Check Out Discovery's 2024 Year-End Sales Event NEW Tumoroid Cell Lines are Now Available NEW Lunaphore COMET Hyperplex IF Services Innovative Metabolic Co-Culture Hematotoxicity CFC Assay Services
Check Out Discovery's 2024 Year-End Sales Event NEW Tumoroid Cell Lines are Now Available NEW Lunaphore COMET Hyperplex IF Services Innovative Metabolic Co-Culture Hematotoxicity CFC Assay Services
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Gentest®
Enzyme Inhibition Services

Cytochrome P450 & UGT and oxidase & esterase inhibition studies
to predict drug-drug interaction.
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Gentest® ADME Research Services' enzyme inhibition assays are valuable predictors of your drug candidate’s drug-drug interaction potential.

Gentest® has been providing expert, regulatory submission-quality ADME services for more than two decades and offers a range of metabolic enzyme studies beyond the standard seven CYPs. Experienced study directors and the use of Gentest® products, including pooled human liver microsomes (Ultrapool™ HLM150) and cDNA expressed individual enzymes (Supersomes® ) ensure you receive robust, IND submission-ready results.
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Testing for Comprehensive Metabolizing Enzymes

  • Major Cytochrome P450s (CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4)
  • Additional Cytochrome P450 isoforms (CYP2A6, 2E1, 4A11, 4F2, 4F3B, and 4F12)
  • UDP-glucuronosyltransferases (UGT1A1, 1A3, 1A4, 1A6, 1A7, 1A8, 1A9, 2B7, 2B10, 2B15, and 2B17)
  • Non-P450 oxidases (AO and MAO)
  • Carboxylesterases (CES1b, 1c, and 2) and Cholinesterases (AChE and BChE)
  • Validated LC-MS/MS analysis for most enzymes (HPLC for CYP4A11 and spectrophotometry for ChE)
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Reversible and Time-Dependent Inhibition Testing for Cytochrome P450s

  • IC50 assay (reversible inhibition)
  • IC50 shift assay (time-dependent inhibition) comparing inhibition following a 30-min pre-incubation (+) and (-) NADPH
  • Follow-up Ki and/or KI&kinact determinations as needed
  • P450 inhibition testing is also available in human hepatocyte suspension
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Qualified Incubation Conditions

  • Enzyme concentration and incubation time within the linear range of metabolite formation
  • Low degree of substrate depletion
  • Substrate concentration near the Km
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Robust IND-Enabling Studies

  • Expert study directors who deliver assays aligned with FDA and EMA recommendations
  • High quality submission-ready data analysis and reports
  • Typical IC50 study design uses triplicate incubations with 7 non-zero concentrations of the test article and positive control inhibitor
  • Microsomal binding assessment available using equilibrium dialysis (RED device)
  • Custom inhibition assay development and validation are available
SPEAK WITH A DISCOVERY EXPERT

Featured Publications​

Validation of cytochrome P450 time-dependent inhibition assays: a two-time point IC50 shift approach
facilitates kinact assay design

Differential time- and NADPH-dependent inhibition of CYP2C19 by enantiomers of fluoxetine

Highly selective inhibition of human CYP3Aa in vitro by azamulin and evidence that inhibition is irreversible

Predictive In Vitro-In Vivo Extrapolation for Time Dependent Inhibition of CYP1A2, CYP2C8, CYP2C9, CYP2C19, and CYP2D6 Using Pooled Human Hepatocytes, Human Liver Microsomes, and a Simple Mechanistic Static Model

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