Ribociclib

Hormone receptor positive (HR+), human epidermal growth factor receptor 2 negative (HER2-) advanced breast cancer is the most common breast cancer subtype in clinical practice, accounting for approximately 70% of all advanced breast cancer cases. Previous endocrine therapy resistance is the main obstacle to long-term survival of such patients. Ribociclib belongs to cyclin-dependent kinase 4/6 (CDK4/6) inhibitors. By specifically blocking the activity of CDK4/6, it inhibits the proliferation of tumor cells from G1 phase to S phase, thereby delaying the occurrence of endocrine resistance. At present, this drug is mainly combined with aromatase inhibitors or fulvestrant for the first-line treatment of premenopausal/perimenopausal or postmenopausal patients with HR+/HER2- advanced breast cancer, which can significantly prolong the progression-free survival of patients, and has become a standard treatment regimen recommended by domestic and foreign guidelines.

The global market size of CDK4/6 inhibitors exceeded USD 9 billion in 2023. With its clear survival benefit in premenopausal patient population, ribociclib achieved a global sales revenue of USD 1.82 billion in 2023, with an annual growth rate of more than 12%. In terms of the Chinese market, ribociclib was included in the National Medical Insurance Catalogue through negotiation in 2023, with a price reduction of nearly 60%, which greatly reduced the out-of-pocket expenses of patients. It is expected that the compound annual growth rate of the domestic market from 2024 to 2028 will exceed 35%. At present, the global supply of ribociclib API is still dominated by the supporting production capacity of the original research enterprise, and there is no large-scale generic API production capacity co-produced with the original research line in China. There is a clear gap in the API demand of generic pharmaceutical enterprises after the patent expiration.

The original research enterprise of ribociclib is Novartis, and the original trade name is "Kisqali®". The expiration date of its core compound patent in the United States is 2029, and the expiration date of the compound patent in China is 2030. The main dosage form approved by the original research is oral tablet, with three specifications including 200mg, 300mg and 400mg. It has been included in the *Catalogue of Reference Preparations for Chemical Drugs* issued by the NMPA, and also included in the FDA Reference Preparations Catalogue. Up to now, no enterprise in China has obtained the marketing license of ribociclib API or the CDE API registration number. The domestically approved and marketed preparations are only original imported products, and no generic preparation has been approved for the time being. (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 ribociclib. Most products are available from stock. For in-stock products, orders placed before 16:00 can be shipped on the same day. All reference standards meet the compliance requirements of multiple regulatory systems such as Chinese Pharmacopoeia and FDA, and can fully meet the reference substance needs of pharmaceutical enterprises in the whole process of API R&D, quality research and generic drug declaration.