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lenvatinib + tislelizumab + capecitabine + oxaliplatin

Development stage
Preclinical
Lead developer
Eisai
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Monoclonal Antibodies → Antibody-Based Therapeutics, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
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Overview

This is a combination regimen consisting of four drugs: - **Lenvatinib** is an oral small molecule multi-kinase inhibitor that targets vascular endothelial growth factor receptors (VEGFR1, VEGFR2, VEGFR3), fibroblast growth factor receptors (FGFR1–4), platelet-derived growth factor receptor alpha (PDGFRα), RET, and KIT. It inhibits angiogenesis and tumor cell proliferation. - **Tislelizumab** is a humanized IgG4 monoclonal antibody that acts as an immune checkpoint inhibitor by binding to programmed death-1 (PD-1) receptor on T cells, blocking its interaction with PD-L1/PD-L2 and enhancing antitumor immune responses. - **Capecitabine** is an oral prodrug of 5-fluorouracil (5-FU), a pyrimidine analog that inhibits thymidylate synthase, leading to impaired DNA synthesis in rapidly dividing tumor cells. - **Oxaliplatin** is a platinum-based chemotherapeutic agent that forms DNA crosslinks and induces apoptosis in cancer cells. This combination brings together targeted therapy (lenvatinib), immunotherapy (tislelizumab), and cytotoxic chemotherapy agents (capecitabine and oxaliplatin). While dual or triple combinations involving these agents have been studied for various solid tumors—most notably hepatocellular carcinoma, biliary tract cancers, and colorectal cancer—the specific quadruple regimen of lenvatinib + tislelizumab + capecitabine + oxaliplatin has not been widely reported in published clinical trials as of May 2025. Each component has demonstrated efficacy within its class; the rationale for combining them would be to maximize antitumor activity through complementary mechanisms.

02

Targets

FGFR4 (Fibroblast growth factor receptor 4)PDGFRA (Platelet-derived growth factor receptor alpha)TS (Thymidylate synthase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDCD1 (Programmed cell death protein 1 receptor)FGFR3 (Fibroblast growth factor receptor 3)DNAVEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)FGFR1 (Fibroblast growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)FGFR2 (Keratinocyte growth factor receptor)

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