Repotrectinib

In response to the clinical pain points that patients with RET fusion mutations in non-small cell lung cancer have limited clinically optional targeted drugs and no available drugs after drug resistance, repotrectinib, as a new generation of potent RET inhibitor, irreversibly binds to the RET kinase domain, significantly overcoming drug resistance types such as gatekeeper mutations and solvent front mutations of first-generation RET inhibitors, and also exhibits excellent inhibitory activity against ROS1 and NTRK fusion mutations. It is clinically mainly used to treat locally advanced or metastatic non-small cell lung cancer, medullary thyroid carcinoma and other solid tumors carrying RET fusion positivity, and is particularly suitable for drug-resistant populations who have progressed after treatment with first-generation RET inhibitors. Compared with traditional therapies, it has greatly improved the objective response rate and progression-free survival, filling the treatment gap in the field of RET resistance mutations.

The global market size of RET inhibitors had exceeded USD 2.8 billion in 2023, and it is expected to climb to USD 8.2 billion in 2028 with a compound annual growth rate of 23.7%. Among them, repotrectinib, relying on its exclusive advantage in drug resistance scenarios, achieved global sales of USD 170 million in the first year of its launch in 2023, becoming the fastest-growing variety targeting RET. In the domestic market, 3 first-generation RET inhibitors have been included in the medical insurance at present. As the first approved second-generation RET inhibitor, repotrectinib has not been included in the centralized procurement catalog for the time being. Its API supply is still dominated by self-production of the original research enterprise at present, and domestic generic drug enterprises are still in the pre-clinical layout stage.

The original research enterprise of repotrectinib is Turning Point Therapeutics of the United States (later acquired by Bristol-Myers Squibb), and its trade name is Augtyro. Its core compound patent will expire in 2039 in the United States, and the core compound patent in China will expire in 2040. The main currently approved dosage form is oral tablet, with two specifications including 20 mg and 40 mg. This variety has been included in the FDA Reference Listed Drug Catalog, and was approved for marketing by the China NMPA in May 2024. At present, there is no registered API DMF number in China, and the only domestically approved preparation is the original imported variety. (Data as of June 2025, please refer to the official CDE website for the latest information)

CATO provides a full set of impurity reference standards for repotrectinib API, covering intermediate impurities, degradation impurities and enantiomers that may be generated during the synthesis process. All products meet the compliance requirements of multiple regulations such as Chinese Pharmacopoeia and FDA. Most products are in regular stock, and orders placed before 16:00 can be shipped on the same day, which can fully meet the reference standard requirements of pharmaceutical enterprises in the whole process of R&D, quality research and declaration.