Chentai Pharmaceuticals/AstraZeneca PLC Sponsored ADR (AZN.US) approved for the launch of EGFR inhibitor "Osimertinib" for crossing the blood-brain barrier.

On November 20, the official website of the National Medical Products Administration showed that the EGFR inhibitor Zolifertinib (AZD3759) developed in collaboration between Menta Pharmaceuticals and Astrazeneca PLC Sponsored ADR (AZN.US) has been approved for marketing. It is used as first-line treatment for adults with locally advanced or metastatic non-small cell lung cancer (NSCLC) with EGFR exon 19 deletion or exon 21 (L858R) substitution mutations and central nervous system (CNS) metastases. EGFR is widely expressed in human epidermal and stromal cells, and is highly expressed in a variety of human malignant tumors, such as non-small cell lung cancer. When EGFR gene mutations occur, there is an increase in the epidermal growth factor receptor on the cell membrane, which accelerates abnormal cell division, ultimately leading to tumor formation. Zolifertinib is an effective, orally available, reversible EGFR-TKI designed to inhibit the tyrosine kinase activity of EGFR activating mutations (L858R and Exon 19Del) for the treatment of advanced non-small cell lung cancer patients with CNS metastases. Preclinical and early clinical data show that Zolifertinib has a blood-brain barrier penetration rate of up to 100%.