Plasma Stability-Dependent Circulation of Acyl Glucuronide Metabolites in Humans: How Circulating Metabolite Profiles of Muraglitazar and Peliglitazar Can Lead to Misleading Risk Assessment

@article{Zhang2011PlasmaSC,
  title={Plasma Stability-Dependent Circulation of Acyl Glucuronide Metabolites in Humans: How Circulating Metabolite Profiles of Muraglitazar and Peliglitazar Can Lead to Misleading Risk Assessment},
  author={Donglu Zhang and Nirmala Raghavan and Lifei Wang and Yongjun Xue and Mary T. Obermeier and Stephanie Y. Chen and Shiwei Tao and Hao Zhang and Peter T. W. Cheng and Wenying Li and Ragu Ramanathan and Zheng Yang and W Griffith Humphreys},
  journal={Drug Metabolism and Disposition},
  year={2011},
  volume={39},
  pages={123 - 131}
}
Muraglitazar and peliglitazar, two structural analogs differing by a methyl group, are dual peroxisome proliferator-activated receptor-α/γ activators. Both compounds were extensively metabolized in humans through acyl glucuronidation to form 1-O-β-acyl glucuronide (AG) metabolites as the major drug-related components in bile, representing at least 15 to 16% of the dose after oral administration. Peliglitazar AG was the major circulating metabolite, whereas muraglitazar AG was a very minor… 

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