Levocetirizine

The recurrent attacks of allergic diseases such as allergic rhinitis and chronic urticaria are common health problems affecting more than 20% of the global population, and there is a long-term clinical demand for treatment regimens that balance safety and onset speed. As the levo-optical isomer of cetirizine, a second-generation antihistamine, levocetirizine exerts its effect by highly selectively blocking histamine H1 receptors, with no obvious central sedative effect or cardiotoxicity. Its pharmacodynamic effect is twice that of racemic cetirizine, with a faster onset of action and a duration of action of up to 24 hours. It is indicated for the symptomatic treatment of allergic diseases such as seasonal/perennial allergic rhinitis and chronic idiopathic urticaria in adults and children over 6 years old, and is currently one of the first-line drugs for long-term control of allergic diseases.

The global market size of levocetirizine-related preparations was approximately USD 1.28 billion in 2023. Driven by factors such as the rising prevalence of allergic diseases year by year and the increasing penetration rate of primary diagnosis and treatment, it is expected to grow at a compound annual growth rate of 4.2% to USD 1.57 billion by 2028. The domestic market currently presents a pattern of coexistence of original research drugs and generic drugs. Since 2021, levocetirizine preparations from more than 20 enterprises have passed the consistency evaluation, among which the oral immediate-release dosage forms have been included in the national centralized procurement catalog, and the winning bid price has dropped by approximately 71% compared with that before the centralized procurement, further promoting the improvement of clinical drug accessibility, and also driving the continuous expansion of market demand for upstream active pharmaceutical ingredients (APIs).

The original research enterprise of levocetirizine is UCB Pharma, Belgium, with the original trade name "Xyzal". Its core compound patent expired in Europe in 2017, in the US market in 2020, and in China in 2016. The main dosage form approved for the original drug is oral tablet with a specification of 5mg, which has been included in the *Catalogue of Reference Preparations for Chemical Drugs* of China and the reference preparation catalogue of the FDA. In terms of domestic API registration, as of now, levocetirizine APIs from more than 15 enterprises have been registered with the Center for Drug Evaluation (CDE) (status A). Domestic and original levocetirizine tablets, oral solutions and other preparations have all 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 impurity reference standards for levocetirizine. All products meet the compliance requirements of multiple regulatory systems such as the Chinese Pharmacopoeia and the FDA. Most impurities are available from stock. For in-stock products, orders placed before 16:00 can be shipped on the same day, which can fully meet the full-process requirements of API manufacturers and preparation R&D institutions for impurity research, quality control, etc.