Drug intelligence / Profile preview

firsekibart + tislelizumab + lenvatinib

Development stage
Unknown
Lead developer
Innovent Biologics
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

This combination therapy is an investigational regimen comprising firsekibart (a CD47-targeted monoclonal antibody), tislelizumab (a PD-1-targeted monoclonal antibody), and lenvatinib (a multi-kinase inhibitor). It is being evaluated for the treatment of advanced, unresectable hepatocellular carcinoma (HCC), particularly in patients with TP53 mutations who have progressed after prior PD-1/PD-L1-based immunotherapy. Firsekibart blocks the CD47-SIRPα interaction, an immune checkpoint that inhibits phagocytosis, thereby promoting the clearance of tumor cells by macrophages. Tislelizumab restores T-cell-mediated anti-tumor immunity by blocking the PD-1 receptor. Lenvatinib inhibits multiple receptor tyrosine kinases involved in angiogenesis and tumor growth, including VEGFR1-3, FGFR1-4, PDGFRα, KIT, and RET. The combination aims to overcome resistance to standard immunotherapy by simultaneously targeting innate and adaptive immune checkpoints while inhibiting tumor vascularization and proliferation.

Other names
IBI188 + BGB-A317 + E7080
02

Targets

CD47 (Cluster of Differentiation 47)FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)FGFR4 (Fibroblast growth factor receptor 4)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR4 (Vascular endothelial growth factor Receptor-3)VEGFR2 (Vascular endothelial growth factor receptor 2)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDCD1 (Programmed cell death protein 1 receptor)PDGFRA (Platelet-derived growth factor receptor alpha)RET (Rearranged during transfection receptor tyrosine kinase)

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