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trametinib + everolimus + lenvatinib

Development stage: Unknown
Lead developer: Eisai
Modality: Small Molecules
Administration: Oral

Overview

This is an investigational combination therapy consisting of three small molecule inhibitors: trametinib, everolimus, and lenvatinib. Trametinib is a selective inhibitor of MEK1 and MEK2, components of the MAPK/ERK pathway; everolimus is an mTOR inhibitor targeting the PI3K/AKT/mTOR signaling pathway; and lenvatinib is a multi-targeted tyrosine kinase inhibitor that blocks vascular endothelial growth factor receptors (VEGFRs), fibroblast growth factor receptors (FGFRs), platelet-derived growth factor receptor alpha (PDGFRα), RET, and KIT. This triple combination aims to simultaneously inhibit tumor cell proliferation, angiogenesis, and survival pathways. It is currently being studied in clinical trials for recurrent or refractory advanced solid tumors[1][3][4][8].

Brand names: Mekinist (trametinib)Afinitor (everolimus)Lenvima (lenvatinib)Kisplyx (lenvatinib)
Other names: trametinib + everolimus + lenvatinib

Targets

FGFR3 (Fibroblast growth factor receptor 3)FGFR4 (Fibroblast growth factor receptor 4)VEGFR2 (Vascular endothelial growth factor receptor 2)RET (Rearranged during transfection receptor tyrosine kinase)FGFR2 (Keratinocyte growth factor receptor)VEGFR4 (Vascular endothelial growth factor Receptor-3)PDGFRA (Platelet-derived growth factor receptor alpha)VEGFR-1 (Vascular endothelial growth factor receptor 1)KIT (c-KIT proto-oncogene receptor tyrosine kinase)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)mTOR (Mammalian target of rapamycin kinase)FGFR1 (Fibroblast growth factor receptor 1)

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