation of HER2 homodimers and heterodimers with other HER family members. It is approved for use in combination with chemotherapy for adults with metastatic HER2-positive breast cancer who have received at least two prior anti-HER2 regimens.

Brand names

Margenza

Other names

margetuximab-cmkb