Drug intelligence / Profile preview

olafertinib

Development stage
Phase 1
Lead developer
Checkpoint Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

Olafertinib is an orally available, third-generation, irreversible small molecule inhibitor that selectively targets activating mutations of the epidermal growth factor receptor (EGFR), including the T790M resistance mutation, L858R mutation, and exon 19 deletion. It demonstrates minimal activity against wild-type EGFR and is designed to overcome resistance to earlier generation EGFR inhibitors in non-small cell lung cancer (NSCLC). Olafertinib covalently binds to mutant EGFR, blocking downstream signaling pathways involved in tumor cell proliferation and survival. The drug has been developed primarily for patients with advanced or metastatic NSCLC harboring specific EGFR mutations[4][5][6][8].

Brand names
olafertinib
Other names
N-(3-(2-(2,3-difluoro-4-(4-(2-hydroxyethyl)piperazin-1-yl)phenylamino)quinazolin-8-yl)phenyl)acrylamide
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)

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