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Single dose pharmacokinetics, pharmacodynamics, tolerability and safety of BAY 60-5521, a potent inhibitor of cholesteryl ester transfer protein.BAY 60-5521，一种强效胆固醇酯转移蛋白抑制剂的单次剂量药代动力学、药效学、耐受性和安全性。
Br J Clin Pharmacol. 2012 Feb;73(2):210-8. doi: 10.1111/j.1365-2125.2011.04083.x.
2
Cholesteryl ester transfer protein and its inhibition.胆固醇酯转移蛋白及其抑制作用。
Cell Mol Life Sci. 2010 Sep;67(18):3139-49. doi: 10.1007/s00018-010-0418-3. Epub 2010 Jun 18.
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Mechanism-based prediction of particle size-dependent dissolution and absorption: cilostazol pharmacokinetics in dogs.基于机制的粒径依赖性溶解和吸收预测：西洛他唑在犬体内的药代动力学。
Eur J Pharm Biopharm. 2010 Sep;76(1):83-94. doi: 10.1016/j.ejpb.2010.06.003. Epub 2010 Jun 8.
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Safety and tolerability of dalcetrapib (RO4607381/JTT-705): results from a 48-week trial.达塞曲匹（RO4607381/JTT-705）的安全性和耐受性：一项为期 48 周的试验结果。
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Metabolism and excretion of anacetrapib, a novel inhibitor of the cholesteryl ester transfer protein, in humans.人对新型胆固醇酯转移蛋白抑制剂——阿昔单抗的代谢和排泄。
Drug Metab Dispos. 2010 Mar;38(3):474-83. doi: 10.1124/dmd.109.028704. Epub 2009 Dec 16.
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Physiologically-based PK/PD modelling of therapeutic macromolecules.治疗性大分子的基于生理的 PK/PD 建模。
Pharm Res. 2009 Dec;26(12):2543-50. doi: 10.1007/s11095-009-9990-3. Epub 2009 Oct 22.
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Whole-body physiologically based pharmacokinetic population modelling of oral drug administration: inter-individual variability of cimetidine absorption.口服给药的基于生理学的全身药代动力学群体建模：西咪替丁吸收的个体间变异性
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通过种属间比较的体表面积法和结合药效学及基于生理学的药代动力学模型预测强效胆固醇酯转移蛋白（CETP）抑制剂 BAY 60-5521 在人体中的潜在有效剂量。

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.

机构信息

Bayer HealthCare AG, Bayer HealthCare Pharmaceuticals Global Drug Discovery, Wuppertal, Germany.

出版信息

Br J Clin Pharmacol. 2012 Feb;73(2):219-31. doi: 10.1111/j.1365-2125.2011.04064.x.

DOI:10.1111/j.1365-2125.2011.04064.x
PMID:21762205
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3269581/
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.

摘要

目的

本研究旨在支持对 CETP 抑制剂 BAY 60-5521 进行人体潜在有效剂量的预测。

方法

采用基于生理的药代动力学（PBPK）模型，对 CETP 抑制剂 BAY 60-5521 的药代动力学进行种属间外推，并结合 CETP 转基因小鼠和人血浆的药效学研究，支持首次人体剂量的选择。

结果

PBPK 方法预测 BAY 60-5521 在人体内的分布范围大于种属间外推法，表现为更大的预测分布容积和更长的消除半衰期。联合方法得出 BAY 60-5521 在人体内潜在有效剂量的估计值为 51mg。

结论

本文描述的方法支持对 CETP 抑制剂 BAY 60-5521 进行人体潜在有效剂量的预测。在首次人体研究中证实了剂量估计值。