Drug intelligence / Profile preview

berotinib

Development stage
Unknown
Lead developer
Avistone Biotechnology
Modality
Small Molecules
Administration
Oral
01

Overview

Berotinib (PLB1004) is an orally bioavailable, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) developed by Avistone Biotechnology (Beijing Anshi Biotechnology). It is designed to irreversibly bind to and inhibit EGFR harboring sensitizing mutations (such as exon 19 deletions and L858R) as well as the T790M resistance mutation, while exhibiting selectivity over wild-type EGFR to minimize off-target toxicities. Berotinib is primarily being developed for the treatment of advanced non-small cell lung cancer (NSCLC). It is frequently studied in combination with vebreltinib (PLB1001), a c-Met inhibitor, to address dual EGFR mutation and MET amplification or overexpression, which is a common resistance mechanism to earlier-generation EGFR-TKI therapy.

Other names
berotinibPLB1004PLB-1004PLB 1004贝罗替尼
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)

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