Rolapitant

Chemotherapy-induced nausea and vomiting is one of the most common adverse reactions in the course of tumor treatment. Nearly 70% of patients receiving highly emetogenic chemotherapy regimens suffer from it, which may even lead to treatment interruption in severe cases. As a representative variety of long-acting NK-1 receptor antagonists, rolapitant can bind to NK-1 receptors in the central nervous system with high selectivity to block the emetic effect of substance P. With a half-life of up to 180 hours, only a single oral administration before chemotherapy is required to maintain the antiemetic effect for multiple days. Compared with short-acting NK-1 receptor antagonists, it greatly improves medication compliance. At present, it is mainly used for the prevention of acute and delayed nausea and vomiting associated with highly and moderately emetogenic chemotherapy in adults. It can also be combined with 5-HT3 receptor antagonists and dexamethasone to form a triple antiemetic regimen to cover more clinical needs.

The global market size of rolapitant was approximately USD 320 million in 2023. In recent years, with the increase in the penetration rate of tumor chemotherapy and the standardization of antiemetic regimens, the compound annual growth rate has remained at around 8%. In the current market pattern, the original research product still occupies a dominant share. In China, with the rising enthusiasm for generic drug application, the market competition for this variety is gradually intensifying. At present, 3 domestic enterprises have submitted generic drug marketing applications, and it is expected to further expand primary clinical application scenarios through centralized procurement in the future, with considerable market growth space.

The original research enterprise of rolapitant is Merck Sharp & Dohme, and the original research trade name is Emend®. Its core compound patent expired in the United States in 2021, and the Chinese compound patent also officially expired in 2022. The main dosage form approved for the original research product is oral capsule, with specifications of 80mg and 125mg. This dosage form has been included in the *Reference Preparations Catalogue of Chemical Drugs* issued by the NMPA, and is also listed in the FDA Reference Preparations Catalogue. In China, at present, the rolapitant APIs of 6 enterprises have obtained A-status registration numbers through the CDE registration platform, another 11 enterprises are in the publicity stage, and 3 domestic rolapitant oral capsules have been approved for marketing. (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 rolapitant API, and most of the products are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day. The products fully comply with the compliance requirements of multiple regulations such as the Chinese Pharmacopoeia and FDA, and can provide reliable reference standard support for the whole-process work of API and preparation enterprises such as quality research, stability study, and declaration and registration.