摘要
近年来,氘代药物引起了制药行业越来越多的关注。自2008年至今,已有1个氘代药物获FDA批准,多个处于临床Ⅲ期研究。综述了氘代药物的研发现状,并重点介绍氘代修饰对药物的3种影响:减缓药物代谢和改善药代动力学、减少毒性代谢物、引起其他生物效应。此外,对氘代药物研发前景、专利权问题以及在发现新化学实体方面的应用进行了阐述。
In recent years, deuterated drugs have received increasing attention from pharmaceutical industry. Since 2008, one drug has been approved by FDA and several candidates have entered phase Ⅲ clinical trial. In this paper, the current development of deuterated drugs in pre- clinical and clinical stages was reviewed, and three scnarios after drug deuteration were introduced, including slowed drug metabolism and improved pharmacokinetics, reduced toxic metabolites and induction of other biological effects. Furthermore, a general outlook of future R＆D, concerns on patent rights and application in the discovery of new chemical entities were described.
出处
《药学进展》
CAS
2017年第12期902-918,共17页
Progress in Pharmaceutical Sciences
关键词
氘代药物
氘同位素效应
药物代谢
药代动力学
活性代谢物
创新药研发
deuterated drug
deuterium isotope effect
drug metabolism
pharmacokinetics
active metabolites
innovative drug research and development
