Entrectinib

Globally, the clinical treatment of ROS1-positive non-small cell lung cancer and NTRK gene fusion solid tumors has long faced the pain points of limited targeted drug options and prominent drug resistance problems. Entrectinib, as a new generation of tyrosine kinase inhibitor, can penetrate the blood-brain barrier and potently inhibit the kinase activities of ROS1, TRKA/B/C, ALK, etc. It can not only be used to treat adult patients with ROS1-positive metastatic non-small cell lung cancer, but also delivers definite clinical benefits to adult and pediatric solid tumor patients who carry NTRK gene fusion, have no known acquired resistance mutations, have metastatic disease or for whom surgical resection may lead to severe morbidity, and have no satisfactory alternative treatment options. It is the first pan-solid tumor targeted drug that takes into account both systemic efficacy and intracranial anti-tumor activity.

According to public statistics, the global market size of entrectinib exceeded USD 1.1 billion in 2023, with a compound annual growth rate remaining above 28%. As a market with a high incidence of ROS1-positive lung cancer, China has a potential applicable patient population of more than 30,000. At present, the market is still dominated by the original research product. With the accelerated progress of targeted drug R&D by domestic enterprises, 3 enterprises have submitted marketing applications for entrectinib generics. It is expected that after the expiration of the core patent in 2026, the penetration rate of domestic generics will increase rapidly, and the market size is expected to exceed RMB 1.5 billion in 2028.

The original research enterprise of entrectinib is Genentech, a subsidiary of Roche, and the original research trade name is "Rozlytrek". Its core compound patent expires in 2031 in the United States and in 2028 in China. The main dosage form currently approved is capsule, with specifications including 100mg and 200mg. The original research product has been included in the *Catalogue of Reference Preparations of Chemical Drugs* issued by the NMPA, and is also included in the FDA Reference Preparations Catalogue. Up to now, there have been 11 registration entries of entrectinib API in China, 7 of which are in A status and can be associated with domestic preparation declarations. The original research preparation was approved for marketing in China by the NMPA in 2020, and 3 generic drugs have been approved for marketing in China at present. (Data as of October 2024, please refer to the official website of CDE for the latest information)

CATO can provide a full set of impurity reference standards for entrectinib API. All products meet the compliance requirements of multiple regulatory systems such as Chinese Pharmacopoeia and FDA, and support impurity qualitative and quantitative research as well as drug registration and declaration. Most impurity products are regularly kept in stock. Spot orders placed before 16:00 can be dispatched on the same day, helping pharmaceutical enterprises accelerate the progress of generic drug R&D and consistency evaluation.