Pitolisant

Narcolepsy is a chronic sleep disorder that is easily missed in diagnosis. Patients often have symptoms such as irresistible daytime sleepiness and cataplexy, which seriously affect their quality of life. Pitolisant, the world's first approved selective histamine H3 receptor antagonist/inverse agonist, exerts long-acting improvement on sleepiness symptoms without causing excessive excitation by upregulating the levels of wakefulness-related neurotransmitters such as central histamine and dopamine. It is currently approved for the treatment of daytime sleepiness and cataplexy in adult patients with narcolepsy, and serves as a first-line treatment option in the field of narcolepsy, filling the previous clinical gap of no targeted therapies.

The global prevalence of narcolepsy is approximately 0.02% to 0.05%, corresponding to a potential patient population of over one million. Currently, the global market size of pitolisant has exceeded USD 1.2 billion, with a compound annual growth rate of over 28% in the past three years. As the patents of the originator drug gradually expire, the development of generic drugs worldwide continues to gain momentum. More than 10 domestic pharmaceutical companies have initiated the generic drug declaration of this product, among which 3 have submitted the associated declaration of API and preparations. With the price drop after the launch of generic drugs in the future, the domestic market penetration rate is expected to increase from the current less than 5% to over 15%.

The originator of pitolisant is the French company Bioprojet, with the originator brand name "Wakix". Its core compound patent in the United States expired in 2023, and the core European patent is expected to expire in 2027. The approved dosage form of the originator drug is oral tablet, with three specifications of 4.5 mg, 9 mg and 18 mg, which has been included in the FDA Reference Listed Drug Catalog and the Chinese *Catalog of Reference Preparations for Chemical Drugs (54th Batch)*. At present, the pitolisant APIs of 8 domestic enterprises have completed registration at CDE. The originator preparation was approved for import in China in 2023, and the generic preparations of 3 domestic enterprises are in the marketing review stage. (Data as of June 2025, please refer to the official CDE website for the latest information.)

CATO provides a full set of pitolisant impurity reference standards. Most products are available in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day. The products can meet the compliance requirements of multiple regulations such as Chinese Pharmacopoeia and FDA, and can provide stable reference standard support for the whole process of API R&D, quality research and generic drug declaration of pharmaceutical enterprises.