Using Deuterium in Drug Discovery: Leaving the Label in the Drug
Top Cited Papers
- 2 December 2013
- journal article
- review article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 57 (9), 3595-3611
- https://doi.org/10.1021/jm4007998
Abstract
Deuterium, the stable isotope of hydrogen, is known to medicinal chemists for its utility in mechanistic, spectroscopic, and tracer studies. In fact, well-known applications utilizing deuterium exist within every subdiscipline in pharmaceutical discovery and development. Recent emphasis on incorporation of deuterium into the active pharmaceutical ingredient has come about as a result of inquiries into the potential for substantial benefits of the deuterium kinetic isotope effect on the safety and disposition of the drug substance. This Perspective traces the author’s experience in reviving and expanding this potential utility, first suggested many decades prior by the discoverer of this, the simplest of all isotopes.Keywords
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