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Drug Drug Interactions (DDI)

Drug-drug interactions (DDI) can be fatal or harmful to a patient taking multiple medications by causing up-regulation or inhibition of drug-metabolizing enzymes or altering activity of drug transporters. Understanding DDI potential of an investigational new drug before clinical trials can help bolster safety data and evaluate risk. To learn more about why DDI potential of a compound is important or to contract relevant studies, visit our Drug-Drug Interactions (DDI) informational page.

 

Webinars

Design Intricacies and Decision-Making Strategy for Drug-Drug Interaction Studies

Presenter: Andrew G. Taylor, Ph.D., Manager of Technical Support for Services at XenoTech Conducting in vitro ADME drug-drug interaction (DDI) studies early on in the drug...
Scientific Posters

Establishment of PALSAR method for quantification of human cells in mouse kidney

Full Title Establishment of PALSAR method for quantification of human cells in mouse kidney Authors Tetsuo Sekino, Akane Omori and AkiraIdeno Analytical Technology Center for...
Blog

Are in vitro drug metabolism and drug-drug interaction studies critical for an IND?

A Guide to What, Why & When to Conduct ADME Studies When drug developers are preparing their IND, drug metabolism...

Webinars

Highlights of the In Vitro Sections of the Draft ICH Drug Interaction Studies Guideline and Comparison with Current Guidance

Presenter: Brian Ogilvie, Ph.D, Vice President of Scientific Consulting at XenoTech In June 2022, the ICH released the first draft of its harmonized Drug Interaction Studies Guideline (M12). The...
Scientific Posters

Highly selective and sensitive hybridization-based assay for quantification of ASOs drug using signal amplification method

Full Title Highly selective and sensitive hybridization-based assay for quantification of ASOs drug using signal amplification method Authors Yuya Ono1, Tetsuo Sekino1, Takuro Akiya1, Funa...
Scientific Posters

A Novel ADA Screening Assay for Immunogenicity Testing of Oligonucleotide Drug Using PALSAR Technology

Full Title A Novel ADA Screening Assay for Immunogenicity Testing of Oligonucleotide Drug Using PALSAR® Technology Authors Masako Osawa, Funa Ogawa, Koichi Shibusawa and Akira...
Blog

4 Ways De-Risking Maximizes Compound Value

Since most new drugs fail because of ADME/Tox, you can add considerable value to your compound by conducting early in...

Scientific Posters

Investigation of the PPB method for oligonucleotide drugs by using the PALSAR

Full Title Investigation of the PPB method for oligonucleotide drugs by using the PALSAR® Authors Rieko Sakai1, Takashi Yamamoto1, Masako Osawa2, Funa Ogawa2, Shun Kumagaya3,...
Blog

New FDA Draft Guidance “Clinical Pharmacology Considerations for the Development of Oligonucleotide Therapeutics” – XenoTech’s perspective on in vitro DDI testing

The FDA has released a new draft guidance for industry titled “Clinical Pharmacology Considerations for the Development of Oligonucleotide Therapeutics.”...

Regulatory Documents

2022 FDA Draft Guidance for Industry “Clinical Pharmacology Considerations for the Development of Oligonucleotide Therapeutics”

“This guidance provides recommendations to assist industry in the development of oligonucleotide therapeutics under section 505 of the Federal Food, Drug, and Cosmetic Act (21...
Blog

Spotlight on Efflux and Uptake Drug Transporters in In Vitro Drug-Drug Interaction Studies

What are drug transporters? Drug transporters are membrane-bound proteins that assist in the movement of drugs into or out of...

Publications

In vitro evaluation suggests fenfluramine and norfenfluramine are unlikely to act as perpetrators of drug interactions

Parthena Martin, Maciej Czerwiński, Pallavi B. Limaye, Brian W. Ogilvie, Steven Smith, Brooks Boyd Abstract Studies support the safety and efficacy of fenfluramine (FFA) as...
Regulatory Documents

2022 ICH M12 Draft Guideline for Drug Interaction Studies

“In clinical practice, patients are often prescribed more than one drug which can result in a DDI (drug-drug interaction). Some patients, in particular fragile older...
Publications

In vitro evaluation of fenfluramine and norfenfluramine as victims of drug interactions

Parthena Martin, Maciej Czerwiński, Pallavi B. Limaye, Seema Muranjan, Brian W. Ogilvie, Steven Smith, Brooks Boyd Abstract Fenfluramine (FFA) has potent antiseizure activity in severe,...
Webinars

