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Abstract
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.
Highlights
There are notable exceptions, the majority of drugs are administered over the course of several days, or even much longer
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)
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
Summary
There are notable exceptions, the majority of drugs are administered over the course of several days, or even much longer. In such cases, the dose and dosage regimen needs to be designed such that the blood level (concentration) of the drug falls within the therapeutic “window”, i.e., between too low (below the required threshold) and too high (into toxicity). A good design of a dosing regimen keeps the drug’s blood level (surrogate for target organ drug concentration) within the therapeutic window as much as possible throughout the course of therapy. Several factors contribute to a drug’s half-life, but one of the most important for most drugs is the rate of its metabolism [1]. Patient compliance is better when only once-per-day dosing is required [3] [4]
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