Mapatumumab

Mapatumumab (HGS-ETR1) is a fully human agonistic monoclonal antibody targeting the TNF-related apoptosis-inducing ligand receptor 1 (TRAIL-R1). Mapatumumab exhibits anticancer activity, primarily by inducing tumor cell death through the activation of the death receptor-mediated apoptosis pathway. Mapatumumab is intended for use in cancer research.

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

Mapatumumab (0.01–100 μg/mL) exhibited very limited activity against 23 PPTP cell lines cultured in vitro; none of the cell lines showed 50% growth inhibition. [1]
Treatment of bladder cancer cells with Mapatumumab (1–100 ng/mL) and EPI (0.1–10 μg/mL) for 24 hours significantly enhanced cytotoxicity and demonstrated synergistic effects.
Mapatumumab (100 ng/mL) does not activate caspase-8, caspase-9, or caspase-3 in T24 cells. [2]
Methods: Colorectal cancer (Colo205, HCT116), non-small cell lung cancer (H2122), and renal cancer cells (A498) were treated with Mapatumumab (0.01, 0.1, 1, 10, 100 μg/mL) for 48 h, and cell viability was assessed using CellTiter-Glo; Caspase-3/7 activity was detected using a fluorescence assay.
Results: Mapatumumab specifically binds to TRAIL-R1, dose-dependently inhibits tumor cell viability, and activates both intrinsic and extrinsic apoptotic pathways.[4]

Mapatumumab (10 mg/kg, intraperitoneal administration, twice weekly for six weeks) demonstrated excessive toxicity in two neuroblastoma xenograft models (NB-1643 and NB-SD). [1]
Methods: A Colo205 colorectal cancer NMRI-nu/nu nude mouse xenograft model was established; When tumor volume reached 115 ± 29 mm³, Mapatumumab was administered intraperitoneally at 10 mg/kg (on days 1, 4, and 8), combined with fractionated radiotherapy (5 × 3 Gy on days 1–5) plus a gradient boost of 0–44.2 Gy on day 8. The study was conducted under both normoxic and hypoxic conditions, with a 270-day follow-up. Tumor volume was monitored using a caliper, and the local tumor control rate was calculated.
Results: The combination of Mapatumumab and radiotherapy significantly prolonged the tumor doubling time and substantially improved the local tumor control rate, with no obvious acute toxicity and good safety. [3]
Methods: Nude mouse xenograft models were established using Colo205 (colorectal cancer), H2122 (NSCLC), and A498 (renal cell carcinoma). When tumor volume reached 100 mm³, Mapatumumab (2.5, 10 mg/kg) was administered intravenously, and tumor volume was monitored using a caliper.
Results: Mapatumumab monotherapy significantly induced tumor regression and inhibited tumor growth; the 10 mg/kg dose group demonstrated highly significant antitumor effects.[4]

Human

Monoclonal

Unconjugated