Mapatumumab (HGS-ETR1) is a fully human IgG1 agonistic monoclonal antibody that exclusively targets and activates tumor necrosis factor-related apoptosis-inducing ligand receptor 1 (TRAIL-R1). It was tested in vitro at concentrations from 0.01 to 100 μg/ml and in vivo at a dose of 10 mg/kg administered intraperitoneally using a twice-weekly schedule. Mapatumumab demonstrated limited activity against the 23 cell lines of the PPTP in vitro panel with no lines achieving 50% growth inhibition. Mapatumumab induced significant differences in event-free survival distribution compared to controls in 9 of 37 evaluable solid tumor xenografts tested, but in none of the 8 ALL xenografts.
Initial testing (stage 1) of mapatumumab (HGS-ETR1) by the pediatric preclinical testing program. / Smith, Malcolm A.; Morton, Christopher L.; Kolb, E. Anders; Gorlick, Richard; Keir, Stephen T.; Carol, Hernan; Lock, Richard; Kang, Min H.; Reynolds, C. Patrick; Maris, John M.; Watkins, Amy E.; Houghton, Peter J.In: Pediatric Blood and Cancer, Vol. 54, No. 2, 01.02.2010, p. 307-310.
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