Zeteletinib

In response to the widespread drug resistance of first- and second-generation ALK inhibitors in the clinical treatment of ALK-positive non-small cell lung cancer (NSCLC), zelebrutinib, as a third-generation ALK tyrosine kinase inhibitor independently developed in China, can effectively overcome common drug resistance mutations such as G1202R through structural optimization of the kinase binding domain, and meanwhile exhibits excellent penetration and inhibitory activity against central nervous system metastatic lesions. At present, this drug is mainly indicated for ALK-positive locally advanced or metastatic NSCLC patients who have progressed after prior treatment with ALK inhibitors or are intolerant to such treatment, providing a new prognosis improvement path for this population with limited clinical treatment options.

The annual number of newly diagnosed ALK-positive NSCLC patients in China is approximately 35,000. With the gradual clinical application of third-generation ALK inhibitors, the domestic market size of third-generation ALK inhibitors exceeded 1.2 billion yuan in 2023, with an annual growth rate of 78%. The current market competition is dominated by domestic innovative drugs. As the first domestically developed third-generation ALK inhibitor approved for marketing, zelebrutinib, relying on its lower incidence of adverse reactions and price advantage after medical insurance negotiations, occupied 42% of the domestic third-generation ALK inhibitor market in the second year after its launch, significantly reducing the medication burden of relevant patients.

Zelebrutinib is independently developed by Betta Pharmaceuticals, with the trade name Beimeina®. Its core compound patent will expire in 2038. The currently approved main dosage form is oral capsule, with specifications of 100mg and 200mg, and it has been included in the *Catalogue of Reference Preparations of Chemical Drugs* issued by the NMPA. Up to now, the CDE database shows that Betta Pharmaceuticals has completed the A-status registration of the API, and the corresponding domestic capsule preparation was approved for marketing in May 2023. (Data as of October 2024, please refer to the official CDE website for the latest information)

CATO can provide a full set of zelebrutinib impurity reference standards, most of which are available in stock. Spot orders paid before 16:00 can be shipped on the same day. All products comply with the regulatory requirements of multiple systems such as the Chinese Pharmacopoeia and FDA, and can fully meet the reference substance use needs of pharmaceutical enterprises in API R&D, quality research, consistency evaluation and other links.