Substituting deuterium for protium at carbon-hydrogen chemical bond locations targeted by metabolic enzymes can help to slow down the breakdown of a drug, thus increasing its half-life in the body. This is due to the kinetic isotope effect, which increases the bond strength between deuterium and carbon in comparison to protium-carbon bond. Longer duration of action of a drug means that patients can take their medication less frequently without decreasing the efficacy of treatment. As additional benefits to the patient, deuteration can reduce drug interactions due to metabolic switching, and increase the patient’s tolerance of a medication.
What are deuterated drugs?
The first deuterated drug to enter the market was deutetrabenazine (deuterated tetrabenazine) from Teva pharmaceuticals in 2017, and it is intended for the treatment of Huntington’s chorea. The benefits of deuteration for this drug are the extended half-life and more stable blood levels of an active metabolite.
Another example of the attractiveness of deuterated pharmaceuticals is the deuterium chemistry platform for drug discovery at Concert Pharmaceuticals, based in Lexington, KY. Their current pipeline includes CTP-543 (deuterated ruxolitinib) in Phase III clinical trials for the treatment of Alopecia areata, and CTP-692 (a deuterium-modified form of D-serine) in Phase II clinical trials for the treatment of schizophrenia.
It has also been shown, that deuteration can help to stabilize drug enantiomers. Although there has been limited exploration in this area outside of basic scientific experiments, this approach could prove to be extremely beneficial in harnessing the potential of pure enantiomers over racemic mixtures. For example, deuteration of the chiral center was explored in stabilizing the enantiomers of thalidomide, because they have unique pharmacological profiles.
Deuteration has the potential to solve several issues with many current drugs, and it is a feasible tool that medicinal chemists should keep in their toolbox. We at deutraMed will be following closely the momentum that deuterated pharmaceuticals are gaining.
About deutraMed
Where do we fit into this story? deutraMed was created in 2017 to help supply deuterated ingredients. The founders, a diverse team of industry professionals, saw a need for a focused and reliable supply of such ingredients. And, it’s not just the drug industry that can benefit from deuterated ingredients. These compounds have applications in a number of fields, from the life sciences to high technology.
Our experts can help you with leading deuterium solutions, expertise, long-term supply, CRO and CMO partnerships, and new product releases. Schedule a call with our experts to learn more.
