Drug intelligence / Profile preview

befotertinib

Development stage
Phase 4
Lead developer
Betta Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Befotertinib is an orally available, third-generation small molecule inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, specifically targeting mutant forms such as T790M. It is structurally derived from osimertinib with a trifluoromethyl group substitution for improved stability and reduced gastrointestinal side effects. Befotertinib has demonstrated superior efficacy compared to icotinib in first-line treatment of EGFR mutation-positive non-small cell lung cancer (NSCLC), including patients with rare EGFR mutations such as p.G719X/p.S768I. The drug is approved in China for locally advanced or metastatic NSCLC and shows particular promise in patients with central nervous system metastases.

Brand names
Semena
Other names
befotertinib mesylate
02

Targets

ABCB1 (P-glycoprotein)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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