page_title: Lesinurad
section_title: Pharmacokinetics
hierarchical_section_title: Lesinurad / Pharmacology / Pharmacokinetics
context_page_description: Lesinurad is a urate transporter inhibitor for treating high blood uric acid levels associated with gout. It is only recommended together with either allopurinol or febuxostat when these medications are not sufficient.
  It received FDA approval on 22 December 2015. The European Commission granted a marketing authorisation valid throughout the European Union on 18 February 2016. In February 2019, it was discontinued in the United States by its manufacturer for business reasons.
context_section_description: Lesinurad is quickly and practically completely absorbed from the gut. Highest blood plasma concentrations are reached after one to four hours. When in the bloodstream, the substance is almost completely (>98%) bound to plasma proteins, mainly albumin.
  It is metabolized mainly by the liver enzyme CYP2C9 to various oxidation products, predominantly to a hydroxylated substance called M3 and an epoxide, M3c. The latter is quickly hydrolyzed to the diol M4 by microsomal epoxide hydrolase (mEH). The enzymes CYP1A1, CYP2C19 and CYP3A only play minor roles in its metabolization. Glucuronidation by the enzymes UGT1A1 and UGT2B7 has also been detected.
  Lesinurad is excreted via the urine (63%) and feces (32%), with a biological half-life of about five hours. Of the excreted dose, 30% are unchanged lesinurad, and the rest are metabolites.
caption: The main metabolic pathways in humans.[7] Involved enzymes are 2C9 = CYP2C9 and mEH = microsomal epoxide hydrolase.