含硼外用药他伐硼罗和克立硼罗的研制

发布时间：2018-06-25 19:15

本文选题：克立 + 药物化学　；参考：《药学学报》2017年06期

【摘要】：新药创制是复杂的智力活动,涉及科学研究、技术创造、产品开发和医疗效果等多维科技活动。每个药物都有自身的研发轨迹,而构建化学结构是最重要的环节,因为它涵盖了药效、药代、安全性和生物药剂学等性质。本栏目以药物化学视角,对有代表性的药物的成功构建,加以剖析和解读。Anacor公司从生化机制出发研究抗菌药,后转向抗真菌药收获了抗甲癣药他伐硼罗;还从炎症的靶标磷酸二酯酶4和炎症因子入手,研发出治疗过敏性皮炎的克立硼罗。研发过程探索了多种可能与渠道,虽然有些与最终目标未能搭界,但始终坚持研究有机硼酸酯类的执着精神,积累了许多经验,终于诞生两个首创药。研发过程涉及的药物化学、分子生物学和作用机制等研究思路,值得借鉴。由于克立硼罗的安全有效和潜在的市场价值,辉瑞公司以52亿美元收购了该公司。本文以药物化学视角简析两个药物的创制过程。
[Abstract]:New drug creation is a complex intellectual activity involving multi-dimensional scientific and technological activities such as scientific research, technological creation, product development and medical effects. Each drug has its own R & D track, and the construction of chemical structures is the most important step because it covers pharmacodynamics, pharmacology, safety and biopharmaceutical properties. From the perspective of pharmacochemistry, this column analyzes and interprets the successful construction of representative drugs. Anacor Company studies antimicrobial drugs from the biochemical mechanism, and then turns to antifungal drugs to harvest the antifungal drug tavaborol; From the inflammatory target phosphodiesterase 4 and inflammatory factors, the development of allergic dermatitis treatment Kriborol. The research and development process explored a variety of possibilities and channels, although some did not match the ultimate goal, but always adhere to the persistent spirit of studying organic borate esters, accumulated a lot of experience, and finally the birth of two first drugs. The research ideas of drug chemistry, molecular biology and action mechanism involved in the R & D process are worthy of reference. Because of its safe, efficient and potential market value, Pfizer bought the company for $5.2 billion. In this paper, the creation process of two drugs is briefly analyzed from the perspective of pharmacochemistry.
【作者单位】：中国医学科学院北京协和医学院药物研究所;
【分类号】：R914

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