The use of stable isotopes in drug metabolism studies

Abstract The use of stable isotopes in drug metabolism studies and drug design are described here. Stable isotopes have been reported as tracers and labels, which allow scientists to utilize a variety of experimental techniques to monitor and study drug metabolism without the use of radioisotopes. In addition, recent findings relating to incorporation of deuterium as a strategy for drug design is described as well. Guidance and mechanistic reasoning for deuterated drugs as tools and clinical compounds to solve metabolism-related issues are provided. This includes, but is not limited to, half-life, bioavailability, reactive metabolite formation, and drug-drug interactions. Clinical case studies are included, with guidance on how to effectively capitalize on the chemical advantages of deuterium for metabolism-guided design.