Filing an IND and Beyond: Development of CTD Section 2.6.4, Pharmacokinetics Written Summary

Presenter: Griff Humphreys, Ph.D, XenoTech Consultant Recorded keynote presentation from XenoTech’s 2022 Seminar Series. Learn about what this important section consists of, the studies that...
Webinars

Role of Sulfotransferases (SULTs) in Drug Metabolism and Potential for Drug-Drug Interactions

Presenter: Maciej Czerwinski, Ph.D., XenoTech Director of Scientific Consulting Abstract: Continuing our series on non-CYP-mediated metabolism pathways, we will be discussing another of the most requested...
Publications

A Guide to In Vitro CYP Inhibition Studies: Elements of Study Design and Important Considerations in Data Analysis

The USFDA, along with other regulatory agencies such as the EMA in Europe and PMDA in Japan, recommend evaluating investigational drugs for their potential to...
Blog

When, Why and How to Conduct CYP2C Induction Studies

Over the years, we have received a lot of questions about cytochrome P450 (CYP) 2C induction studies. In February of...

Webinars

ADME 101: Microsomal Protein Binding of Drugs

Presenter: Kusum Parikh, MBBS, PhD, XenoTech Senior Scientist in Program Oversight Abstract: Regulatory guidance states that drug developers should correct for nonspecific binding in microsomes...
Blog

Why Do Most Polled Researchers Run Red Blood Cell Partitioning Studies with Plasma Protein Binding?

Many compounds bind to or diffuse into red blood cells (RBCs), which can significantly impact clearance and cause inaccuracies in PK calculations...

Blog

Highlights from the 2021 Marbach Drug-Drug Interaction Workshop

Reflecting on the virtual conferences in 2021, I would like to look back at some of the highlights from the...

Blog

2021 Service Expansions: Microsomal Protein Binding and Red Blood Cell Partitioning

Over the course of 2021, we expanded access to two important and related study offerings at our US laboratory headquarters....

Webinars

Role of UDP-Glucuronosyltransferases (UGTs) in Drug Metabolism and Drug-Drug Interactions

Presenter: Maciej Czerwinski, Ph.D., XenoTech Director of Scientific Consulting Abstract: The importance of glucuronidation for metabolism of xenobiotics in humans is illustrated by the abundance and...
Scientific Posters

Establishment of the PPB method for antisense oligonucleotides (ASOs) by using the PALSAR method

Full Title Establishment of the PPB method for antisense oligonucleotides (ASOs) by using the PALSAR® method Authors Rieko Sakai1, Takashi Yamamoto1, Masako Osawa2, Funa Ogawa2,...
Blog

ADME/PK & DDI Best Practices Industry Survey Results & Infographic

With over 3500 respondents, only 4% of respondents said they had never experienced any repercussions from postponing these studies...

Publications

SAFETY FIRST: Assessing drugs early can preclude regulatory and health issues

Authors: Madison Esely-Kohlman, Dr. Maciej Czerwinski, Dr. Pallavi Limaye, Dr. Brian Ogilvie A Guide to When & Why to Evaluate ADME/PK & Drug-Drug Interactions With...
Blog

Four Ways CROs Drive Innovation for Improved In Vitro Drug Metabolism and Pharmacokinetics (DMPK) Studies

Agility and focused growth allow drug developers to outsource expertise and benefit the industry at-large by fostering innovation. Panelists at the 2021 Annual DMDG Meeting…

Webinars

Red Blood Cell Partitioning Studies to Improve Accuracy in Pharmacokinetics (PK) Calculations

Presenter: Steven McGreal, Ph.D, Study Director at XenoTech Abstract: Pharmacokinetic (PK) parameters of a new drug candidate are typically determined by measuring the drug’s concentration...
Blog

DDI & Drug Repurposing Article featured in Drug Discovery World (DDW) Spring Edition 2021

Repurposing (repositioning, re-profiling, or re-tasking) a drug potentially saves years of costly testing from going to waste and potentially providing a higher chance of success.…

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.
Blog

Interview with Outsourcing Pharma: Repurposing existing drugs accelerates discovery

“Exploring alternative uses for drugs tapped for other indications, can save considerable time and money in discovery, according to an...

