galunisertib + sorafenib

Galunisertib + sorafenib is an oral **combination regimen** of two small molecule inhibitors being investigated for the treatment of advanced hepatocellular carcinoma (HCC). **Galunisertib** is a selective ATP-mimetic inhibitor of transforming growth factor-beta receptor type I (TGF-βRI), blocking pro-tumorigenic TGF-β signaling pathways involved in cell proliferation, survival, invasion, and immunosuppression. **Sorafenib** is a multi-kinase inhibitor approved for HCC, targeting RAF kinases, vascular endothelial growth factor receptors (VEGFRs), and platelet-derived growth factor receptor (PDGFR), thereby inhibiting tumor cell proliferation and angiogenesis. Preclinical and clinical data have shown that galunisertib can potentiate the antitumor effects of sorafenib by further inhibiting TGF-β signaling, leading to enhanced anti-proliferative and pro-apoptotic activity compared to either monotherapy.

Brand names

Nexavar

Other names

galunisertib and sorafenibgalunisertib plus sorafenib