Quick and Easy Deuteration and Tritiation of Potential Compounds to Speed Drug Development


During the development of many drugs, radioactive markers and so-called stable labels, typically deuterium and tritium respectively, are often used to trace the destination of  chemical compounds and their metabolites. This is a pretty easy thing to do in lab animals, once you have enough molecules of the compound you’re testing in which typical hydrogen atoms are replaced by their heavier isotopes. Performing this deuteration or tritiation process is currently slow and difficult, taking up to three months to perform on a pretty small amount. Now researchers from Princeton University and Merck, the pharma firm, are reporting in journal Science on a way to compress this process into a day. The development should help to speed the development of new drugs and to get them to market, now a very slow process, a bit faster.

The technique is rather simple, and involves mixing the compound to be tested into a solution of heavy water containing the tritium and deuterium versions of hydrogen. Blue light is shone into this mix, and amazingly the hydrogen atoms swap out, leading some of the hydrogens within the tested compound to be tritium or deuterium.

This was already tested on 18 drugs already used in medicine, as well as candidate drug compounds that Merck is in the process of developing. Because the new technique of deuteration and tritiation is so easy and cheap to perform, drugs in earlier stages of the development process can begin to be tested using injectable labels that would otherwise not qualify due to cost constraints.

Study in Science: Photoredox-catalyzed deuteration and tritiation of pharmaceutical compounds…

Via: Princeton…

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