Chinese research team develops a malignant cancer inhibitor

　　China News Service, Hefei, September 25 (Reporter Wu Lan) A reporter learned from the Hefei Research Institute of the Chinese Academy of Sciences on the 25th that researchers from the Institute have developed a malignant cancer inhibitor.

The efficacy evaluation in animals showed that the tumor inhibition rate (TGI) reached 96%.

　　The results are currently published online in the international journal Signal Transduction and Targeted Therapy.

　　Recently, the pharmaceutical team of researcher Liu Qingsong and researcher Liu Jing from the Institute of Health and Medical Technology, Hefei Research Institute, Chinese Academy of Sciences has developed a new generation of highly selective and active BTK kinase inhibitor CHMFL-BTK for B-cell non-Hodgkin’s lymphoma -85.

　　B-cell non-Hodgkin’s lymphoma is a common malignant cancer with an incidence rate of 10-15 per 100,000. Its incidence increases with age, and the survival rate of patients is low.

Bruton's tyrosine kinase (BTK) is a non-receptor tyrosine kinase. A large number of studies have shown that overexpression and activation of BTK kinase is one of the main pathogenic factors that cause this type of cancer.

　　In the preliminary research, the research team has developed a series of BTK kinase inhibitors with independent intellectual property rights through drug design and high-throughput screening methods.

In order to further improve its activity, selectivity and druggability, the research team continued to develop a small molecule inhibitor CHMFL-BTK-85 with good druggability through structure-based drug design methods.

　　Studies on the protein and cell levels show that the inhibitor can significantly reduce the inhibitory effect on immune cell-mediated ADCC compared with the BTK inhibitor ibrutinib that has been marketed.

　　In terms of animal efficacy evaluation, the inhibitor can significantly inhibit the growth of mouse subcutaneous xenograft tumors constructed by TMD8 cells at a dose of 100 mg/kg/day, with a tumor inhibition rate (TGI) of 96%. 1 The mouse orthotopic tumor model constructed by cells can significantly extend the survival time of animals.

　　At present, the research team is conducting further preclinical evaluation of CHMFL-BTK-85, in order to quickly promote the drug to enter the industrial development stage.