本文選題：克立 + 藥物化學(xué)��； 參考：《藥學(xué)學(xué)報(bào)》2017年06期

【摘要】：新藥創(chuàng)制是復(fù)雜的智力活動(dòng),涉及科學(xué)研究、技術(shù)創(chuàng)造、產(chǎn)品開發(fā)和醫(yī)療效果等多維科技活動(dòng)。每個(gè)藥物都有自身的研發(fā)軌跡,而構(gòu)建化學(xué)結(jié)構(gòu)是最重要的環(huán)節(jié),因?yàn)樗w了藥效、藥代、安全性和生物藥劑學(xué)等性質(zhì)。本欄目以藥物化學(xué)視角,對(duì)有代表性的藥物的成功構(gòu)建,加以剖析和解讀。Anacor公司從生化機(jī)制出發(fā)研究抗菌藥,后轉(zhuǎn)向抗真菌藥收獲了抗甲癬藥他伐硼羅;還從炎癥的靶標(biāo)磷酸二酯酶4和炎癥因子入手,研發(fā)出治療過敏性皮炎的克立硼羅。研發(fā)過程探索了多種可能與渠道,雖然有些與最終目標(biāo)未能搭界,但始終堅(jiān)持研究有機(jī)硼酸酯類的執(zhí)著精神,積累了許多經(jīng)驗(yàn),終于誕生兩個(gè)首創(chuàng)藥。研發(fā)過程涉及的藥物化學(xué)、分子生物學(xué)和作用機(jī)制等研究思路,值得借鑒。由于克立硼羅的安全有效和潛在的市場(chǎng)價(jià)值,輝瑞公司以52億美元收購(gòu)了該公司。本文以藥物化學(xué)視角簡(jiǎn)析兩個(gè)藥物的創(chuàng)制過程。
[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.
【作者單位】： 中國(guó)醫(yī)學(xué)科學(xué)院 北京協(xié)和醫(yī)學(xué)院藥物研究所;
【分類號(hào)】：R914

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