Drug intelligence / Profile preview

sutetinib

Development stage
Phase 2
Lead developer
Teligene
Modality
Small Molecules
Administration
Oral
01

Overview

Sutetinib (also known as sutetinib maleate) is an orally active, small molecule tyrosine kinase inhibitor (TKI) that acts as an irreversible inhibitor of the epidermal growth factor receptor (EGFR). It is specifically designed to target rare, non-drug-resistant EGFR mutations, including L861Q, S768I, and G719X, which are often less responsive to first-generation TKIs. Beyond its activity against EGFR, sutetinib exhibits multi-targeted inhibitory effects on other kinases involved in tumor growth and angiogenesis, including vascular endothelial growth factor receptors (VEGFR-1, -2, and -3), platelet-derived growth factor receptors (PDGFR-α and -β), and the proto-oncogene c-KIT. The drug is currently in Phase 2 clinical development for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) harboring these specific rare mutations. It is being developed by Suzhong Pharmaceutical Group in collaboration with Jiangsu Maidu Pharmaceutical and SuZhou Teligene.

Brand names
sutetinib
Other names
sutetinib maleatesutetinib N-oxide
02

Targets

ABCG2 (Breast cancer resistance protein)PDGFRA (Platelet-derived growth factor receptor alpha)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)CSF1R (Macrophage colony-stimulating factor receptor)PDGFRB (Platelet-derived growth factor receptor beta)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)RET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)ABCB1 (P-glycoprotein)

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