Drug intelligence / Profile preview

mapatumumab + sorafenib

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

Overview

Mapatumumab + sorafenib is a combination therapy of mapatumumab, a fully human agonistic monoclonal antibody targeting tumor necrosis factor-related apoptosis-inducing ligand receptor 1 (TRAIL-R1), and sorafenib, a small molecule multikinase inhibitor. Mapatumumab induces apoptosis in tumor cells via TRAIL-R1 activation, while sorafenib inhibits multiple kinases involved in tumor proliferation and angiogenesis (notably RAF kinases, VEGFR, and PDGFR). This combination was investigated primarily for treatment of advanced hepatocellular carcinoma but did not demonstrate significant efficacy benefit over sorafenib alone in clinical trials[1][2][5][7][8].

02

Targets

FLT3 (Fms related receptor tyrosine kinase 3)VEGFR (VEGFR family)PDGFRA (Platelet-derived growth factor receptor alpha)TNFRSF10A (Death receptor 4)RET (Rearranged during transfection receptor tyrosine kinase)RAF1 (c-Raf-1 (Y340D/Y341D))

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