Drug intelligence / Profile preview

gefitinib + apatinib

Development stage
Phase 3
Lead developer
Hengrui Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

Gefitinib + apatinib is a combination therapy of two small molecule tyrosine kinase inhibitors used primarily in the treatment of advanced non–small cell lung cancer (NSCLC) with EGFR mutations. Gefitinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that blocks the ATP-binding site of EGFR, inhibiting downstream signaling pathways involved in cell proliferation and survival. Apatinib selectively inhibits vascular endothelial growth factor receptor-2 (VEGFR-2), thereby blocking angiogenesis required for tumor growth. The combination has demonstrated superior progression-free survival compared to gefitinib alone as first-line therapy for patients with advanced EGFR-mutant NSCLC[1][2][3][4][8].

Brand names
Iressa (for gefitinib)Aitan (for apatinib mesylate)
Other names
apatinibgefitinib
02

Targets

EGFR (Epidermal growth factor receptor)VEGFR2 (Vascular endothelial growth factor receptor 2)

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