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The First FDA Approved Drug that uses Deuterium

Accepted submission by Anonymous Coward at 2017-04-06 14:51:56

The first deuterated drug has finally been approved by the FDA. It’s Austedo (deutetrabenazine), from Teva, and it targets Huntington’s chorea. This is an interesting development on several levels. The idea of adding deuteriums (instead of plain hydrogens) to drug structures had been kicking around for many years, but only in the last 8 or 10 years has serious development been underway on them.

[...] Deuterium is the (fairly well known) “heavy hydrogen” isotope of regular hydrogen, which is heavy because it has another neutron in it. That basically doubles its weight (the single electron in the atom is a roundoff error in that regard), so these two are an isotope pair with a large percentage difference in weight indeed.
[...] The reason this weight difference makes a difference is when a bond breaks between the hydrogen (or deuterium) and another atom. The bond is actually harder to break with the heavier isotope, an effect that can be modeled surprisingly well with springs and fishing weights. This is the “primary kinetic isotope effect”, and if that bond-breaking is an important step in some process, you can slow the whole works down by just putting in a D where an H used to be. For drugs, the key is that many of them are metabolized and destroyed when they hit they liver, and this is often done through breaking a C-H bond. So a well placed deuterium (or two, or three) can actually have a significant effect on how long a drug will circulate in the bloodstream, by slowing down the liver’s clearance mechanism. [] [] []

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