Pitavastatin lactone-d4 is intended for use as an internal standard for the quantification of pitavastatin lactone by GC- or LC-MS. Pitavastatin lactone is a major phase 2 metabolite of the HMG-CoA reductase inhibitor pitavastatin .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.
1.Fujino, H., Yamada, I., Shimada, S., et al.Metabolic fate of pitavastatin, a new inhibitor of HMG-CoA reductase: Human UDP-glucuronosyltransferase enzymes involved in lactonizationXenobiotica33(1)27-41(2003) 2.Aoki, T., Nishimura, H., Nakagawa, S., et al.Pharmacological profile of a novel synthetic inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A reductaseArzneimittelforschung47(8)904-909(1997)