Structure and Function of PXR and CAR

Zhou, Xuemei; Xu, Hongxia

doi:10.1002/9780470409107.ch5

Nuclear Receptors in Drug Metabolism 2008

DOI: 10.1002/9780470409107.ch5

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Structure and Function of PXR and CAR

Xuemei Zhou

Hongxia Xu

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2014

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Novel pre-clinical methodologies for pharmacokinetic drug–drug interaction studies: spotlight on “humanized” animal models

Jaiswal

Sharma

Shukla

et al. 2014

Drug Metabolism Reviews

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Poly-therapy is common due to co-occurrence of several ailments in patients, leading to the elevated possibility of drug-drug interactions (DDI). Pharmacokinetic DDI often accounts for severe adverse drug reactions in patients resulting in withdrawal of drug from the market. Hence, the prediction of DDI is necessary at pre-clinical stage of drug development. Several human tissue and cell line-based in vitro systems are routinely used for screening metabolic and transporter pathways of investigational drugs and for predicting their clinical DDI potentials. However, ample constraints are associated with the in vitro systems and sometimes in vitro-in vivo extrapolation (IVIVE) fail to assess the risk of DDI in clinic. In vitro-in vivo correlation model in animals combined with human in vitro studies may be helpful in better prediction of clinical outcome. Native animal models vary remarkably from humans in drug metabolizing enzymes and transporters, hence, the interpretation of results from animal DDI studies is difficult. With the advent of modern molecular biology and engineering tools, novel pre-clinical animal models, namely, knockout rat/mouse, transgenic rat/mouse with humanized drug metabolizing enzymes and/or transporters and chimeric rat/mouse with humanized liver are developed. These models nearly simulate human-like drug metabolism and help to validate the in vivo relevance of the in vitro human DDI data. This review briefly discusses the application of such novel pre-clinical models for screening various type of DDI along with their advantages and limitations.

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Novel pre-clinical methodologies for pharmacokinetic drug–drug interaction studies: spotlight on “humanized” animal models

Jaiswal

Sharma

Shukla

et al. 2014

Drug Metabolism Reviews

View full text Add to dashboard Cite

show abstract

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Structure and Function of PXR and CAR

Cited by 1 publication

References 33 publications

Novel pre-clinical methodologies for pharmacokinetic drug–drug interaction studies: spotlight on “humanized” animal models

Novel pre-clinical methodologies for pharmacokinetic drug–drug interaction studies: spotlight on “humanized” animal models

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