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Cyprotex Extends Time Dependent Inhibition Service to Include IC50 Shift and Kinact/KI Determination

Cyprotex announces that it has extended its time dependent CYP450 inhibition offering to include IC50 shift and kinact/KI determination assays. These assays complement its existing single-point time dependent inhibition assay.

Inhibition of CYP450 is one of the main causes of drug-drug interactions. The type of inhibition can be either a reversible or irreversible interaction. The time dependent inhibition assay identifies compounds which have the potential to form an irreversible interaction. These types of interactions are more serious than reversible interactions because the inactivated enzyme must be re-synthesised for activity to be restored.

The time dependent IC50 shift assay should be performed during drug discovery. It simultaneously detects reversible and time dependent inhibitors, it predicts drug-drug interactions, and it sets the range of optimal concentrations for more detailed kinact/KI studies. kinact/KI studies are performed later in drug development to elucidate the kinetics of inactivation, predict in vivo drug interactions, and to plan clinical drug interaction studies.

To learn more about Time Dependent Inhibition, click here.

A PhRMA perspective review by Grimm et al., in 2009 (Drug Metab Dispos 37(7); 1355-1370) highlights the approaches taken by the pharmaceutical industry in conducting these studies. The services provided by Cyprotex cover the recommended methods summarised in this paper.

Dr. Katya Tsaioun, Cyprotex’s Chief Scientific Officer, comments on the launch of this new service. ‘The interest in time dependent inhibition has grown dramatically over the past 5 years due to the serious clinical implications that have been identified due to irreversible inhibition of cytochrome P450 enzymes. Cyprotex is pleased to now offer a comprehensive range of time dependent CYP450 inhibition assays to support faster and more cost-efficient drug discovery.’

For further information:

Cyprotex PLC
Helen Gill PhD, Product Development Manager
Tel: +44 1625 505 100

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