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    Home > Active Ingredient News > Drugs Articles > Shanghai Pharmaceutical Institute's "national class 1.1 new drug Antofloxacin hydrochloride" project won the second prize of 2017 national technological invention

    Shanghai Pharmaceutical Institute's "national class 1.1 new drug Antofloxacin hydrochloride" project won the second prize of 2017 national technological invention

    • Last Update: 2018-01-09
    • Source: Internet
    • Author: User
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    Source: Dream pursuing tour January 8, 2018, 2017 National Science and technology award conference was held in Beijing Led by Yang Yushe, researcher of Shanghai Institute of pharmaceutical research, Chinese Academy of Sciences, and cooperated with Anhui Global Pharmaceutical Co., Ltd., the "national class 1.1 new drug Antofloxacin hydrochloride" project won the second prize of 2017 national technical invention (the main completers are Yang Yushe, Wang Xiang, Jiang Hualiang, Chen Kaixian, Zhang Shu, Ji Ruyun, etc.) Fluoroquinolones (floxacin) are one of the three main varieties of antibacterial drugs in China, which play an important role in ensuring the health of Chinese people Although the first generation of quinolones, nalidixic acid, was imitated in China as early as 1967, there has been no innovative drug in this field for more than 40 years Yang Yushe Ji Ruyun, a scientist from Shanghai Institute of pharmaceutical research, Chinese Academy of Sciences, began to study the synthesis methodology, structure-activity relationship, structure-generation relationship, structure-toxicity relationship, and drug-forming property of fluoroquinolones with the support of NSFC, "863" plan, major national new drug creation project, and knowledge innovation project of Chinese Academy of Sciences, etc., and here Based on the rational drug design and the strategy of structural optimization, 5 classes of 62 new compounds were designed and synthesized After 16 years, the first class 1.1 new chemical drug, Antofloxacin hydrochloride, with novel chemical structure (NCE) and independent intellectual property rights, was successfully launched in 2009 Antofloxacin hydrochloride is a new molecular entity with a new chemical structure By creatively optimizing the molecular structure and introducing an amino group at the 5-position of the mother nucleus, the antibacterial activity (superior to cyclopropane and ofloxacin, which are excellent varieties of fluoroquinolones) and the metabolic properties are significantly improved, the cardiovascular safety is greatly improved, the phototoxicity is eliminated, and the corresponding compounds are obtained patent for synthetic method and use (ZL 97106728.7) Antofloxacin hydrochloride is a successful example of joint development of innovative drugs by scientific research institutes and enterprises in China In 2001, Anhui Global Pharmaceutical Co., Ltd accepted the transfer of original patent technology of Antofloxacin and its derivatives, jointly carried out phase I, II and III clinical research, and combined production and research, which accelerated the pace of research and development of this product to market Compared with the same kind of drugs, Antofloxacin hydrochloride is superior in both efficacy and safety First, there is almost no phototoxicity; second, the safety of the heart is greatly improved; third, the pharmacokinetic performance is excellent; fourth, the clinical treatment of various acute bacterial infectious diseases has excellent efficacy and safety In addition, Antofloxacin hydrochloride overcomes the shortcomings of the original fluoroquinolones, such as weak antibacterial activity, poor metabolic properties and large side effects It is a safer and more efficient new generation of fluoroquinolones, which benefits the majority of patients in China By the end of 2016, Antofloxacin hydrochloride tablets had been used in more than 150 hospitals and medical institutions in 22 provinces and autonomous regions, including Beijing and Chongqing, and entered the medical insurance catalogue of more than 10 local provinces and cities, with sales of more than 2.82 million boxes and sales of about 235 million yuan, benefiting more than 1 million patients The successful development of Antofloxacin hydrochloride has filled in the gap of independent innovation in the field of fluoroquinolones in China for more than 40 years It is the first chemical innovative drug created by Chinese scientists since the implementation of the drug patent law in 1993 It has made positive contributions to promoting the historical transformation of China's pharmaceutical industry from imitation to innovation It has been rated as the "Eleventh Five Year Plan" national major new drug creation Major landmark achievements of special project At the award ceremony, researcher Yang Yushe took a photo of researcher Yang Yushe and his team in the laboratory before the award ceremony (second from the right: Yang Yushe)
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