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Drug Discov Today. 2005 Nov 1;10(21):1421-33.

Keynote review: in vitro safety pharmacology profiling: an essential tool for successful drug development.

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PreClinical Profiling, Lead Discovery Center, Novartis Institutes for BioMedical Research, Cambridge, MA 02139, USA.


Broad-scale in vitro pharmacology profiling of new chemical entities during early phases of drug discovery has recently become an essential tool to predict clinical adverse effects. Modern, relatively inexpensive assay technologies and rapidly expanding knowledge about G-protein coupled receptors, nuclear receptors, ion channels and enzymes have made it possible to implement a large number of assays addressing possible clinical liabilities. Together with other in vitro assays focusing on toxicology and bioavailability, they provide a powerful tool to aid drug development. In this article, we review the development of this tool for drug discovery, its appropriate use and predictive value.

[Indexed for MEDLINE]

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