Scientific Posters

Effects of Monocyte Chemoattractant Protein-1, Macrophage Inflammatory Protein-1α and Interferon-α2a on P450 Enzymes in Human Hepatocytes in Vitro

Some immunomodulatory drugs, such as tilsotolimod, stimulate the innate immune system to release cytokines that may change expression of drug-metabolizing enzymes. In drug development, regulation of multiple pro- and anti-inflammatory cytokines by Toll-like receptors (TLR) has gained attention in parallel to targeting the therapeutic potential of these receptors. The aim of this study was to establish whether MCP-1, MIP-1α or IFN-α2a were responsible for the effects of tilsotolimod-stimulated plasma on CYP1A2 and CYP2B6 mRNA and enzyme activity levels...
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

Suicide by Binding: Putting Time-Dependent Inhibition of CYP Enzymes into Perspective

Presenter: Brian Ogilvie, Ph.D., XenoTech Vice President of Scientific Consulting with special guest for Q&A, Lois Haupt, XenoTech Principal Scientist in Program Oversight Many drug candidates...
Regulatory Documents

2020 FDA Draft Guidance, “Drug-Drug Interaction Assessment for Therapeutic Proteins Guidance for Industry”

In August 2020, the FDA released the draft guidance for industry to evaluate therapeutic proteins for drug-drug interaction (DDI) potential using a risk-based approach. “The...
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

Drug-Drug Interaction (DDI) Prediction Models Following In Vitro Studies in Preclinical Development

In preclinical development, a drug will be evaluated for potential to cause a drug-drug interaction (DDI) using in vitro experiments and then calculations that...

Blog

Important DDI Considerations for Repurposing Drugs to Treat COVID-19

“Given the rapid spread of COVID-19 and its relatively high mortality, filling the gap for coronavirus-specific drugs is urgent. […]...

Blog

What is DMPK and how does it fit into drug development?

Drug metabolism and pharmacokinetics (DMPK) is a core discipline in drug development that considers the biotransformation of a drug compound...

Webinars

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

Presenter: Jennifer Horkman, Senior Scientist in Program Oversight at XenoTech When evaluating drug-drug interaction (DDI) risk of an investigational drug, a battery of studies is needed to investigate victim/perpetrator...
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., 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 will...
Webinars

In Vitro ADME & Drug-Drug Interaction Considerations for Toxicologists

In vitro ADME and drug-drug interaction (DDI) investigations are early activities in the drug development process that are critical for framing downstream decision making. This ADME 101 webinar will provide insights at a high-level related to regulatory drivers, investigatory objectives, and practical concerns for such studies that are relevant to interested general toxicologists. Participants will gain insight as to the critical need and utility for in vitro ADME and DDI investigations as related to drug development. Regulatory expectations will be reviewed as will points of particular interest for enabling successful achievement of investigatory goals...
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

COVID-19 Updates

As a global Life Sciences and Healthcare company, XenoTech recognizes the seriousness of the Coronavirus Pandemic. We are constantly monitoring...

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...

Scientific Posters

Comparison Between the Final US FDA, Japan PMDA and EMA In Vitro DDI Guidance

Comparison Between the Final US FDA (2020), the Final Japan PMDA (2018), and Final EMA (2013) In Vitro DDI Guidance Documents: Are We Finally Harmonized?...
Webinars

ADME 101: Metabolite ID & Characterization Studies FAQ

Presenter: Mark Horrigan, XenoTech Principal Scientist, Program Oversight In this short, information-packed ADME 101 video, one of our study directors discusses the main frequently asked questions...
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...

Publications

Effects of monocyte chemoattractant protein-1, macrophage inflammatory protein-1α, and interferon-α2a on P450 enzymes in human hepatocytes in vitro

Maciej Czerwiński, Krystal Gilligan, Kevin Westland, Brian W. Ogilvie Some immunomodulatory agents stimulate the release of cytokines capable of suppressing P450 enzymes and potentially affecting pharmacokinetics of coadministered medications. Cytokines...
Webinars

Drug Metabolism Related Safety Considerations in Drug Development

Approximately 30 years ago, sub-optimal DMPK properties were recognized as the primary contributor to the failure (~40%) of potential new therapies in early clinical trials. This observation precipitated a renaissance period across the discipline which served to align DMPK efforts within discovery to assist in selecting optimal drug candidates to advance to clinical testing...
Blog

How to Choose the Right Test Systems for Your DMPK Studies

Test systems for DMPK in vitro studies are part of the very foundation of our company. Our labs were borne of...

Blog

Transporters of Emerging Importance in Drug Development: Beyond the Guidance Documents

Dr. Ogilvie’s presentation discusses critical literature and case studies which have been published following the FDA’s 2017 guidance revision, and covered...

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...

Blog

Minding Your Binding: Plasma Protein Binding Potential Study Now Available at Our US Labs

While liver and intestine are important in ADME, behavior in blood is also crucial. When an orally administered drug or...

