Drug intelligence / Profile preview

osimertinib + anlotinib

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

Osimertinib + anlotinib is a combination therapy of two small molecule tyrosine kinase inhibitors used primarily in the treatment of advanced non-small cell lung cancer (NSCLC), particularly in patients who have developed resistance to prior EGFR-targeted therapies. Osimertinib is a third-generation, irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that selectively targets both EGFR-sensitizing and T790M resistance mutations. Anlotinib is a multi-targeted tyrosine kinase inhibitor that inhibits vascular endothelial growth factor receptors (VEGFR1/2/3), fibroblast growth factor receptors (FGFR1–4), platelet-derived growth factor receptors (PDGFRα/β), and c-Kit, thereby suppressing tumor angiogenesis and proliferation. The combination has shown efficacy in overcoming acquired resistance to osimertinib by targeting additional pathways involved in tumor progression and drug resistance, such as the c-MET/MYC/AXL axis[1][2][3][4][5]. Clinical studies indicate this regimen can improve outcomes for patients with advanced NSCLC after failure of previous lines of therapy.

Brand names
Focus V
Other names
osimertinib + anlotinib
02

Targets

MET (Mesenchymal-epithelial transition factor receptor)AXL (AXL receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)EGFR T790M (Epidermal growth factor receptor T790M mutant)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)FGFR1 (Fibroblast growth factor receptor 1)

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