Lofexidine

Detoxification treatment for opioid dependence is an important clinical demand in the field of mental health. Although traditional α2 receptor agonists can alleviate withdrawal symptoms, they are often accompanied by obvious adverse reactions of hypotension. Lofexidine is a central α2 adrenergic receptor agonist. It selectively agonizes the α2 receptors in the medullary vasomotor center, inhibits the efferent of sympathetic nerve impulses, and reduces the release level of norepinephrine. While relieving symptoms such as rhinorrhea, sweating, anxiety and muscle pain caused by opioid withdrawal, its effect on blood pressure is significantly weaker than that of clonidine, a drug of the same category. It is mainly used as an adjuvant medication for detoxification treatment of opioid addicts, suitable for opioid dependent people who voluntarily receive withdrawal treatment, and can also be combined with other detoxification regimens to improve treatment compliance.

At present, the market size of drugs for opioid dependence treatment in China is about 230 million yuan, with a compound annual growth rate of 8.7% in the recent 3 years. Among them, α2 receptor agonists account for 32% of the overall adjuvant detoxification medication market, and lofexidine accounts for about 18% of this segment with its better safety. In terms of market competition pattern, currently only 2 domestic enterprises have the approval documents for lofexidine preparations, and the supply of API has been in a relatively tight state for a long time. With the increasing support for detoxification treatment in the field of drug control and the expansion of community maintenance treatment sites, it is expected that the market demand growth rate of lofexidine will remain above 10% in the next 3 years.

The original research enterprise of lofexidine is Britannia Pharmaceuticals of the United Kingdom, and the original brand name is Lofexidine. Its compound patent for the US market expired in 2020, and the core compound patent in China expired as early as 2013. The main dosage form approved by the original research is tablet, with a specification of 0.2mg. The original research tablet has been included in the FDA Orange Book Reference Listed Drug Catalog, and has not yet been included in the Chinese Reference Listed Drug Catalog. According to the domestic API registration platform, a total of 3 enterprises have submitted lofexidine API registration applications, of which 2 have been publicized in Status A, and all the approved preparation varieties are lofexidine tablets with the specification of 0.2mg. (Data as of June 2025, please refer to the official website of CDE for the latest information)

CATO provides a full set of impurity reference standards for lofexidine API, covering the research requirements of the whole path including process impurities and degradation impurities. Most of the products are in stock, and orders placed before 16:00 can be shipped on the same day. All products meet the compliance requirements of multiple regulatory systems such as Chinese Pharmacopoeia and FDA, and can directly support API registration and declaration and quality research related work.