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Current Drug Metabolism

Editor-in-Chief

ISSN (Print): 1389-2002
ISSN (Online): 1875-5453

Applications of LC-MS in PET Radioligand Development and Metabolic Elucidation

Author(s): Ying Ma, Dale O. Kiesewetter, Lixin Lang, Dongyu Gu and Xiaoyuan Chen

Volume 11, Issue 6, 2010

Page: [483 - 493] Pages: 11

DOI: 10.2174/138920010791636167

Price: $65

Abstract

Positron emission tomography (PET) is a very sensitive molecular imaging technique that when employed with an appropriate radioligand has the ability to quantititate physiological processes in a non-invasive manner. Since the imaging technique detects all radioactive emissions in the field of view, the presence and biological activity of radiolabeled metabolites must be determined for each radioligand in order to validate the utility of the radiotracer for measuring the desired physiological process. Thus, the identification of metabolic profiles of radiolabeled compounds is an important aspect of design, development, and validation of new radiopharmaceuticals and their applications in drug development and molecular imaging. Metabolite identification for different chemical classes of radiopharmaceuticals allows rational design to minimize the formation and accumulation of metabolites in the target tissue, either through enhanced excretion or minimized metabolism. This review will discuss methods for identifying and quantitating metabolites during the pre-clinical development of radiopharmaceuticals with special emphasis on the application of LC/MS.

Keywords: Positron emission tomography (PET), Radiopharmaceutical, LC/MS/MS, Metabolite

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