Drug intelligence / Profile preview

nazartinib

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

Overview

Nazartinib is an orally available, irreversible, third-generation, mutant-selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI). It is designed to selectively inhibit mutant forms of EGFR—including the T790M resistance mutation—while sparing wild-type EGFR. By covalently binding to and inhibiting these mutant receptors, nazartinib blocks EGFR-mediated signaling pathways that drive tumor cell proliferation and survival. This mechanism may induce cell death and inhibit tumor growth in cancers with EGFR mutations, particularly non-small cell lung cancer (NSCLC). Nazartinib has demonstrated promising efficacy as a first-line treatment for patients with advanced or metastatic NSCLC harboring activating EGFR mutations, including activity against brain metastases. The drug was developed by Novartis Oncology and has been studied in multiple phase I–III clinical trials for NSCLC[1][2][3][4][5][6].

Other names
nazartinib mesylate1508250-71-2
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)

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