Drug intelligence / Profile preview

third-generation EGFR-TKI + anlotinib

Development stage
Unknown
Lead developer
Chia Tai-Tianqing Pharmaceutical Group
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination therapy consisting of a third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) and the multi-targeted small molecule tyrosine kinase inhibitor, anlotinib. Third-generation EGFR-TKIs—such as osimertinib, almonertinib, lazertinib, furmonertinib, and nazartinib—are mutant-selective inhibitors that irreversibly bind to mutant forms of the EGFR protein including T790M resistance mutations in non-small cell lung cancer (NSCLC), while sparing wild-type EGFR[1][2]. Anlotinib is a multi-targeted TKI that inhibits angiogenesis and tumor growth by targeting vascular endothelial growth factor receptors (VEGFRs), fibroblast growth factor receptors (FGFRs), platelet-derived growth factor receptors (PDGFRs), and c-Kit. The combination is used primarily in NSCLC patients who have developed resistance to prior lines of EGFR-TKIs. Clinical studies suggest this regimen can prolong progression-free survival compared to monotherapy with either agent alone[3][4][5][8]. The mechanism involves dual inhibition of tumor cell proliferation via mutant-EGFR blockade and suppression of angiogenesis through VEGF pathway inhibition.

Other names
third-generation EGFR tyrosine kinase inhibitor plus anlotinib3rd generation EGFR-TKI + anlotinibosimertinib + anlotinibalmonertinib + anlotinib
02

Targets

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

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