药物代谢研究在新药开发中的作用（The role of drug metabolism in the development of new drugs）.docVIP

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药物代谢研究在新药开发中的作用（The role of drug metabolism in the development of new drugs）.doc

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药物代谢研究在新药开发中的作用（The role of drug metabolism in the development of new drugs）

药物代谢研究在新药开发中的作用（The role of drug metabolism in the development of new drugs） The role of drug metabolism in the development of new drugs Zhao Dongmei *, Li Yan Lu Yehong., 1 (Institute of medicine, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, china; 1 、 Department of oncology, School of pharmacy, New Jersey State University, New Jersey, USA The process of new drug research can generally be divided into drug design and drug discovery Two stages. Drug design included: (1) targeting a particular treatment Target design lead compounds, (2) according to the pharmacological properties of lead compounds, Structural modification of toxicology and metabolism to obtain new candidate In the drug development stage, the candidate is mainly treated with drug efficacy and toxicity Assessment。 The study of drug metabolism has played an important role in these two stages Use. In the design phase of new drugs, the metabolism of lead compounds is too fast Or produce the characteristics of the toxic metabolite, structural modification to achieve safety Stable candidate, so that it has greater development value, can also be synthesized The structure of effective metabolites or analog effective metabolites to obtain new candidates While in the new drug development phase, various in vitro models are used for candidates Metabolic characteristics (e.g., enzyme induction, inhibition, and metabolism of enzymes Classes, the generation of active metabolites, etc., may be subjected to high-throughput screening in order to Determine whether or not the drug has continued development in the early stages of research and development, Metabolic studies in vivo can be used to infer the presence of drugs in laboratory animals Biotransformation patterns in the human body. A recent report in the United States pointed out, Only 10% of new drug candidates are available in the drug study Field [1], and about 40% of the drugs are due to no in vivo activity or drug gene