Abstract
Many drugs have adverse absorption, distribution, metabolism, and
excretory (ADME) properties that prevent their widespread use or limit
their use in some indications. In addition to preparation techniques and
prodrug strategies, deuterium modification is a viable method for
improving ADME properties. Deuteriated drugs have attracted increasing
attention from the pharmaceutical industry in recent years. To date, two
deuterated drugs have been approved by the FDA. In 2017, austedo was
approved by the FDA as a new drug for huntington’s disease in the United
States, which is the first deuterium drug to be marketed in the world.
Recently (June 9, 2021), donafinil is listed in China, this result has
caused major pharmaceutical companies and the pharmaceutical industry to
pay attention to deuterium technology again. In addition, BMS-986165,
RT001, ALK-001, HC-1119, AVP-786 and other drugs are in phase Ⅲ clinical
studies, and some deuterium solid compounds have entered phase I and
Ⅱclinical trials. At present, deuterium strategy has been widely used in
pharmaceutical research, and has become a hot spot in pharmaceutical
research in recent years.In this paper, the research and development of
deuterated drugs are reviewed, and the influence of deuterium
modification on drugs, the advantages of deuterium strategies and the
synthesis strategies of deuterated drugs are mainly introduced. Hope to
provide reference for clinical application, discovery of new deuterium
chemical entities and research and development of new deuterated drugs.