Nalmefene

Opioid overdose is a prominent risk in the global public health field. As a new-generation opioid receptor antagonist, nalmefene competitively blocks the three types of opioid receptors μ, κ and δ, and can rapidly reverse the central inhibitory effects such as respiratory depression and sedation caused by opioids. Compared with the similar product naloxone, it has a longer half-life, higher affinity and better clinical safety. At present, this drug is mainly used for first aid of opioid overdose, reversal of adverse reactions of postoperative opioids, and adjuvant treatment of alcohol dependence and opioid dependence, covering clinical needs of multiple departments including emergency department, anesthesiology department and psychiatry department, and is an important drug in the acute and critical care system.

The current global nalmefene market size is approximately USD 230 million, with a compound annual growth rate maintained at around 7.2%. The growth momentum mainly comes from the rising demand for first aid for opioid overdose and the expansion of applications in the field of addiction treatment. In terms of the domestic market, the terminal sales of nalmefene in public medical institutions have stabilized at RMB 1.2 billion in recent years, of which injections account for more than 95%; the competitive landscape is dominated by generics, with more than 10 domestic enterprises currently approved to produce nalmefene for injection. After centralized procurement, the product price has dropped by more than 80%, and the market is gradually concentrated on leading generic pharmaceutical enterprises.

The original developer of nalmefene is Akorn, a subsidiary of Bausch Health, and the original brand name is Revia. The core compound patent in the US market expired in 2008, and there is no compound patent restriction in China. The main dosage forms of the original drug are injections, with specifications including 0.1mg/ml and 1mg/ml, among which the 0.1mg/ml injection has been included in the FDA Orange Book Reference Listed Drug Catalog. Up to now, no original preparation of nalmefene has been marketed in China. A total of 17 domestic nalmefene APIs have been registered and publicized by CDE, among which 9 are A-status registration numbers, and more than 20 domestic nalmefene injections have been approved for marketing. (Data as of November 2024, please refer to the official CDE website for the latest information)

In response to the R&D and quality control requirements of nalmefene, CATO provides a full set of impurity reference standards for this API, which fully covers the research needs of various impurities in the synthesis process and degradation pathways. Most products are in stock, and orders placed before 16:00 can be shipped on the same day. All reference standards meet the compliance requirements of multiple regulatory systems such as Chinese Pharmacopoeia and FDA, and can be directly used in method validation, stability study and registration declaration scenarios.