Qilu Pharmaceutical's Aprepitant Injection Approved in China, Entering the Antiemetic Market with First Domestic Submicron Emulsion Formulation

The National Medical Products Administration recently released a new batch of drug approval certificates for collection. Qilu Pharmaceutical's Aprepitant Injection has been approved for marketing, becoming the first approved Aprepitant submicron emulsion injection in China. The original injectable form of the drug was approved for marketing in the United States in 2017 and has not yet entered the Chinese market. Qilu Pharmaceutical had previously also obtained the first generic approval for Aprepitant capsules.

As the world's first approved NK-1 receptor antagonist antiemetic, Aprepitant is the first Peptan-class drug launched in China, with Merck & Co. facing competition domestically only from Qilu Pharmaceutical and Zhengdatianqing.

The original research drug Aprepitant (trade name: Emend), developed by Merck, was approved for marketing in the United States in 2003 and gained approval to enter China in 2013. As an oral neurokinin-1 receptor antagonist, Aprepitant is administered in combination with other antiemetic drugs and is suitable for preventing acute and delayed nausea and vomiting that occur during the initial and repeated treatments with highly emetogenic antineoplastic chemotherapy.

 

Aprepitant can cross the blood-brain barrier, selectively and strongly binding to neurokinin-1 receptors in the brain, thereby inhibiting chemotherapy-induced nausea and vomiting at the central level. It has been recommended by authoritative guidelines both in China and internationally as a first-line and recommended medication for preventing nausea and vomiting caused by highly emetogenic anti-tumor chemotherapy. The 2014 edition of China's "Guidelines for the Prevention and Treatment of Vomiting Related to Tumor Therapy" emphasizes the importance of preventing chemotherapy-induced nausea and vomiting for patients and the execution of chemotherapy regimens. It explicitly recommends the triple-drug regimen of 5-HT3 receptor antagonists, dexamethasone, and NK-1 receptor antagonists to prevent nausea and vomiting induced by highly emetogenic chemotherapy regimens.

In 2018, the sales of the original research drug Aprepitant Capsules in China's key provincial public hospital terminals reached 74.78 million yuan, a year-on-year increase of 14.31%. The overall market in China has reached a scale of 200 million yuan. On July 20, 2020, Qilu Pharmaceutical's Aprepitant Capsules (brand name: Oukoping) were approved for marketing and deemed to have passed the consistency evaluation, becoming the first domestically produced generic Aprepitant to be marketed in China. In July 2021, Zhengda Tianqing's Aprepitant Capsules, under China Biologic Products Holdings, were also approved for marketing and deemed to have passed the consistency evaluation. According to a search by a reporter from the Beijing News on the Insight database, to date, apart from the original research drug, only Qilu Pharmaceutical and Zhengda Tianqing have been approved for the capsule formulation of Aprepitant.

According to the PharmaCloud database, the national hospital sales of Aprepitant capsules in China exceeded 300 million yuan in 2021, of which the original research company, Merck, accounted for 57% of the market share, a significant decrease compared to previous years, while Qilu Pharmaceutical accounted for over 40%; in the first quarter of this year, sales were nearly 100 million yuan, an increase of 86% year-on-year, indicating broad market prospects.

Aprepitant Injection is a submicron emulsion formulation made by encapsulating aprepitant in soybean oil, which significantly improves bioavailability and medication compliance compared to oral formulations; it also effectively reduces the incidence of allergic reactions in clinical use of similar injectable formulations.

According to information released on Qilu Pharmaceutical's official WeChat account, Qilu Pharmaceutical initiated the Aprepitant Injection project in 2018. Researchers utilized nano-solubilization technology to solve the problem of the main drug's poor solubility and successively overcame technical barriers in critical excipient screening, formulation process development, and quality standard establishment. They developed a proprietary preparation method with independent intellectual property rights and built a research and industrialization technology platform for drug-loaded submicron emulsion formulations. Researchers rigorously followed relevant domestic and international guidelines and technical principles to conduct comprehensive quality comparison studies and clinical studies between their self-produced products and reference preparations, fully ensuring equivalent quality, clinical safety, and efficacy.

As of now, Qilu Pharmaceutical has launched several products in the antiemetic field, including, in addition to the recently approved intravenous Aprepitant, 5-HT3 inhibitors (Palonosetron Hydrochloride, Granisetron, Ondansetron, and Tropisetron Hydrochloride Injection) and NK-1 inhibitors (Aprepitant Capsules, Fosaprepitant dimeglumine for injection).