Urate Transport Inhibitors: Compounds Designed for Their Uricosuric Action


Heightened urate levels are prevalent in a variety of disease states, including gout, hypertension, diabetes, and cardiovascular disease. Currently, there are few drugs approved in the USA for the lowering of blood urate levels. Among those marketed, many either have extreme unintended maladies, like Stevens Johnson syndrome, require frequent dosing, or show low activity. Researchers at the University of Colorado have synthesized a number of new chemical structures which show potent inhibition of urate transport proteins and have IC50 values on the order of nanomolar concentrations. The lab has probed dozens of compounds and determined a metric for preferable use while also illustrating proof-of-concept oral administration with in vivo mouse experiments. Increasing demand for treatment of diseases involving hyperuricemia position these compounds to be desirable as clinical trial candidates.


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For Information, Contact:
Mary Tapolsky
University of Colorado
Michael Wempe
Hitoshi Endou
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