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Drug Discov Today Technol. 2004 Dec;1(4):365-72. doi: 10.1016/j.ddtec.2004.10.008.

Metabolic screening in vitro: metabolic stability, CYP inhibition and induction.

Author information

1
Department of Physical and Metabolic Science, AstraZeneca R&D Charnwood, Loughborough, Leics, UK LE11 5RH. Electronic address:rob.riley@astrazeneca.com.
2
Department of Physical and Metabolic Science, AstraZeneca R&D Charnwood, Loughborough, Leics, UK LE11 5RH.

Abstract

Automated, miniaturised assays are now commonplace within Discovery DMPK (drug metabolism and pharmacokinetics). These have evolved considerably since their inception around a decade ago, in-line with both technology and the desire to provide quality data comparable to more traditional analyses. Several formats exist for routine screening of metabolic stability and cyp (cytochrome P450; see Glossary) inhibition and induction, with the major focus being on in vitro systems using human-derived material. Data from other species remain valuable in assessing in vitro-in vivo projections and are pivotal to support safety assessment studies.

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