Webinars

In Vitro Evaluation of Immunomodulating Drugs as Perpetrators of Drug Interactions

Presenter: Dr. Maciej Czerwinski, XenoTech Director of Consulting; Synopsis: On October 15th, 2018, XenoTech presented on “In Vitro Direct and Cytokine-Mediated Effects of Therapeutic Peptides and other Biologics on CYP Enzymes” at the Peptide ADME Discussion Group Workshop...
Blog

Important Considerations for the Conduct of In Vitro Drug Transporter Assays

Not only can drug transporters affect the absorption and excretion of drugs, they can be involved in pharmacokinetic-based drug-drug interactions...

Publications

2017 FDA Guidance: Many In Vitro DDI Evaluations Should Precede FIH Studies

Dr. Brian Ogilvie, Andrea Wolff While the 2017 FDA DDI guidance contains many important changes, the earlier timing of drug-drug interaction studies is perhaps the most...
Publications

Chapter 6: Biotransformation of Xenobiotics

Andrew Parkinson, Brian W. Ogilvie, David B. Buckley, Faraz Kazmi and Oliver Parkinson This book chapter will be part of Casarett and Doull’s Toxicology: The...
Scientific Posters

Ultrasensitive quantitation assay of oligonucleotide therapeutics based on the PALSAR method

Full Title Ultrasensitive quantitation assay of oligonucleotide therapeutics based on the PALSAR method Abstract Recently, development of oligonucleotide therapeutics has accelerated in the pharmaceutical industry,...
Blog

To GLP or not to GLP?

That is the question. . . Knowing the answer may save you time and money Good Laboratory Practices (GLP) are...

Publications

Considerations from the IQ Induction Working Group in Response to Drug-Drug Interaction Guidances from Regulatory Agencies

Jane R Kenny, Diane Ramsden, David B Buckley, Shannon Dallas, Conrad Fung, Michael Mohutsky, Heidi J Einolf, Liangfu Chen, Joshua G Dekeyser, Maria Fitzgerald, Theunis...
Blog

In Vitro DDI Regulatory Guidance Reference Poster

At the 2018 Marbach Castle Drug-Drug Interaction Workshop in Germany, Dr. Brian Ogilvie, Vice President of Scientific Consulting, presented a comparison...

Publications

Direct and cytokine‐mediated effects of albumin‐fused growth hormone, TV‐1106, on CYP enzyme expression in human hepatocytes in vitro

Maciej Czerwiński, Immaculate Amunom, Victor Piryatinsky, Hussein Hallak, Yousif Sahly, Oren Bar‐Ilan, Paul Bolliger, Merav Bassan Some biologics can modulate cytokines that may lead to...
Blog

Further Research on the Drug-Drug Interaction Between Gemfibrozil and Repaglinide Presented

The clinically-relevant drug-drug interaction (DDI) between the dyslipidemia drug gemfibrozil and the antidiabetic repaglinide is well-documented throughout the literature. In...

Scientific Posters

Further exploration into the DDI between Gemfibrozil & Repaglinide in rats: Uptake Transporters

Full Title Further exploration into the DDI between Gemfibrozil & Repaglinide in rats: Uptake Transporters Authors Chase I. McCoy, Forrest A. Stanley, Chandra Kollu, Seema...
Blog

Considerations In Response to Drug-Drug Interaction Guidances

Check out the recent IQ consortium publication: Considerations from the IQ Induction Working Group in Response to Drug-Drug Interaction Guidances from...

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...
Webinars

Drug Metabolizing Enzymes and Transporters in NASH

“Drug Metabolizing Enzymes and Transporters in NASH: Research Application of Variants of Fatty Liver Disease (FLD) Tissues” Presented by Maciej Czerwinski, Ph.D., XenoTech Director of Consulting
Webinars

Adverse drug interaction risks in genetically-defined subpopulations

Presenter:  Maciej Czerwinski, Ph.D., Director of XenoTech Products R&D Synopsis: An increased appreciation of the effects of genetic variability on the pharmacokinetic and pharmacodynamic properties of xenobiotics creates a...
Blog

XenoTech Scientists Publish Paper, Present Research Evaluating Ketoconazole and its Alternative Clinical CYP3A4-5 Inhibitors as Inhibitors of Drug Transporters

XenoTech scientists published a paper in Drug Metabolism and Disposition evaluating Ketoconazole and its alternative clinical CYP3A4-5 inhibitors as inhibitors of drug...

