Interspecies Scaling and Prediction of Human Clearance: Comparison of Small- and Macro-molecule Drugs

Overview

Journal Xenobiotica

Publisher Informa Healthcare

Specialties Biochemistry
Toxicology

Date 2011 Sep 7

PMID 21892879

Citations 39

Authors

Yeamin Huh

David E Smith

Meihau Rose Feng

Affiliations

Soon will be listed here.

Abstract

Human clearance prediction for small- and macro-molecule drugs was evaluated and compared using various scaling methods and statistical analysis. Human clearance is generally well predicted using single or multiple species simple allometry for macro- and small-molecule drugs excreted renally. The prediction error is higher for hepatically eliminated small-molecules using single or multiple species simple allometry scaling, and it appears that the prediction error is mainly associated with drugs with low hepatic extraction ratio (Eh). The error in human clearance prediction for hepatically eliminated small-molecules was reduced using scaling methods with a correction of maximum life span (MLP) or brain weight (BRW). Human clearance of both small- and macro-molecule drugs is well predicted using the monkey liver blood flow method. Predictions using liver blood flow from other species did not work as well, especially for the small-molecule drugs.

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