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Drug–Drug Interaction – Enzyme Inhibition

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Drug Discovery and Evaluation

1 Introduction

Inhibitory drug interactionsdrug–drug interaction received considerable attention in the 1990s because some prominent drugs (e.g. terfenadine) caused life-threatening adverse effects when prescribed with other commonly used drugs (e.g. antibiotics). At about the same time, in vitro technology was developed to study drug interaction with individual human P450 enzymes by using either enzyme specific substrates or recombinant P450 isoenzymes. Along with guidance documents issued by the US FDA and the European Agency for the Evaluation of Medicinal Products, the evaluation of in vitro drug interactions have become as an integral part of the drug development process (FDA 1997, EMEA 1997).

The following discussions and assay descriptions are related to cytochrome P450 inhibition. Most drug interaction studies are related to P450 isoenzymes. Nevertheless, other enzyme systems may contribute to significant drug interactions such as transporter (e.g. Floren 1997; Abel 2001)...

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Correspondence to Gert Ulrich Kürzel .

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© 2006 Springer-Verlag Berlin Heidelberg New York

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Dudda, A., Kürzel, G.U. (2006). Drug–Drug Interaction – Enzyme Inhibition. In: Vogel, H.G., Hock, F.J., Maas, J., Mayer, D. (eds) Drug Discovery and Evaluation. Springer, Berlin, Heidelberg. https://doi.org/10.1007/3-540-29804-5_28

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