手性药物的毒理学特点及安全性评价要点

Toxicological characteristics of chiral drugs and their toxicology evaluation

目前临床上使用的很多药物属于手性药物的消旋体,但手性药物的不同对映体与生物大分子的作用具有不同的选择性,其立体选择性能够对机体产生不同的毒性作用,因此手性药物的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的毒理学评价。通过比较分析不同手性异构体的毒理学作用特点,能够加快研发过程,为临床提供更安全的药物。现综述手性药物独特的毒性作用特点以及不同国家手性药物的安全性评价要点,阐述其毒理学评价基本过程,为手性药物的毒理学评价提供参考。

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 reactions, which can have important impacts on human health. Therefore, the toxicology evaluation of chiral drugs should be paid more and more attention, and many countries published the regulations to standard the toxicology evaluation. Through the comparison and analysis of the toxicological reactions, the developing process can be speed up, and the safer drugs can be provided. This paper outlined the distinctive toxic characteristics and different statements in development of chiral drugs, elucidated the process of the toxicology evaluation, and offered information for the toxicology evaluation of chiral drugs.