Enoblituzumab (MGA271) is a humanized IgG1κ monoclonal antibody recognizing human B7-H3 protein, a member of the B7 family of immune regulators[1].
Enoblituzumab interacts with B7-H3 and causes strong antibody-dependent cellular cytotoxicity (ADCC) against a wide spectrum of cancer cells[2].
Enoblituzumab (0.01 ng/mL-10 mg/mL) mediates antibody-dependent cellular cytotoxicity (ADCC) against A498 cells with cynomolgus monkey peripheral blood mononuclear cells (PBMCs)[3].
Enoblituzumab (5 mg/kg; i.v.; single dose) exhibits estimated half-life of 249 hours with a Cmax of 43 mg/mL in mice (mCD16-/-hCD16A+) that murine CD16 gene knocked out and are transgenic for human CD16A-158F[3].
Enoblituzumab (0.1-10 mg/kg; i.v.; once weekly; 5 weeks) exhibits potent antitumor activity in B7-H3-expressing xenograft mice models of renal cell and bladder carcinoma[3].
| Animal Model: | mCD16-/-hCD16A+ mice implanted with A498 renal cell carcinoma, 786-0 renal cell carcinoma, or HT-1197 bladder carcinoma cells (s.c.)[3] |
| Dosage: | 1 mg/kg, 5 mg/kg, 10 mg/kg |
| Administration: | Intravenous injection; once weekly; 5 weeks |
| Result: | Significantly inhibited tumor growth at doses of 1 mg/kg or greater with once weekly treatment. Achieved a cytostatic response at 5 or 10 mg/kg until day 52, after which the average tumor volume of the 5 mg/kg treatment group remained near predose administration levels, whereas a nonsignificant trend toward relapse exhibited in the 10 mg/kg group. |
[1]. Hińcza-Nowak K, et al. Immune Profiling of Medullary Thyroid Cancer-An Opportunity for Immunotherapy. Genes (Basel). 2021 Sep 28;12(10):1534.
[2]. Chapoval, et al. Immune Checkpoints of the B7 Family. Part 2. Representatives of the B7 Family B7-H3, B7-H4, B7-H5, B7-H6, B7-H7, and ILDR2 and Their Receptors. Russ J Bioorg Chem 45, 321-334 (2019).
[3]. Loo D, et al. Development of an Fc-enhanced anti-B7-H3 monoclonal antibody with potent antitumor activity. Clin Cancer Res. 2012 Jul 15;18(14):3834-45.