Class 1.1 new drug "anti-Alzheimer's disease" independently developed by the Institute of Biology was approved for clinical trials

  Recently, designed and synthesized by the research group of Hu Wenhui, Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences, and preclinical research led by the South China New Drug Innovation Center, the jointly developed anti-Alzheimer's 1.1 new drug-GIBH130 and its tablets have been awarded the National Foodstuff "Drug Clinical Trial Approval" issued by the Drug Administration (CFDA).

   Alzheimer’s disease (AD), commonly known as Alzheimer’s disease, is a degenerative disease of the central nervous system that causes cognitive impairment and memory impairment in patients, leading to deteriorating living ability and death. Celebrities such as the late former US President Reagan and former British Prime Minister Margaret Thatcher are all troubled and tortured by this disease.

   The pathogenesis of Alzheimer's disease is still unclear, and there is a lack of effective treatment and preventive measures. Clinical drugs are mainly cholinesterase inhibitors (AChEI) and N-methyl-D-aspartate (NMDA) receptor antagonists. Although these drugs are widely used, they can only relieve symptoms to a certain extent and improve patients' cognition, but they cannot cure the disease or even delay the progression of the disease. Regardless of the pathogenesis of AD, neuronal apoptosis and severe brain atrophy are the main causes of Alzheimer’s. As a neuroinflammation inhibitor, GIBH130 can block the excessive activation of glial cells induced by factors such as β-amyloid, inhibit the increase of inflammatory factors in the brain, and reduce neuronal damage, thereby preventing the disease process of AD and alleviating AD symptom.

   After ten years, Hu Wenhui's research group started the project in 2006 and began to build a centralized compound library for neuroinflammation inhibitors. Thanks to funding from Chia Tai Tianqing Pharmaceutical, the research team obtained the anti-neuro-inflammation inhibitor GIBH130, which has drug potential, in 2008. Afterwards, the research team of Sheng Guoqing, Wu Donghai's research team, Dai Renke's research team, Zou Libo's research team of Shenyang Pharmaceutical University, especially the research and development center of the research institute's drug research and development center Michito Trella and other biological teams supported and With the collaboration, it was confirmed that GIBH130 has good in vitro anti-inflammatory effects, good oral availability, easy to penetrate the blood-brain barrier, and superior efficacy in multiple senile dementia animal models such as injection of Aβ amylase and APP/PS1 double transgene. The effect of first-line clinical drugs such as donepezil can be achieved at very low doses.

   In 2012, the Guangzhou Institute of Biomedicine and Health of the Chinese Academy of Sciences and the South China Center for New Drug Development reached a cooperation to jointly conduct preclinical research on the "Class 1.1 Anti-Alzheimer Drug Candidate GIBH130". In 2014, in accordance with the requirements of the relevant technical guidelines of the State Food and Drug Administration, the Innovation Center completed all preclinical studies of GIBH130 and applied for new drug clinical studies. In the end, GIBH130 and its tablets passed the review of experts, and in February 2016, they obtained the "Clinical Trial Approval for Drugs" issued by the State Food and Drug Administration (CFDA).

   At present, GIBH130 has applied for patents in many countries/regions, and has been authorized by the United States, Japan, and Germany. The project has received funding support from Jiangsu Zhengda Tianqing, Guangzhou Science and Technology Bureau, Guangdong Provincial Science and Technology Department, and Guangzhou Institute of Biological Medicine Research and Development Center. It is thanks to the technical support of many scientific teams and the financial support of many departments that "a sword has been sharpened in ten years."

  Different from any existing Alzheimer's drugs, GIBH130 is a new mechanism, a new structure of neuroinflammation inhibitor, with high activity, high bioavailability, good safety, easy availability of raw materials, and simple process. In particular, the dosage is low, and it is expected that patients only need to take it once a day (dose 1-10mg), which is convenient and effective. If the drug can be successfully marketed, it is expected to become a "good drug that Chinese people can afford."