The lactone form of rosuvastatin
Rosuvastatin lactone is the lactone form of the HMG-CoA reductase inhibitor rosuvastatin .1 It is found in vivo following rosuvastatin administration.2 Rosuvastatin lactone is an inhibitor of the cytochrome P450 (CYP) isoforms CYP2C9.1 and CYP2C9.3 (IC50s = 8.52 and 4.1 µM, respectively).1
1.Shiozawa, A., Yamaori, S., Kamijo, S., et al.Effects of acid and lactone forms of statins on S-warfarin 7-hydroxylation catalyzed by human liver microsomes and recombinant CYP2C9 variants (CYP2C9.1 and CYP2C9.3)Drug Metab. Pharmacokinet.36100364(2021) 2.Martin, P.D., Warwick, M.J., Dane, A.L., et al.Metabolism, excretion, and pharmacokinetics of rosuvastatin in healthy adult male volunteersClin. Ther.25(11)2822-2835(2003)
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