Phase I clinical study of azvudine (FNC), an anti HIV drug, showed significant effect

According to the website of the Chinese Academy of Sciences, nucleoside reverse transcriptase inhibitors (NRTIs) are an important part of anti HIV drugs, and also constitute the basic component of effective antiretroviral therapy (HARRT) Azvudine (FNC) is a new cytosine analogue It is different from other nucleoside reverse transcriptase inhibitors in 2 `, 3 ` - dideoxynucleoside FNC contains 3 ` - Oh, so its mechanism is different from the listed nucleoside reverse transcriptase inhibitors Zheng Yongtang, research group of the Key Laboratory of animal model and human disease mechanism of Kunming Institute of zoology, Chinese Academy of Sciences, and Chang Junbiao, Professor of School of chemistry and molecular engineering, Zhengzhou University, jointly studied the in vitro anti HIV activity of FNC The results showed that FNC has excellent anti HIV-1 activity, and its in vitro activity is better than the listed cytosine analogues lamivudine (3TC) and en FTC, EC50 is only 1 / 2000 of 3TC FNC also showed good inhibitory activity on HIV resistant strains, including M184V, a highly resistant strain of 3TC In vitro drug resistance studies showed that the main drug resistance mutation of FNC was M184I, and molecular docking simulation showed that it was probably due to the influence of the azide group of FNC that it was not easy to transform to M184V FNC also showed a good combination of drug activity, with the listed nucleoside reverse transcriptase inhibitor - zidovudine (AZT), 3TC, non nucleoside reverse transcriptase inhibitor - nevirapine (NVP), membrane fusion inhibitor - enfluviride (T-20), integrase inhibitor - retegvir (RAL) and protease inhibitor - indenavir (IDV) and other six drugs have a good synergistic effect The above results show that FNC has good anti HIV activity and development potential According to the above research results, FNC has obtained the clinical research approval from the State Food and Drug Administration (CFDA) in April 2013, and the new drug is currently undergoing phase I clinical research The research results were published in the international academic journal PLoS One (Public Science Library - Comprehensive) (2014, 9 (8): e105617) Wang Ruirui, an associate researcher of Kunming Institute of zoology, is the first author, and Zheng Yongtang, a researcher, and Professor Chang Junbiao are the co correspondents In addition, Huang Jingfei, research group of National Key Laboratory of genetic resources and evolution of Kunming Institute of zoology, participated in the research Relevant research was supported by major national science and technology projects, National Natural Science Foundation and other projects Inventor: Chang Junbiao, male, born in October 1965 in Huaxian County, Henan Province In 1986, he graduated from the Department of chemistry of Henan University, and in 1989, he graduated from Zhengzhou University of science and technology of China; in 1996, he graduated from Peking Union Medical University, and in 1996-1998, he graduated from the University of Georgia, USA; in 2000-2002, he visited scientists at Novartis gene Research Institute (G stork Foundation) At present, he is vice president of Zhengzhou University, part-time professor of China University of science and technology, doctoral supervisor, part-time professor of Tianjin University, doctoral supervisor, member of national pharmacopoeia committee, director of Henan fine chemical Key Laboratory, and director of Henan analysis and test center Engaged in the research of organic chemistry and pharmaceutical chemistry, the research direction is the synthesis of antiviral drugs (hepatitis B, AIDS), successively presided over the National Science Fund for Distinguished Young Scholars, the National Natural Science Fund, the national key basic research and development plan (973 Plan), the national high technology research and development plan (863 plan), the national major new drug project, and the new century of the Ministry of education Talent support program He presided over and completed the "Research on the total synthesis of schisandrin A and a, the active component of schisandrin" in the world For the first time, he biomimetically synthesized the same bioactive products as natural schisandrin A and a, which has a good development prospect For a series of compounds whose receptor structure is unknown but nearly effective, he analyzed the molecular pharmacophore and its conformation through computer-aided research A series of new nucleoside compounds were synthesized The pharmacological screening and animal experiments showed that some compounds have high anti AIDS activity and little side effects As the host of the project, he won one second prize of national science and Technology Progress Award; in 2006, he won the first prize of science and technology progress award of Henan Province, three second prizes of science and technology progress award of Henan Province; five third prizes; two American invention patents; 18 national invention patents of China, which produced remarkable social and economic benefits He has applied for 2 international invention patents, 16 Chinese invention patents, published more than 160 papers and 7 academic monographs in nature; science; chem.rev., a famous international journal, and China 16 doctoral students and 46 master students were trained Honorary title: in 1998, he was awarded the "national young and middle-aged experts with outstanding contributions"; in 1999, he enjoyed the special government allowance of the State Council; in 2004, he was awarded the "national candidate for the new century million talents project"; in 2008, he was awarded the "Central Plains scholars" in Henan Province.