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The First Approved “Deuterated” Drug: A Short Review of the Concept

The First Approved “Deuterated” Drug: A Short Review of the Concept

作     者:Robert B. Raffa Joseph V. Pergolizzi Robert Taylor 

作者机构:Neumentum Inc. Palo Alto CA USA Colleges of Pharmacy University of Arizona Tucson AZ USA Temple University School of Pharmacy Philadelphia PA USA NEMA Research Inc. Naples FL USA 

出 版 物:《Pharmacology & Pharmacy》 (药理与制药(英文))

年 卷 期:2018年第9卷第10期

页      面:440-446页

学科分类:1002[医学-临床医学] 100214[医学-肿瘤学] 10[医学] 

主  题:Deuterium Drug Structure Chemical Bonds Drug Metabolism Duration of Action 

摘      要:The first “deuterated drug has recently been approved by the U.S. FDA (Food & Drug Administration). A “deuterated drug is a drug in which the hydrogen atom in one or more of the carbon-hydrogen bonds in its chemical structure is replaced by deuterium (“heavy hydrogen, a hydrogen isotope that has a neutron, i.e., one neutron instead of the usual no neutrons). A carbon-deuterium (C-D) bond is more stable in the body than a carbon-hydrogen (C-H) bond. If the deuterium is strategically located in a drug’s chemical structure, the extra stability of the bond will be more resistant to metabolic breakdown, and the duration of drug action will be prolonged. We review the general concept of deuterated drugs, historical examples of the classes of application, and the new approval.

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