Mapatumumab (HGS-ETR1) is a fully human agonistic monoclonal antibody targeting TNF-related apoptosis-inducing ligand receptor 1, with anticancer activity, capable of inducing apoptosis in cancer cells.

TNFRSF10A/TRAILR1 (human):17.21 ng/mL (EC50)

Mapatumumab (0.01-100 μg/mL) showed very limited activity against 23 cell lines of PPTP cultured in vitro, with no cell lines achieving 50% growth inhibition. [1]
Mapatumumab (1-100 ng/ml) and EPI (0.1-10 μg/ml) treated bladder cancer cells for 24 h, and showed significantly enhanced cytotoxicity and synergistic effect.
Mapatumumab (100 ng/ml) does not activate T24 cells casapse-8, casapse-9 and casapse-3. [2]

Mapatumumab (10 mg/kg intrperitoneally administered twice weekly for six weeks), two neuroblastoma xenotransplantation models (NB-1643 and NB-SD) showed excessive toxicity. [1]