Zorifertinib (AZD3759), a Brain-Penetrant EGFR Inhibitor Co-Developed by Centaurus Pharma and AstraZeneca (AZN.US), Receives NMPA Approval for First-Line Treatment of NSCLC with CNS Metastases

Intelligent Finance APP learned on November 20 that the official website of the National Medical Products Administration (NMPA) showed that zorifertinib (AZD3759), an EGFR inhibitor co-developed by Alpha Biopharma and AstraZeneca (AZN.US), has been approved for marketing. It is indicated as a first-line treatment for adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) who have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations, accompanied by central nervous system (CNS) metastases.

EGFR is widely expressed in human epidermal cells and stromal cells, and is highly expressed in various human malignant tumors, such as non-small cell lung cancer. EGFR gene mutations can lead to an overabundance of epidermal growth factor receptors on the cell membrane surface, accelerating abnormal cell growth and division, ultimately resulting in tumor development.

Zorifertinib is an effective, orally administered, reversible inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase activity with activating mutations (L858R and Exon 19Del), specifically designed for the treatment of patients with advanced non-small cell lung cancer and central nervous system metastases. Preclinical and early clinical data show that Zorifertinib has a blood-brain barrier penetration rate of up to 100%.