Applications of deuterium in medicinal chemistry

T Pirali, M Serafini, S Cargnin… - Journal of medicinal …, 2019 - ACS Publications
The use of deuteration in medicinal chemistry has exploded in the past years, and the FDA
has recently approved the first deuterium-labeled drug. Precision deuteration goes beyond …

Deuterium medicinal chemistry: a new approach to drug discovery and development

SL Harbeson, RD Tung - MedChem News, 2014 - jstage.jst.go.jp
Selective replacement of hydrogen atoms with deuterium (deuteration) has the unique
benefit of retaining the pharmacologic profile of physiologically active compounds while, in …

Deuterium in drug discovery and development

SL Harbeson, RD Tung - Annual reports in medicinal chemistry, 2011 - Elsevier
Publisher Summary 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 medicinal chemistry comes of age

RD Tung - Future medicinal chemistry, 2016 - Taylor & Francis
Deuterium is gaining increased appreciation and utilization as a component of active
pharmaceutical ingredients. Deuteriummodified or-deuterated compounds retain the …

[HTML][HTML] Deuterium in drug discovery: progress, opportunities and challenges

RMC Di Martino, BD Maxwell, T Pirali - Nature Reviews Drug Discovery, 2023 - nature.com
Substitution of a hydrogen atom with its heavy isotope deuterium entails the addition of one
neutron to a molecule. Despite being a subtle change, this structural modification, known as …

[HTML][HTML] Deuterated Drug Molecules: Focus on FDA-Approved Deutetrabenazine: Published as part of the Biochemistry series “Biochemistry to Bedside”

SH DeWitt, BE Maryanoff - Biochemistry, 2018 - ACS Publications
For the longest time, researchers have sought to use deuterium in place of hydrogen in drug
molecules to inhibit metabolic conversion to less active or inactive molecules or to stabilize …

Using deuterium in drug discovery: leaving the label in the drug

TG Gant - Journal of medicinal chemistry, 2014 - ACS Publications
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 …

Impact of deuterium substitution on the pharmacokinetics of pharmaceuticals

EM Russak, EM Bednarczyk - Annals of Pharmacotherapy, 2019 - journals.sagepub.com
Objective: Stable heavy isotopes of hydrogen, carbon, and other elements have been
incorporated into drug molecules, largely as tracers for quantitation during the drug …

Deuterated drugs draw heavier backing: the FDA is considering a first approval of a deuterated drug, and large pharmaceutical companies have started to incorporate' …

A Mullard - Nature Reviews Drug Discovery, 2016 - go.gale.com
If the FDA approves Teva Pharmaceutical's deutetrabenazine next month, it will be giving
the first ever green light to a drug containing deuterium, a heavy isotope of hydrogen …

Deuterated drugs: where are we now?

GS Timmins - Expert opinion on therapeutic patents, 2014 - Taylor & Francis
Introduction: Deuterated versions of existing drugs can exhibit improved pharmacokinetic or
toxicological properties due the stronger deuterium–carbon bond modifying their …