Drug intelligence / Profile preview

gozanertinib

Development stage
Phase 1
Lead developer
National Health Research Institutes
Modality
Small Molecules
Administration
Oral
01

Overview

Gozanertinib is an orally bioavailable dual kinase inhibitor of epidermal growth factor receptor (EGFR; ErbB1) and human epidermal growth factor receptor 2 (HER2; EGFR2; ErbB2). It targets and inhibits the activity of EGFR or HER2, including specific mutations such as EGFR L858R, EGFR T790M, and HER2 exon 20 insertion mutations. This action prevents EGFR/HER2-mediated signaling, which can induce cell death and inhibit tumor growth in EGFR/HER2-overexpressing tumor cells. It is a furanopyrimidine-based EGFR inhibitor that has demonstrated improved potency against EGFR and HER2 exon 20 insertion mutations compared to osimertinib. Gozanertinib is being developed for its potential antineoplastic activity, particularly in non-small cell lung cancer. [1, 2, 3, 4, 6, 7]

02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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