News
The Alzheimer's disease drug huperzine A controlled-release tablet has been approved to enter clinical trials.
Date:
01 Mar,2021
On June 11, 2018, the Class 2.2 new drug Huperzine A controlled-release tablets (FN12), jointly developed through collaborative efforts by Wanbangde Pharmaceutical and the research teams led by Gan Yong and Zhang Haiyan at the Shanghai Institute of Materia Medica, Chinese Academy of Sciences, received clinical trial approval from the National Medical Products Administration, officially clearing the way for its entry into clinical trials. The approval number is 2018L02643. Currently, there are no Huperzine A controlled-release products available for clinical use in China.
As early as 2016, Wanbangde Pharmaceutical signed a technology transfer and industrialization cooperation agreement with the Shanghai Institute of Materia Medica, Chinese Academy of Sciences, focusing on the research and development of a new anti-Alzheimer’s drug—Huperzine A controlled-release tablets. The recent approval of clinical trial permits for this innovative drug marks a significant breakthrough for Wanbangde Pharmaceutical in the field of cutting-edge pharmaceutical R&D.
Huperzine A is a highly effective, highly selective, and reversible acetylcholinesterase inhibitor derived from Huperzia serrata, a traditional Chinese medicinal herb. Clinically, it is used in China to treat benign memory impairment and Alzheimer’s disease. However, the conventional twice-daily dosing regimen of Huperzine A often leads to poor patient compliance among Alzheimer’s disease (AD) patients. Moreover, given the widespread distribution of acetylcholinesterase—both in the central nervous system and peripherally—increasing the dosage to enhance efficacy frequently results in heightened cholinergic side effects in the peripheral nervous system, thereby limiting further dose escalation and ultimately compromising the drug’s therapeutic potential.
To further enhance the efficacy, safety, and patient compliance of this drug in Alzheimer’s disease (AD) patients, under the guidance of Academician Tang Xican, Gan Yong’s research team and Zhang Haiyan’s team addressed the limitations of huperzine A—namely, its rapid burst release in peripheral plasma and relatively short half-life. Leveraging huperzine A’s unique central nervous system pharmacokinetics, characterized by slow elimination, as well as its central acetylcholinesterase-targeted pharmacodynamics featuring prolonged, yet controlled drug action, they designed and developed a novel, dual-phase controlled-release tablet with huperzine A that meets the precise temporal and spatial delivery requirements. Preclinical studies—including pharmacokinetic, pharmacodynamic, and toxicological assessments—demonstrated that this innovative formulation significantly reduces the abrupt release of the original huperzine A molecule, ensuring a steady and sustained drug release profile. Moreover, it markedly extends both the duration of drug maintenance and the persistence of therapeutic effects, while minimizing peripheral cholinergic side effects. As a result, this huperzine A-controlled-release tablet holds great promise for achieving multiple therapeutic goals, including improved patient adherence, long-lasting efficacy, and reduced toxicity, positioning it as a promising candidate for future clinical development.
The development of the controlled-release tablets containing huperzine A also received strong support from research groups led by Dr. Chuan Li and Dr. Dafang Zhong at the Drug Metabolism Research Center of the Shanghai Institute of Materia Medica. Additionally, the project was funded through the New Drug Discovery Program at the Shanghai Institute of Materia Medica, Chinese Academy of Sciences.
Related Recommendations