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OBESITY RESEARCH SOLUTIONSPitavastatin lactone is a major phase 2 metabolite of the HMG-CoA reductase inhibitor pitavastatin (Item No. 15414).1,2 Pitavastatin lactone is formed when pitavastatin undergoes glucuronidation by the UDP-glucuronysyltransferase (UGT) isoforms UGT1A1, UGT1A3, or UGT2B7 to form pitavastatin glucuronide, which then undergoes non-enzymatic conversion to pitavastatin lactone. It can be retroconverted to pitavastatin via hydrolysis.
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1. Metabolic fate of pitavastatin, a new inhibitor of HMG-
2. Pharmacological profile of a novel synthetic inhibitor of 3-