Aprepitant

Nausea and vomiting caused by highly emetogenic chemotherapy drugs (CINV) is one of the most common adverse reactions in tumor patients during treatment. If not effectively controlled, it will significantly reduce treatment compliance and even lead to chemotherapy interruption. As the world's first approved highly selective neurokinin-1 (NK-1) receptor antagonist, aprepitant can block the binding of substance P to NK-1 receptors, filling the mechanism gap in the prevention and control of delayed CINV that cannot be covered by 5-HT3 receptor antagonists. At present, it is clinically mainly used to prevent acute and delayed nausea and vomiting occurring during initial and repeated courses of highly and moderately emetogenic antineoplastic chemotherapy. It can also be combined with other antiemetics to form a triple antiemetic regimen, meeting the antiemetic needs of adult and adolescent tumor patients over 12 years old.

The current global market size of aprepitant has exceeded 1.8 billion US dollars. In recent years, with the expansion of the tumor patient population and the improvement of the standardization of antiemetic therapy, the compound annual growth rate has remained at around 6%. The growth rate of the Chinese market in the past five years is significantly higher than the global average, with a compound annual growth rate of 12%, and the market size exceeded 1.2 billion yuan in 2023. In terms of the competitive landscape, the original research product still accounts for about 40% of the market share. More than 10 domestic enterprises have obtained approval for the marketing of generic preparations of this variety, which has been included in the national centralized drug procurement. The maximum price reduction of the winning bids compared with the original research product exceeds 90%, further promoting the improvement of clinical accessibility, and the demand for upstream API has also continued to expand.

The original research enterprise of aprepitant is Merck, and the original research trade name is "Emend". Its core compound patent in China expired in 2022. The main dosage forms approved for the original research include capsules (80mg, 125mg) and aprepitant for injection (115mg). Relevant dosage forms have all been included in the *Catalogue of Reference Preparations of Chemical Drugs* in China, and are also listed as reference preparations by the FDA. In terms of domestic API registration, there are currently 12 aprepitant API registration numbers, 8 of which have been activated to A status, which can be associated with preparation declaration or marketing use. More than 20 aprepitant preparation varieties, including capsules and injections, have been approved for marketing in China. (Data as of October 2024, please refer to the official website of CDE for the latest information)

CATO can provide a full set of aprepitant impurity reference standards. Most products are available from stock. Stock orders placed before 16:00 can be shipped on the same day. All products meet the compliance requirements of multiple regulatory systems such as the Chinese Pharmacopoeia and FDA, and can fully meet the full-process needs of API enterprises for process R&D, quality research and declaration.