Perspective

Using Deuterium in Drug Discovery: Leaving the Label in the Drug

Recondite Falls Discovery, LLC, Greengarden Blvd, Erie, Pennsylvania 16509 United States
J. Med. Chem., 2014, 57 (9), pp 3595–3611
DOI: 10.1021/jm4007998
Publication Date (Web): December 2, 2013
Copyright © 2013 American Chemical Society
*E-mail: tgant@reconfalls.com. Phone: (978) 500-7267.
Biography

Thomas G. Gant completed undergraduate studies at Wayne State University, MI, and doctoral studies at Colorado State University. Postdoctoral studies were carried out at Harvard University, MA, under the mentorship of Nobel laureate Professor E. J. Corey. His professional career in drug discovery and DKIE applications to medicines began at Pfizer (1995), moving then to Millennium Pharmaceuticals, leading the chemistry efforts for the Velcade backup. He then became the Scientific Founder (2004) and CSO of Auspex Pharmaceuticals, completing the first clinical trial to directly demonstrate a substantial kinetic isotope effect of a deuterated drug (SD-254) in humans. He is currently Associate Professor and Director of Pharmacy Post-Baccalaureate studies at Lake Erie College of Osteopathic Medicine, PA, and is President of the pharmaceutical consulting firm Recondite Falls Discovery, LLC.

Abstract

Abstract Image

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.

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Article Views: 6,651 Times
Received 29 May 2013
Published online 2 December 2013
Published in print 8 May 2014
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