Deuterium in Drug Discovery and Development
作者： Scott L. Harbeson , Roger D. Tung
DOI: 10.1016/B978-0-12-386009-5.00003-5
关键词: Pharmacokinetics 、 Drug discovery 、 In vivo 、 Pharmaceutical industry 、 Drug 、 Context (language use) 、 Deuterium 、 Biochemistry 、 Chemistry
摘要: Publisher Summary This chapter briefly reviews the use of deuterium to alter metabolic properties compounds and discusses past current development potential deuterium-containing drugs. Deuterated have been widely studied in nonclinical settings seen broad application as or pharmacokinetic (PK) probes both vitro vivo. Depending upon a given compound's route metabolism location deuterium, deuteration can be metabolically silent, thereby enabling utility PK tracer, it metabolism, acting mechanistic probe. The incorporation into pharmacologically active agents offers benefits, such improved exposure profiles decreased production toxic metabolites that could yield improvements efficacy, tolerability, safety. Deuterium powerful medicinal chemistry tool, which has received little attention context new A majority examples are deuterated versions known, well-characterized drugs with established therapeutic utilities. Most reported date appear retain full biochemical potency selectivity. However, select cases, show differentiated profile versus hydrogen-only compounds. Scientists pharmaceutical industry using tool improve drug properties.
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