Applications of Human Pharmacokinetic Prediction in First-in-Human Dose Estimation

被引：0
作者：
Peng Zou
Yanke Yu
Nan Zheng
Yongsheng Yang
Hayley J. Paholak
Lawrence X. Yu
Duxin Sun
机构：
[1] University of Michigan,Department of Pharmaceutical Sciences, College of Pharmacy
[2] Food and Drug Administration,Office of Testing and Research, Center for Drug Evaluation and Research
[3] Food and Drug Administration,Office of Generic Drugs, Center for Drug Evaluation and Research
来源：
The AAPS Journal | 2012年 / 14卷
关键词：
allometric scaling; FIH dose; correlations; pharmacokinetics; prediction;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
Quantitative estimations of first-in-human (FIH) doses are critical for phase I clinical trials in drug development. Human pharmacokinetic (PK) prediction methods have been developed to project the human clearance (CL) and bioavailability with reasonable accuracy, which facilitates estimation of a safe yet efficacious FIH dose. However, the FIH dose estimation is still very challenging and complex. The aim of this article is to review the common approaches for FIH dose estimation with an emphasis on PK-guided estimation. We discuss 5 methods for FIH dose estimation, 17 approaches for the prediction of human CL, 6 methods for the prediction of bioavailability, and 3 tools for the prediction of PK profiles. This review may serve as a practical protocol for PK- or pharmacokinetic/pharmacodynamic-guided estimation of the FIH dose.
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页码：262 / 281
页数：19
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