Drug intelligence / Profile preview

E7386 + pembrolizumab + lenvatinib

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

Overview

E7386 + pembrolizumab + lenvatinib is a triple combination therapy under clinical investigation for the treatment of advanced or recurrent solid tumors, including endometrial carcinoma. E7386 is a novel small molecule inhibitor targeting the Wnt/β-catenin signaling pathway. Pembrolizumab is a monoclonal antibody and immune checkpoint inhibitor targeting programmed cell death protein 1 (PD-1), enhancing T-cell mediated immune responses against tumor cells. Lenvatinib is an oral small molecule that inhibits multiple receptor tyrosine kinases involved in tumor angiogenesis and proliferation, including VEGFR1-3, FGFR1-4, PDGFRα, RET, and KIT. The rationale for this combination is to enhance anti-tumor efficacy by simultaneously modulating tumor cell-intrinsic pathways, tumor angiogenesis, and the immune microenvironment. The combination is being studied primarily in patients who have progressed following standard therapies, including anti-PD-(L)1 treatment, with ongoing clinical trials assessing safety, tolerability, and anti-tumor activity[1][2][3][4].

Other names
E7386 + pembrolizumab + lenvatinib
02

Targets

FGFR4 (Fibroblast growth factor receptor 4)CREBBP (CREB-binding protein)PDCD1 (Programmed cell death protein 1 receptor)PDGFRA (Platelet-derived growth factor receptor alpha)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)FGFR3 (Fibroblast growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)FGFR2 (Keratinocyte growth factor receptor)FGFR1 (Fibroblast growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)

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