手性药物的毒理学特点和安全性评价要点_闫长会.pdfVIP

Chinese Journal ofNew D rugs 2008, Vol. 17N o. 16 2008 17 16 * , ( 中国人民解放军疾病预防控制所毒理学评价研究中心, 北京 100071) [] 目前临床上使用 很多药物属于手性药物 消旋体, 但手性药物 不同对映体与生物大分子 作用具有不同 选择性, 其立体选择性能够对机体产生不同 毒性作用, 因此手性药物 安全性评价日益 受到重视, 各国政府纷纷颁布法规规范手性药物 毒理学评价通过比较分析不同手性异构体 毒理学作 用特点, 能够加快研发过程, 为临床提供更安全 药物现综述手性药物独特 毒性作用特点以及不同国家 手性药物 安全性评价要点, 阐述其毒理学评价基本过程, 为手性药物 毒理学评价提供参考 [] 手性药物; 立体选择性; 安全性评价 [] R96513 [] A [] 1003- 3734( 2008) 16- 1372- 03 Toxicological characteristics of ch iral drugs and th eir toxicology evaluation YAN Chang-hu,i P NG Shuang-qing (Research and Evaluation Centerf orToxicology, Institute of D iseasePrevention and Control, A cademy of M ilitaryM edicalScience, eijing 100071, China) [ Ab stract] There are many chiral drugs in clinical application. The different enantiomeres of a chiral drug can have distinct effects on the biomacromolecules. The stereoselectivity of chiral drug results in different toxic re- actions, which can have mi portant mi pacts on human health. Therefore, the toxicology evaluation of chiral drugs should be paidmore and more attention, andm any countries published the regulations to standard the toxicology e- valuation. Through the comparison and analysis of the toxicologicalreactions, the developing process can be speed up, and the safer drugs can be provided. This paper outlined the distinctive toxic characteristics and different state- ments in development of chiral drugs, elucidated the process of the toxicology evaluation, and offered information for the toxicology evaluation of chiral drugs. [ Key w ord s] chiral drug; stereoselectivity; safety evaluation , , 2 2 , , , 60% 1 1,