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

被引：95

作者：

Zou, Peng ^{[3
]}

Yu, Yanke ^{[3
]}

Zheng, Nan ^{[3
]}

Yang, Yongsheng ^{[2
]}

Paholak, Hayley J. ^{[3
]}

Yu, Lawrence X. ^{[1
]}

Sun, Duxin ^{[3
]}

机构：

[1] US FDA, Ctr Drug Evaluat & Res, Off Gener Drugs, Rockville, MD 20857 USA

[2] US FDA, Ctr Drug Evaluat & Res, Off Testing & Res, Silver Spring, MD 20993 USA

[3] Univ Michigan, Coll Pharm, Dept Pharmaceut Sci, Ann Arbor, MI 48109 USA

来源：

AAPS JOURNAL | 2012年 / 14卷 / 02期

基金：

美国国家卫生研究院;

关键词：

allometric scaling; FIH dose; in vitro-in vivo correlations; pharmacokinetics; prediction; HUMAN DRUG CLEARANCE; HEPATIC METABOLIC-CLEARANCE; IN-VITRO DATA; CRYOPRESERVED HUMAN HEPATOCYTES; HUMAN LIVER-MICROSOMES; HUMAN ORAL BIOAVAILABILITY; MEMBRANE PERMEATION ASSAY; INTRINSIC CLEARANCE; PHASE-I; VERTICAL ALLOMETRY;

D O I：

10.1208/s12248-012-9332-y

中图分类号：

R9 [药学];

学科分类号：

1007 ;

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.

引用

页码：262 / 281

页数：20

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