新藥評(píng)價(jià)已經(jīng)成為新藥研發(fā)中最關(guān)鍵的階段，也是安全合理用藥所面臨的重大課題。近年來(lái)，藥動(dòng)學(xué)–藥效學(xué)（PK/PD）模型受到了越來(lái)越廣泛的關(guān)注，這一模型是將PK和PD兩個(gè)相互關(guān)聯(lián)的動(dòng)力學(xué)過(guò)程有機(jī)地結(jié)合起來(lái)，同時(shí)探討機(jī)體對(duì)藥物的作用及藥物對(duì)機(jī)體的作用，為更全面和準(zhǔn)確地了解藥物的效應(yīng)隨劑量（或濃度）及時(shí)間而變化的規(guī)律，從而為臨床用藥的安全性和有效性提供更為科學(xué)的理論依據(jù)。著重綜述PK/PD模型的發(fā)展和在臨床前和臨床中的應(yīng)用，證實(shí)了PK/PD模型可以為新藥評(píng)價(jià)提供有效的理論指導(dǎo)，并大幅度縮短實(shí)驗(yàn)周期，節(jié)省實(shí)驗(yàn)資源，比傳統(tǒng)的藥物開(kāi)發(fā)策略更加準(zhǔn)確可靠。隨著藥物評(píng)價(jià)學(xué)的不斷完善，模擬軟件和模擬條件的標(biāo)準(zhǔn)化，PK/PD模型在未來(lái)的藥物開(kāi)發(fā)中必將更充分地發(fā)揮其重要作用并加速藥物開(kāi)發(fā)的進(jìn)程。

Drug evaluation has become one of the most critical stages during drug development as well as an important tool to assess the efficacy and safety of novel drugs. Pharmacokinetics/pharmacodynamics (PK/PD) modeling, taking both PK and PD process into consideration and thus comprehensively understanding the relationship between dosing (concentration) and time, has drawn more and more attention from the public recently. By investigating the interaction between the drug and the body system, it provides more valuable information for drug application. In this paper, the development history of PK/PD modeling and its application in preclinical and clinical practice will be discussed. It is now proved that the PK/PD modeling can shorten the research cycle, save the experiment resource, and is more accurate and reliable than traditional drug development strategy. With the constant improvement of drug evaluation, the standardization of analytical software, and its simulation process, PK/PD modeling will play more and more important role in drug development and accelerate the overall process.

國(guó)家973項(xiàng)目（2010735602）和天津市科技計(jì)劃項(xiàng)目（08JCYBJC07500）