AstraZeneca and Centaurus Therapeutics Announce NMPA Approval of Zorifertinib (Zelini), a Novel First-in-Class EGFR-TKI for NSCLC with CNS Metastases

On November 20, according to the NMPA website, "Zorifertinib Hydrochloride Tablets" (brand name: Zerenee), a Class 1 new drug jointly developed by AstraZeneca and Alpha Biopharma, has been approved for marketing in China.

Image Source: NMPA Official Website

According to the NMPA official website, this drug is suitable for first-line treatment of 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, providing patients with a new treatment option.

Zorifertinib (AZD3759) is an effective, orally administered, reversible inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase activity, targeting activating mutations L858R and Exon 19Del, developed by AstraZeneca. In January 2018, Alpha Biopharma in-licensed the drug and took charge of advancing its Phase II and III clinical development. On January 29, 2023, the New Drug Application (NDA) for Zorifertinib was accepted by the CDE.

Source of the image: Pharma Data Enterprise Edition —— Global Drug Analysis System Database

It is understood that central nervous system (CNS) metastasis is a common metastatic site in patients with EGFR mutation-positive non-small cell lung cancer. The spread of tumors in the CNS mainly includes scenarios such as meningeal dissemination and brain metastasis, with early disease progression, poor prognosis, short survival time, and low quality of life for patients. Although whole-brain radiotherapy is currently the standard treatment, its efficacy is limited and it has significant toxic side effects. Additionally, the blood-brain barrier increases the difficulty of drug penetration into the brain, making the cranium a refuge for lung cancer cells.

Patients with epidermal growth factor receptor (EGFR) mutation-positive non-small cell lung cancer (NSCLC) are prone to tumor spread to the central nervous system, occurring in more than half of cases. Currently available EGFR tyrosine kinase inhibitor (TKI) drugs struggle to provide long-lasting and stable efficacy against this condition. Zoritini is a next-generation EGFR-TKI specifically designed for treating advanced NSCLC with central nervous system metastases, capable of fully penetrating the blood-brain barrier.

According to a previous report by Alpha Biopharma, the global first international multicenter randomized controlled Phase III clinical study EVEREST completed by Zoritini (AZD3759) specifically targeted patients with CNS metastases. All enrolled patients had CNS metastases and had not previously received intracranial radiotherapy, including over 20% with symptoms of CNS metastases, more than half with L858R mutations, and more than half with more than three intracranial lesions. The results of this study validated the efficacy and safety of Zoritini (AZD3759) as a first-line monotherapy for EGFR mutation-positive advanced NSCLC patients with CNS metastases.

The successful approval and market launch of Zolitinib will provide new treatment options for lung cancer patients.

Editor: Muyan

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