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Enzyme Induction

Enzyme Induction studies predict a compound’s likelihood to increase clearance of a concomitant (victim) drug by up-regulating (inducing) enzymes that metabolize it. To learn more about this service, visit our Enzyme Induction contract service page.

 

Webinars

2C or Not 2C: CYP2C Induction Studies for Successful Preclinical Risk Assessment

As a part of IND-enabling preclinical drug development studies companies are required to meet regulatory expectations to evaluate the induction potential of their compound for the cytochrome P450 CYP enzymes CYP1A2, 2B6, 2C8, 2C19 and 3A4.  While only CYP1A2, 2B6 and 3A4 must be assessed in the initial induction panel, any observed induction of CYP3A4 requires further investigation of induction potential for enzymes in the CYP2C family due to crosstalk between the PXR and CAR nuclear receptor pathways.  This webinar will focus on CYP2C induction and will emphasize when to include CYP2C induction in a study, how to design the study to generate meaningful data and meet the regulatory requirements, what endpoints to measure, and how to interpret results.
Webinars

ADME 101: Model-Based Approaches to DDI Risk Prediction – Navigating the Transition from In Vitro Data to In Silico Modeling

This informative ADME 101 discusses In Vitro to In Vivo Extrapolation (IVIVE) and how a model-based approach following routine perpetrator potential studies (i.e. CYP inhibition, CYP induction, and transporter inhibition) assessing clinical potential may eliminate the need of conducting clinical studies. Listen in as Dr. Limaye outlines a step–wise approach for bringing robustness to the prediction, including...
Webinars

ADME 101: Enzyme Induction Studies

The clearance of a drug can be increased and its effectiveness or safety compromised if it is co-administered with a second drug that induces the enzyme responsible...
Blog

ADME and Drug-Drug Interactions for the Toxicologist

Highlights from the recent webinar presented by our newest expert consultant, Dr. Pallavi Limaye In her recent webinar (now available for...

Webinars

Comparison Between the Final US FDA, Japan PMDA, and EMA In Vitro DDI Guidance Documents: Are We Finally Harmonized?

Presenter: Brian Ogilvie, Ph.D., SEKISUI XenoTech Vice President of Scientific Consulting In January, the FDA published its final guidance for industry on in vitro drug-drug interaction (DDI) studies. Dr. Ogilvie...
Webinars

The Basics of In Vitro Xenobiotic Metabolism and Drug-Drug Interaction Investigations: Applicability to All Xenobiotics

Since SOT’s 59th Annual Meeting and ToxExpo has been canceled due to COVID-19 concerns, we are bringing the tradeshow to you! SOT is hosting this...
Blog

In Vitro Evaluation of Drug-Drug Interaction (DDI) Potential

In its most recent in vitro drug interaction guidance update, the US Food and Drug Administration (FDA) emphasized harmony with the...

Blog

Four ways to optimize preclinical in vitro data to mitigate risk of late-stage clinical failure

1. Collect high-quality data to make informed, confident go/no go decisions for moving your drug candidate forward If you need...

Blog

Timing of In Vitro Studies: Early, Thorough ADME for Your Compound’s Success

Beyond the need for evidence that a drug works, Food and Drug Administration (FDA) and other regulatory bodies around the...

Scientific Posters

The evaluation of induction and inhibition potency of various drugs on CYP3A4 and OATP1B1/1B3

Presented at the 34th JSSX Annual Meeting in Tsukuba, Japan Authors Ryota Takeuchi, Rena Kusano, Tomoko Sasai, Takami Sarashina, Ryo Fujino, Kenta Hashizume  Drug Development...
Blog

What In Vitro Metabolism and DDI Studies Do I Actually Need?

Though there is no ‘roadmap’ spelling out required studies to achieve regulatory approval for clinical entry, a drug candidate’s metabolism...

Blog

Can CYP3A4 Induction Predict P-glycoprotein Induction in DDI Studies?

Generally, a drug’s effects on enzyme and transporter activity are examined independently in a drug development program, but what if...

Blog

In Vitro Induction Studies: Elements of Design and Important Considerations in Data Analysis

Why do induction studies? Induction potential is an important piece of the drug-drug interaction (DDI) component of an IND submission. Simply put, we...

