Drug intelligence / Profile preview

margetuximab + chemotherapy

Development stage
Unknown
Lead developer
MacroGenics
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous
01

Overview

Margetuximab + chemotherapy is a combination regimen approved for the treatment of HER2-positive metastatic breast cancer in adults who have received at least two prior anti-HER2 regimens, including at least one for metastatic disease. Margetuximab is a chimeric IgG1 monoclonal antibody engineered to bind the extracellular domain of HER2 (human epidermal growth factor receptor 2) with similar affinity as trastuzumab but has an Fc domain optimized for increased antibody-dependent cell-mediated cytotoxicity (ADCC). This is achieved via increased binding to activating Fc gamma receptor IIIA (CD16A) and decreased affinity for inhibitory FcγRIIB (CD32B), enhancing NK cell and macrophage-mediated immune responses. Used in combination with chemotherapy, it blocks HER2-driven cell proliferation and encourages immune-mediated tumor destruction. Developed by MacroGenics, the regimen is administered intravenously, and the chemotherapy agent is selected according to standard clinical options (such as capecitabine, eribulin, gemcitabine, or vinorelbine)[1][2][3][4][5][6].

Other names
margetuximab-cmkb + chemotherapy
02

Targets

FcγRIIIa (Low affinity immunoglobulin gamma Fc region receptor III-A)ERBB2 (Erb-b2 receptor tyrosine kinase 2)FCGR2B (Fc gamma receptor IIB)

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