Modeling of PET Data in CNS Drug Discovery and Development

Overview

Journal J Pharmacokinet Pharmacodyn

Publisher Springer

Specialty Pharmacology

Date 2013 May 11

PMID 23660778

Citations 14

Authors

Katarina Varnas

Andrea Varrone

Lars Farde

Affiliations

Soon will be listed here.

Abstract

Positron emission tomography (PET) is increasingly used in drug discovery and development for evaluation of CNS drug disposition and for studies of disease biomarkers to monitor drug effects on brain pathology. The quantitative analysis of PET data is based on kinetic modeling of radioactivity concentrations in plasma and brain tissue compartments. A number of quantitative methods of analysis have been developed that allow the determination of parameters describing drug pharmacokinetics and interaction with target binding sites in the brain. The optimal method of quantification depends on the properties of the radiolabeled drug or radioligand and the binding site studied. We here review the most frequently used methods for quantification of PET data in relation to CNS drug discovery and development. The utility of PET kinetic modeling in the development of novel CNS drugs is illustrated by examples from studies of the brain kinetic properties of radiolabeled drug molecules.

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