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Gentest^®
Enzyme Inhibition Services

Cytochrome P450 & UGT and oxidase & esterase inhibition studies
to predict drug-drug interaction.

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.

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)

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 K_i and/or K_I&k_inact determinations as needed
P450 inhibition testing is also available in human hepatocyte suspension

Qualified Incubation Conditions

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

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

Gentest® Enzyme Inhibition Services

Gentest® ADME Research Services' enzyme inhibition assays are valuable predictors of your drug candidate’s drug-drug interaction potential.

Testing for Comprehensive Metabolizing Enzymes

Reversible and Time-Dependent Inhibition Testing for Cytochrome P450s

Qualified Incubation Conditions

Robust IND-Enabling Studies

Featured Publications​

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May 2024

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Gentest^®
Enzyme Inhibition Services

Gentest^® ADME Research Services' enzyme inhibition assays are valuable predictors of your drug candidate’s drug-drug interaction potential.

Featured Publications

Development and Clinical
Trial Solutions

Development and Clinical
Trial Solutions