• Chemistry, Medicine
  • Published in
    CPT: pharmacometrics…
    2015
  • DOI:10.1002/psp4.27

Analysis of “On/Off” Kinetics of a CETP Inhibitor Using a Mechanistic Model of Lipoprotein Metabolism and Kinetics

@inproceedings{Lu2015AnalysisO,
  title={Analysis of “On/Off” Kinetics of a CETP Inhibitor Using a Mechanistic Model of Lipoprotein Metabolism and Kinetics},
  author={James Lu and Yumi Cleary and Cyrille Maugeais and CI Kiu Weber and NA Mazer},
  booktitle={CPT: pharmacometrics & systems pharmacology},
  year={2015}
}
RG7232 is a potent inhibitor of cholesteryl-ester transfer protein (CETP). Daily oral administration of RG7232 produces a dose- and time-dependent increase in high-density lipoprotein-cholesterol (HDL-C) and apolipoproteinA-I (ApoA-I) levels and a corresponding decrease in low-density lipoprotein-cholesterol (LDL-C) and apolipoproteinB (ApoB) levels. Due to its short plasma half-life (∼3 hours), RG7232 transiently inhibits CETP activity during each dosing interval ("on/off" kinetics), as… CONTINUE READING

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