Drug intelligence / Profile preview

oprozomib + sorafenib

Development stage
Discontinued
Lead developer
Amgen
Modality
Small Molecules
Administration
Oral
01

Overview

**Oprozomib + sorafenib is an investigational oral combination therapy for advanced hepatocellular carcinoma and other solid tumors, comprising two small molecules with distinct mechanisms.** Oprozomib is a next-generation oral proteasome inhibitor that induces cell cycle arrest and apoptosis by blocking proteasomal protein degradation, interfering with the unfolded protein response (UPR), and enhancing ER stress selectively in tumor cells. Sorafenib is an oral multikinase inhibitor that targets RAF, vascular endothelial growth factor receptors (VEGFR), and platelet-derived growth factor receptor (PDGFR), suppressing tumor angiogenesis and proliferation. This combination has been investigated in phase 1/2 studies for synergistic anti-tumor efficacy, with clinical interest especially in hepatocellular carcinoma[4][5][6][7][8].

Brand names
Nexavar (for sorafenib; no marketed brand name for oprozomib as of 2025)
Other names
oprozomib + sorafenib
02

Targets

FLT3 (Fms related receptor tyrosine kinase 3)PDGFRB (Platelet-derived growth factor receptor beta)PSMB5 (Proteasome subunit beta Type-5)RAF1 (c-Raf-1 (Y340D/Y341D))VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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