第一个批准的“氘化”药物:概念的简短回顾

R. Raffa, J. Pergolizzi, R. Taylor
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引用次数: 7

摘要

第一种“氘化”药物最近获得了美国食品药品管理局(FDA)的批准。“氘化”药物是一种药物,其化学结构中一个或多个碳氢键中的氢原子被氘(“重氢”,一种氢的同位素,有一个中子,即一个中子而不是通常的没有中子)所取代。碳-氘(C-D)键在体内比碳-氢(C-H)键更稳定。如果将氘策略性地放置在药物的化学结构中,则该键的额外稳定性将更能抵抗代谢分解,并且药物作用的持续时间将延长。我们回顾了氘化药物的一般概念,历史上申请类别的例子,以及新的批准。
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The First Approved “Deuterated” Drug: A Short Review of the Concept
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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