Lemborexant

Affected by the accelerated pace of global life and the continuous rise of pressure, the prevalence of insomnia in adults has reached 10%~20%. Most of the existing sedative-hypnotic drugs have clinical pain points such as next-day residual sedation and high risk of addiction. As the world's first approved dual orexin receptor antagonist, lemborexant can simultaneously block the binding of orexin OX1 and OX2 receptors to endogenous orexin, inhibit excessive excitation of the central nervous system, and does not widely inhibit neuronal activity. At present, this drug is mainly used to treat adult insomnia with difficulty falling asleep and difficulty maintaining sleep. It is not only suitable for patients with short-term insomnia to improve acute symptoms, but also can be used for long-term symptom management of patients with chronic insomnia. The incidence of adverse reactions such as next-day drowsiness and decreased attention after administration is significantly lower than that of traditional benzodiazepine and non-benzodiazepine hypnotic drugs.

At present, the global market size of insomnia treatment drugs has exceeded 16 billion US dollars. As an innovative category, orexin receptor antagonists have a compound annual growth rate of more than 22%, making them the fastest-growing segment. The global sales of lemborexant exceeded 1.4 billion US dollars in 2023. Since its approval and launch in China in 2023, the annual terminal sales in sample hospitals have exceeded 100 million yuan, with strong growth momentum. At present, only the original research product is on the domestic market, and no generic drug has been approved. A total of 12 enterprises have submitted marketing applications for generic preparations, and more than 8 enterprises have laid out the API sector. With the successive launch of subsequent generic drugs, accessibility will be further improved.

The original research enterprise of lemborexant is Eisai Co., Ltd. of Japan, and the original trade name is "Dayvigo". Its core compound patent will expire in 2033 in China, and the core patent in the US market will expire in 2035. At present, the dosage form approved by the original research in China is tablet, with specifications of 5mg and 10mg, which has been included in the China Listed Drug Catalogue as a reference preparation. In terms of API registration, as of now, the lemborexant API of the original research Eisai has completed registration in CDE with the status of A, and the API registration of 6 domestic enterprises is under review and approval; except for the original research preparations in China, no generic preparations have been approved for marketing. (Data as of June 2025, please refer to the official website of CDE for the latest information.)

In response to the impurity research needs in the development of generic lemborexant, CATO can provide a full set of impurity reference standards for this API. Most of the products are in stock, and in-stock products ordered before 16:00 will be shipped on the same day. All reference standards meet the requirements of multiple regulations such as Chinese Pharmacopoeia and FDA, and can support the whole process of research for declaration.