Margetuximab (MGAH22) is a chimeric anti-HER2 monoclonal antibody optimized Fc domain, with an EC50 value of 39.33 ng/mL. Margetuximab can be used for researching metastatic HER2-positive breast cancer[1].
Margetuximab (MGAH22) enhances the antibody-dependent cell-mediated cytotoxicity activity of effector cells expressing the CD16A-158F variant[1].
Cell Proliferation Assay
| Cell Line: | JIMT-1, MCF-7, ZR-75-1, SKBR-3, HT-29, SW750 and N87[1] |
| Concentration: | 0.001-1000 ng/mL |
| Incubation Time: | 6 days |
| Result: | Enhances the antibody-dependent cell-mediated cytotoxicity activity of effector cells expressing the CD16A-158F variant. |
Margetuximab (2-4 mg/kg; IP 5 or 6 times at weekly) can firstly and significantly reduces the tumor size at day 30 - 37 in mice model[1].
Margetuximab (15-150 mg/kg; IV; 6 weekly) exhibits well tolerated in cynomolgus monkeys, decreases NK cells by an average of 51%, and induces IL-6 release[1].
Margetuximab (50 mg/kg; IV; single dosage) exhibits favorable safety profile[1].
Pharmacokinetic Parameters of Margetuximab in cynomolgus monkeys[1].
| Male, IV (50 mg/kg) | Female, IV (50 mg/kg) | |
| Cmax (mg/mL) | 1.62 ± 0.10 | 1.70 ± 0.14 |
| AUC0-¥ (mg.hour/mL) | 294.1 ± 53.2 | 314.2 ± 31.3 |
| T1/2β (days) | 9.3 ± 1.8 | 9.7 ± 1.1 |
| Clearance (mL/hour) | 0.43 ± 0.07 | 0.40 ± 0.04 |
| VSS (mL) | 132 ± 2 | 127 ± 8 |
[1]. Nordstrom JL, et al. Anti-tumor activity and toxicokinetics analysis of MGAH22, an anti-HER2 monoclonal antibody with enhanced Fcγ receptor binding properties. Breast Cancer Res. 2011;13(6):R123. doi:10.1186/bcr3069