Difelikefalin

Moderate to severe pruritus associated with chronic kidney disease is a common complication in patients on maintenance dialysis. The response rate of previous conventional treatment regimens such as antihistamines and glucocorticoids is less than 30%, and the clinical demand has been unmet for a long time. Difelikefalin is a peripherally selective kappa opioid receptor agonist. It only acts on kappa opioid receptors in the peripheral nervous system and does not penetrate the blood-brain barrier to cause central nervous system-related adverse reactions. It can effectively relieve symptoms by inhibiting the peripheral transmission of pruritus signals. Currently, it is approved for the treatment of moderate to severe pruritus in chronic kidney disease patients receiving hemodialysis, and it is the first targeted therapeutic drug in this细分 field.

At present, the global market size of dialysis-related pruritus therapeutic drugs has exceeded 1.2 billion US dollars, with a compound annual growth rate of more than 8%, among which peripheral opioid receptor agonists account for more than 60%. The number of existing dialysis patients in China exceeds 900,000, and the incidence of pruritus is as high as 60%~70%, corresponding to more than 500,000 potential applicable populations. As the only targeted drug approved for this indication in China, the sales volume of difelikefalin in sample hospitals has exceeded 120 million yuan in 2023. With the improvement of clinical awareness, the growth rate of the domestic market is expected to remain above 35% in the next three years. At present, no generic drug has been approved in China, and the market is still in the stage of original research exclusivity.

The original research enterprise of difelikefalin is Cara Therapeutics, and the original research trade name is Korsuva. The core compound patent of the drug expires in 2033 in the United States and in 2032 in China. The currently approved original research dosage form is injection, with a specification of 0.5mg/1ml. This product has been included in the Reference Listed Drug Catalogue of NMPA and is also included in the Reference Listed Drug Catalogue of FDA. Up to now, there is no API registration information of difelikefalin on the CDE API registration platform. Only the original imported injection has been approved for marketing in China, and no domestic preparation has been approved. (Data as of October 2024, please refer to the official CDE website for the latest information)

CATO can provide a full set of impurity reference standards for difelikefalin, most of which are in stock regularly. Spot orders placed before 16:00 can be shipped on the same day. All products meet the requirements of multiple regulatory systems such as Chinese Pharmacopoeia and FDA, and can provide stable compliance support for the whole process of drug R&D, quality research and registration.