Ezetimibe

Hyperlipidemia is a chronic metabolic disease with high incidence globally. More than 40% of patients cannot achieve the lipid-lowering target with statin monotherapy, and the advent of ezetimibe has filled this clinical gap. As the first selective cholesterol absorption inhibitor, it targets and inhibits the NPC1L1 protein in the brush border of the small intestine to reduce the intestinal absorption of cholesterol from food and bile, without affecting the absorption of bile acids and fat-soluble vitamins. In clinical practice, it can be used as monotherapy for lipid-lowering treatment in statin-intolerant patients, and can also be used in combination with statins and PCSK9 inhibitors to further reduce low-density lipoprotein cholesterol levels in patients with primary hypercholesterolemia and homozygous sitosterolemia, covering adult patients and children with homozygous familial hypercholesterolemia over 10 years old.

Currently, the global market size of ezetimibe preparations has exceeded 3 billion US dollars. Driven by the rising prevalence of hyperlipidemia and the popularization of combined lipid-lowering regimens, the compound annual growth rate has maintained at 4.8% in the past 5 years. For the domestic market, after ezetimibe was included in the National Medical Insurance Catalog in 2017, its market size has expanded rapidly to nearly 2 billion RMB, with a compound growth rate of 22%. In terms of the competitive landscape, the original research product still accounts for nearly 60% of the market share. More than 10 domestic enterprises have obtained approval for generic drugs of this variety, which has been included in the 7th batch of national centralized drug procurement. The maximum price reduction of the winning bids compared with the original research product exceeds 90%. The expansion of downstream preparation capacity has directly driven the continuous growth of the demand for active pharmaceutical ingredients.

The original research enterprise of ezetimibe is Merck Sharp & Dohme, with the original brand name of Ezetrol®. Its compound patent expired in the United States in 2016, and the core compound patent in China expired in 2014. The main dosage form approved by the original research is tablet with a specification of 10mg, which has been listed as the reference preparation in the Catalogue of Marketed Drugs in China, and is also included as a reference preparation by the FDA. For domestic API registration, there are currently nearly 30 registration numbers for ezetimibe API, among which nearly 20 are in A status, which can meet the associated review requirements of domestic preparation enterprises. In China, 10mg ezetimibe tablets from the original research enterprise and multiple generic drug enterprises have been approved for marketing. (Data as of October 2024, please refer to the official website of CDE for the latest information)

CATO provides a full set of impurity reference standards for ezetimibe API, which can meet the impurity research requirements of different process routes. Most products are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day. The products meet the compliance requirements of multiple regulations including the Chinese Pharmacopoeia and FDA, and can provide stable technical support for API and preparation enterprises in the links of quality research and associated declaration.