Enzyme Inhibition

To assess the potential of drug candidates to inhibit (i.e. down-regulate) the expression of drug-metabolizing enzymes
 

Enzyme Inhibition & DDI Studies

Evaluate CYP450 and UGT Inhibition to Predict Drug–Drug Interaction Risk

Enzyme inhibition studies are critical for predicting pharmacokinetics because inhibition of these enzymes may result in decreased clearance of the drug or another metabolized compound.

As part of our comprehensive portfolio of ADME-Tox research services we provide the following enzyme inhibition studies. Our study designs comply with current regulatory guidance for enzyme inhibition studies.

CYP450 Inhibition

CYP450 inhibition studies predict if exposure to a test article will result in decreased synthesis and concentration of CYP450 enzymes.

CYP450 Inhibition

CYP450 inhibition studies predict if exposure to a test article will result in decreased synthesis and concentration of CYP450 enzymes.

Fluorescence CYP-Inhibition

We offer fluorescent based cyp-inhibition screening services to determine CYP inhibition potential of novel compounds, using BACTOSOMES™ as the enzyme source.

UGT Inhibition

We offer definitive In vitro UDP-glucuronosyltransferase (UGT) Inhibition Studies to predict if drug candidates inhibit cytochrome P450 enzymes.

Automation and Analysis

Enzyme inhibition studies are implemented in our state-of-the-art laboratory where we offer:

  • Tecan liquid handling automation systems

  • LC-MS/MS analysis

  • High throughput autosamplers

  • Deuterated metabolites used as internal standards (all CYPs and most UGTs)

  • Automated data retrieval and processing

  • Comprehensive reports