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• W1551685198 abstract "This chapter briefly reviews the use of deuterium to alter the metabolic properties of compounds and discusses the past and current development of potential deuterium-containing drugs. Deuterated compounds have been widely studied in nonclinical settings and have seen broad application as metabolic or pharmacokinetic (PK) probes both in vitro and in vivo. Depending upon a given compound's route of metabolism and the location of the deuterium, deuteration can be metabolically silent, thereby enabling utility as a PK tracer, or it can alter the compound's metabolism, thereby acting as a mechanistic probe. The incorporation of deuterium into pharmacologically active agents offers potential benefits, such as improved exposure profiles and the decreased production of toxic metabolites that could yield improvements in efficacy, tolerability, or safety. Deuterium can be a powerful medicinal chemistry tool, which has received little attention in the context of new drugs. A majority of examples in the chapter are deuterated versions of known, well-characterized drugs with established therapeutic utilities. Most deuterated compounds reported to date appear to retain full biochemical potency and selectivity. However, in select cases, deuterated drugs show a differentiated PK profile versus the hydrogen-only compounds. Scientists in the pharmaceutical industry are using deuterium as a tool to improve drug properties." @default.
• W1551685198 created "2016-06-24" @default.
• W1551685198 creator A5046617419 @default.
• W1551685198 creator A5060714537 @default.
• W1551685198 date "2011-01-01" @default.
• W1551685198 modified "2023-10-11" @default.
• W1551685198 title "Deuterium in Drug Discovery and Development" @default.
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• W1551685198 doi "https://doi.org/10.1016/b978-0-12-386009-5.00003-5" @default.
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