摘要
药物代谢产物存在质和/或量的种属差异,现综述药物代谢产物安全性评价的重要性及评价策略和评价项目。当发现代谢产物是人特有或人体主要代谢产物高于给药剂量或全身暴露量(二者中的较低者)的10%,特别是这些物质比毒性试验动物体内水平高时更应关注其安全性,必须及早确证这些代谢产物,并进行一般毒性试验、遗传毒性试验、胚胎-胎仔发育试验和致癌试验等。
There do exist quantitative and/or qualitative differences of drug metabolites in species. When metabolites are human unique or major metabolites accounting for greater than 10 percent of drug related materials （ administered dose or systemic exposure whichever is less）, especially these major metabolites are at much higher levels in humans than in the species used during standard nonclinical toxi- cology testing, metabolites must be identified, measured, and characterized as early as possible. Safety assessments such as general toxicity studies, genotoxicity studies, embryo-fetal development studies, and carcinogenicity studies should be carried out if necessary. The importance, strategies and items of safety evaluation of drug metabolites were reviewed.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2006年第14期1145-1148,共4页
Chinese Journal of New Drugs
关键词
代谢产物
安全性评价
种属差异
毒性
metabolite
safety evaluation
species difference
toxicity
