Drug intelligence / Profile preview

capecitabine + margetuximab

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

Overview

Capecitabine + margetuximab is a combination regimen used primarily for the treatment of metastatic HER2-positive breast cancer. Capecitabine is an oral prodrug of 5-fluorouracil (5-FU), functioning as an antimetabolite that interferes with DNA synthesis in rapidly dividing cells, leading to cell death. Margetuximab is a chimeric, Fc-engineered monoclonal antibody targeting the extracellular domain of the human epidermal growth factor receptor 2 (HER2). It binds to HER2-overexpressing tumor cells and enhances immune-mediated cytotoxicity by increasing affinity for activating Fcγ receptors on immune effector cells, thereby promoting antibody-dependent cellular cytotoxicity (ADCC). This combination is indicated for patients who have received two or more prior anti-HER2 regimens, at least one in the metastatic setting[2][5][6]. The regimen aims to shrink tumor size and alleviate symptoms but is not curative[2].

02

Targets

FCGR2B (Fc gamma receptor IIB)FCGR3A (Low affinity immunoglobulin gamma Fc region receptor III-A)ERBB2 (Erb-b2 receptor tyrosine kinase 2)TS (Thymidylate synthase)

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