Webinars

In Vitro Induction Studies: Elements of Design and Important Considerations in Data Analysis

Presenter: Joanna Barbara, Ph.D., Vice President of Scientific Operations at SEKISUI XenoTech Synopsis: When evaluating drug-drug interaction (DDI) risk of an investigational drug, a battery of...
Webinars

In Vitro Evaluation of Immunomodulating Drugs as Perpetrators of Drug Interactions

Presenter: Dr. Maciej Czerwinski, SEKISUI XenoTech Director of Consulting Synopsis: On October 15th, 2018, SEKISUI XenoTech presented on “In Vitro Direct and Cytokine-Mediated Effects of Therapeutic Peptides...
Blog

IQ Induction Working Group Publishes Recommendations for Data Interpretation of In Vitro Induction – Focus on CYP3A4 mRNA

SEKISUI XenoTech is proud to have made contributions to the paper entitled, “Considerations from the IQ Induction Working Group in...

Publications

DDI Guidance Recommendations on Down-Regulation, CYP2C Induction and CYP2B6 Control

Considerations from the IQ Induction Working Group in Response to Drug-Drug Interaction Guidances from Regulatory Agencies: Focus on Down-regulation, CYP2C Induction and CYP2B6 Positive Control...
Blog

UGT Activities, Concomitant Drugs, and DDI

If you have concerns about how your compound may affect UDP-glucuronosyltransferase (UGT) induction and/or inhibition when combined with other therapeutic...

Scientific Posters

The Impact of Various Solvents and Solvent Concentrations on In Vitro Enzyme Induction Assessment

Induction of cytochrome P450 (CYP) enzymes is one of the principal mechanisms of drug-drug interactions inasmuch as regulators recommend that new drug candidates be evaluated for...
Scientific Posters

Rapid mRNA Induction Screen

Full Title A Rapid High Content Cytochrome P450 (CYP) mRNA Induction Screen for Early Drug Development Abstract Cytochrome P450 (CYP) enzymes play an important role...
Scientific Posters

The Impact of Incomplete Dose-Response Curves on EC50 and Emax Determinations in Enzyme Induction

The Impact of Incomplete Dose-Response Curves on EC50 and Emax Determinations in Enzyme Induction Assessment In evaluating the enzyme induction potential of a new drug...
Scientific Posters

Induction of UDP-Glucuronosyltransferases in Cultures of Fresh and Immortalized Human Hepatocytes

We have examined the induction of UDP-glucuronosyltransferases (UGTs) in primary cultures of Human hepatocytes and in immortalized Human hepatocytes (Fa2N-4 cells) under conditions that result...
Publications

2012 XenoTech Products & Services Catalog

The 2012 Products & Services Catalog was developed to provide an overview of our entire portfolio of capabilities, with a heavy emphasis on the services...
Scientific Posters

Time-course of Cytochrome P450 (CYP450) induction in cultured human hepatocytes

Full Title Time-course of Cytochrome P450 (CYP450) induction in cultured Human hepatocytes: Evaluation of activity and mRNA expression profiles for six inducible CYP450 enzymes Abstract...
Scientific Posters

In vitro inhibition and induction of human liver cytochrome P450 enzymes by NTBC and its metabolism in human liver microsomes

In vitro inhibition and induction ofHuman liver cytochrome P450 enzymes by NTBC and its metabolism in human liver microsomes 2-(2-Nitro-4-trifluoromethylbenzoyl)-1, 3-cyclohexanedione (NTBC, also known as...
Scientific Posters

In situ evaluation of CYP1A2, CYP2B6 and CYP3A4/5 induction in cultured human hepatocytes with a cocktail of probe substrates: A comparison of percent positive control values

It has previously been demonstrated that a cocktail of probe substrates can be effectively used to screen simultaneously for induction of CYP1A2, CYP2B6 and CYP3A4/5...
Scientific Posters

Induction of Liver and Intestinal Cytochrome P450 (CYP) Enzymes in Male and Female Cynomolgus Monkey

The objective of the present study was to determine the effects of various prototypical inducers on the activity and mRNA expression of multiple CYP enzymes...
Scientific Posters

Cytochrome P450 3A4 and 1A2 Induction in Immortalized and Primary Cultures of Human Hepatocytes

Full Title Cytochrome P450 3A4 and 1A2 Induction in the Immortalized Hepatocyte Line, Fa2N-4, and Comparison with Primary Cultures of Human Hepatocytes Abstract Primary cultures...
Scientific Posters

The Use of Immortalized Hepatocytes in Induction Studies

Abstract Primary cultures of human hepatocytes are widely used to evaluate the cytochrome P450 (CYP) enzyme-inducing potential and/or toxicity of drug candidates. However, the availability...

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