Mapatumumab

Mapatumumab (HGS-ETR1) is a fully human IgG1 agonistic monoclonal antibody that targets tumor necrosis factor-related apoptosis-inducing ligand receptor 1 (TRAIL-R1). Mapatumumab can be used for the research of cancer[1].

Research Areas >> Cancer

Signaling Pathways >> Others >> Others

Mapatumumab (0.01-100 μg/mL; 4 h) shows no growth inhibition to Pediatric Preclinical Testing Program (PPTP) cell lines[1]. Mapatumumab (1-100 ng/mL; 24 h) shows significant potentiation of cytotoxicity and synergy when combined with (epirubicin) EPI for bladder cancer cells[2]. Mapatumumab (100 ng/mL; 12 h) induces significant cell apoptosis of T24, 253J and J82 cells with the combination of EPI (1 µg/mL)[2]. Mapatumumab (100 ng/mL; 6-24 h) significantly activates caspase-8, -9 and -3 with the combination of EPI (1 µg/mL)[2].

Mapatumumab (10 mg/kg; i.p. for three times) controls tumor growth when combined with irradiation[3]. Animal Model: Colo205-xenograft–bearing NMRI (nu/nu) nude mice[3] Dosage: 10 mg/kg Administration: Intraperitoneal injection; 10 mg/kg; on days 1, 4, and 8 Result: Showed no significant differences when used alone, but when combined with irradiation (5×3 Gy, d1–5) showed a pronounced tumor regrowth-delay.

[1]. Smith MA, et al. Initial testing (stage 1) of mapatumumab (HGS-ETR1) by the pediatric preclinical testing program. Pediatr Blood Cancer. 2010 Feb;54(2):307-10.

[2]. Ahmed SM, et al. Synergistic induction of apoptosis by mapatumumab and anthracyclines in human bladder cancer cells. Oncol Rep. 2015 Feb;33(2):566-72.  

[3]. Marini P, et al. Combination of the pro-apoptotic TRAIL-receptor antibody mapatumumab with ionizing radiation strongly increases long-term tumor control under ambient and hypoxic conditions. Int J Radiat Oncol Biol Phys. 2009 Sep 1;75(1):198-202.