Drug properties

An in vivo click chemistry reaction could help clear drugs from the circulation in the event of toxicity. The approach involves synthesizing an azide-containing analog of the therapeutic, and administering a clearing agent containing a strained alkyne that reacts with the azide in vivo to yield a product that is rapidly cleared from the circulation. In mice pretreated with an azide analog of warfarin, circulating levels of the analog were below limits of detection within one hour post-injection of a 20-fold excess concentration of a strained bicyclononyne-based clearing agent. Next steps include developing a library of tissue-tropic reactants that could be used to clear other drugs, nanoparticles or metabolites (see "Clearing Chemistry." BioCentury Innovations (June 15, 2017))...