The class
Modeling predicts an effective human dose for the CETP inhibitor BAY 60-5521, later confirmed in a first-in-man study (Br J Clin Pharmacol 2012)
Original title: Prediction of a potentially effective dose in humans for BAY 60-5521, a potent inhibitor of cholesteryl ester transfer protein (CETP) by allometric species scaling and combined pharmacodynamic and physiologically-based pharmacokinetic modelling
To support first-in-man dose selection for the CETP inhibitor BAY 60-5521, researchers combined allometric species scaling of its pharmacokinetics with pharmacodynamic data from CETP-transgenic mice and human plasma, alongside physiologically based pharmacokinetic (PBPK) modelling. The PBPK approach predicted a greater extent of distribution in humans than the allometric scaling method, reflected in a larger predicted volume of distribution and longer elimination half-life. Combining both approaches yielded an estimated potentially effective human dose of 51 mg, an estimate that was subsequently confirmed in a first-in-man study.
Original abstract
Aims: The purpose of this work was to support the prediction of a potentially effective dose for the CETP-inhibitor, BAY 60-5521, in humans.
Methods: A combination of allometric scaling of the pharmacokinetics of the CETP-inhibitor BAY 60-5521 with pharmacodynamic studies in CETP-transgenic mice and in human plasma with physiologically-based pharmacokinetic (PBPK) modelling was used to support the selection of the first-in-man dose.
Results: The PBPK approach predicts a greater extent of distribution for BAY 60-5521 in humans compared with the allometric scaling method as reflected by a larger predicted volume of distribution and longer elimination half-life. The combined approach led to an estimate of a potentially effective dose for BAY 60-5521 of 51 mg in humans.
Conclusion: The approach described in this paper supported the prediction of a potentially effective dose for the CETP-inhibitor BAY 60-5521 in humans. Confirmation of the dose estimate was obtained in a first-in-man study.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.