Drug intelligence / Profile preview

mapatumumab + bortezomib

Development stage
Preclinical
Lead developer
GSK
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous
01

Overview

Mapatumumab + bortezomib is a **combination therapy composed of mapatumumab, a fully human monoclonal antibody targeting tumor necrosis factor-related apoptosis-inducing ligand receptor 1 (TRAIL-R1), and bortezomib, a small molecule proteasome inhibitor.** Mapatumumab activates TRAIL-R1, inducing apoptosis in cancer cells through the extrinsic apoptotic pathway, while bortezomib disrupts cellular protein degradation pathways by inhibiting the 26S proteasome, leading to accumulation of misfolded proteins, apoptosis, and increased tumor cell immunogenicity. The combination was investigated primarily for the treatment of **relapsed or refractory multiple myeloma**, showing that while it can induce cell apoptosis and an immune response, it did not improve clinical outcomes over bortezomib alone in phase II trials. Mapatumumab was developed by Human Genome Sciences.

Other names
mapatumumab and bortezomib combination
02

Targets

TNFRSF10A (Death receptor 4)26S proteasome

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