First deuterated drug approved

  title={First deuterated drug approved},
  author={Charles Schmidt},
  journal={Nature Biotechnology},
493 In April, the US Food and Drug Administration cleared the first deuterated drug, Austedo (deutetrabenazine), from Teva of Petach Tikva, Israel, for the treatment of Huntington’sdisease-related movement disorders. Austedo is also the first new treatment in over a decade for this indication. Deuteration has come in and out of fashion for more than 50 years and recently companies have started to pay big sums for heavy-hydrogen drugs. Teva acquired rights to Austedo through its $3.5-billion… Expand
Deuterated Drug Molecules: Focus on FDA-Approved DeutetrabenazinePublished as part of the Biochemistry series "Biochemistry to Bedside".
The FDA granting marketing approval for the first deuterated drug molecule, deutetrabenazine (1; a racemic mixture), which is useful in treating chorea, an involuntary movement disorder associated with Huntington’s disease and tardive dyskinesia. Expand
Deuterated drugs; updates and obviousness analysis
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While the importance of §103 ‘obviousness’ rejections remains in patent applications under current prosecution, IPR of issued patents is developing and will affect likely affect §103 interpretations in this area. Expand
Deutetrabenazine for the treatment of Huntington’s chorea
This review, based largely on a detailed PubMed search, will summarize the pharmacological properties, clinical evidence of efficacy and tolerability of deutetrabenazine in the treatment of HD chorea. Expand
Deuterated active pharmaceutical ingredients: A science-based proposal for synthesis, analysis, and control. Part 1: Framing the problem.
A cross functional team of scientists with expertise in isotope chemistry, process chemistry, analytical chemistry, and drug metabolism and pharmacokinetics have been meeting under the auspices of IQ to define and address questions about deuterated APIs. Expand
Preclinical evaluation of [18F]D3FSP, deuterated AV-45, for imaging of β-amyloid in the brain.
Preclinical studies suggest that [18F]D3FSP is useful as a β-amyloid-targeting PET imaging agent and substituting N-CH3 with N-CD3 at the metabolically labile position may reduce in vivo N-demethylation. Expand
40 Years of Hydrogen–Deuterium Exchange Adjacent to Heteroatoms: A Survey
Deuteration of bioactive molecules is gaining more and more attention, especially after the approval of the first deuterated drug (Austedo™) by the US Food and Drug Administration (FDA). Not only isExpand
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The molecular mechanisms underlying the new treatment modalities in these diseases are described and the encouraging results of ongoing studies for candidate drugs are described. Expand
Synthesis and Biological Evaluation of [18F]FECNT-d4 as a Novel PET Agent for Dopamine Transporter Imaging
The proposed deuterium-substituted DAT radiotracer may serve as a promising PET imaging agent to assess DAT-related disorders and display a high binding affinity for DAT comparable to that of [18F]FECNT in rat striatum homogenates. Expand
Structure-Guided In Vitro to In Vivo Pharmacokinetic Optimization of Propargyl-Linked Antifolates
The resulting compound was characterized and demonstrated to have a low projected clearance in humans with limited potential for drug-drug interactions as predicted by cytochrome P450 inhibition as well as an in vivo exposure profile that optimizes the potential for bactericidal activity, highlighting how structural data, merged with substitutions to introduce metabolic stability, are a powerful approach to drug design. Expand
A rapid MS/MS method to assess the deuterium kinetic isotope effect and associated improvement in the metabolic stability of deuterated biological and pharmacological molecules as applied to an imaging agent.
This work incubates a 1:1 ratio of both the deuterated and protio-form of an imaging agent together in the same liver microsomal assay and determines the relative rate of consumption of both moieties, based upon specific MS-MS transitions unique to both molecules without the need for liquid chromatography-mass spectrometry (LC-MS) and quantification. Expand


Effect of Deutetrabenazine on Chorea Among Patients With Huntington Disease: A Randomized Clinical Trial.
Deutetrabenazine is a novel molecule containing deuterium, which attenuates CYP2D6 metabolism and increases active metabolite half-lives and may therefore lead to stable systemic exposure while preserving key pharmacological activity in patients with Huntington disease. Expand