cidoxepin / Elorac - LARVOL DELTA

Use of Phenotypically Poor Metabolizer Individual Donor Human Liver Microsomes to Identify Selective Substrates of UGT2B10. (PubMed, Drug Metab Dispos) - "Of these, dothiepin, cidoxepin, cyclobenzaprine, azatadine, cyproheptadine, bifonazole, and asenapine were indicated to be selective UGT2B10 substrates which have not previously been described...SIGNIFICANCE STATEMENT: The role of highly polymorphic UGT2B10 is likely to be underestimated currently for many compounds cleared via N-glucuronidation due to high test concentrations often used in vitro and low activity of UGT2B10 preparations. The methodology described in this study can be combined with the assessment of UGT vs oxidative in vitro metabolism to rapidly identify compounds likely to be sensitive to UGT2B10 polymorphism, enabling either chemical modification or prospective exposure polymorphism risk assessment to be performed before candidate selection."

Clinical • Journal