Publications

The reliability of estimating Ki values for direct, reversible inhibition of cytochrome P450 enzymes from corresponding IC50 values: A retrospective analysis of 343 experiments

Lois J. Haupt, Faraz Kazmi, Brian W. Ogilvie, David B. Buckley, Brian D. Smith, Sarah Leatherman, Brandy Paris, Oliver Parkinson, and Andrew Parkinson In the...
Scientific Posters

In Vitro Assessment of the Drug-Drug Interaction of Rasagiline and Its Metabolite Aminoindan

Full Title In Vitro Assessment of the Drug-Drug Interaction of Rasagiline and Its Metabolite Aminoindan Abstract Rasagiline mesylate (PAI) is the active pharmaceutical ingredient of...
Scientific Posters

Exploring the Drug-Drug Interaction Between Gemfibrozil and Repaglinide in Rats

Full Title Exploring the Drug-Drug Interaction Between Gemfibrozil and Repaglinide in Rats: Metabolism and Transport Abstract A clinically-relevant drug-drug interaction (DDI) between the dyslipidemia drug gemfibrozil...
Publications

Anti-CD28 Monoclonal Antibody-stimulated Cytokines Released from Blood Suppress CYP1A2, CYP2B6 and CYP3A4 in Human Hepatocytes In Vitro

Maciej Czerwiński, Faraz Kazmi, Andrew Parkinson, and David B. Buckley Like most infections and certain inflammatory diseases, some therapeutic proteins cause a cytokine-mediated suppression of...
Publications

In vitro inhibition of human liver cytochrome P450 (CYP) and UDP-glucuronosyltransferase (UGT) enzymes by rose bengal: system-dependent effects on inhibitory potential

Faraz Kazmi, Lois J. Haupt, Jennifer R. Horkman, Brian D. Smith, David B. Buckley, Eric A. Wachter, and Jamie M. Singer 1. Rose bengal (4,5,6,7-tetrachloro-2′,4′,5′,7′-tetraiodofluorescein)...
Scientific Posters

An in vitro test system to evaluate drug-drug interactions with biologics

Full Title An in vitro test system to evaluate drug-drug interactions with biologics Authors Maciej Czerwinski1, Christina Renneke2, Joanne Parker2, Chad Pope1, Kevin Lyon1, Catherine...
Scientific Posters

Evaluation of dilution, dialysis and ultracentrifugation methods to assess the reversibility of metabolism-dependent inhibitors (MDIs) of cytochrome P450 (CYP) enzymes

Full Title Evaluation of dilution, dialysis and ultracentrifugation methods to assess the reversibility of metabolism-dependent inhibitors (MDIs) of cytochrome P450 (CYP) enzymes Abstract Metabolism-dependent inhibition...
Publications

An Evaluation of the Dilution Method for Identifying Metabolism-Dependent Inhibitors of Cytochrome P450 Enzymes

Andrew Parkinson, Faraz Kazmi, David B. Buckley, Phyllis Yerino, Brandy L. Paris, Jeff Holsapple, Paul Toren, Steve M. Otradovec and Brian W. Ogilvie Abstract Metabolism-dependent...
Publications

The Proton Pump Inhibitor, Omeprazole, but Not Lansoprazole or Pantoprazole, Is a Metabolism-Dependent Inhibitor of CYP2C19: Implications for Coadministration with Clopidogrel

Ogilvie BW, Yerino P, Kazmi F, Buckley DB, Rostami-Hodjegan A, Paris BL, Toren P, Parkinson A As a direct-acting inhibitor of CYP2C19 in vitro, lansoprazole...
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

Identification of a novel carbamoyl glucuronide as a metabolism-dependent inhibitior of CYP2C8

Full Title Identification of a novel carbamoyl glucuronide as a metabolism-dependent inhibitior of CYP2C8 Abstract Glucuronidation is a major route of drug biotransformation and detoxification,...
Scientific Posters

Pitfalls in the Design of Metabolism-Dependent CYP Inhibition (MDI) Experiments With a Dilution Step: Inhibitor Depletion by Metabolism and/or Microsomal Binding Leads to Underestimation of the Shifted IC50 Value

Full Title Pitfalls in the Design of Metabolism-Dependent CYP Inhibition (MDI) Experiments With a Dilution Step: Inhibitor Depletion by Metabolism and/or Microsomal Binding Leads to...
Scientific Posters

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

Full Title Induction of Liver and Intestinal Cytochrome P450 (CYP) Enzymes in Male and Female Cynomolgus Monkey Abstract The objective of the present study was...
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...