Enoblituzumab

Enoblituzumab (MGA271) is a humanized IgG1κ monoclonal antibody recognizing human B7-H3 protein, a member of the B7 family of immune regulators[1].

Research Areas >> Cancer

Signaling Pathways >> Others >> Others

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.