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Drug Transporters

Drug transport studies use regulatory guidance-compliant test systems to investigate a compound’s potential to operate as a substrate or inhibitor of known uptake (SLC) and efflux (ABC) transporters, precipitating a potential drug-drug interaction. For more information about these services, visit our Drug Transport contract service page.

 

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...
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...
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...
Blog

Interesting Topics at the 3rd SCI-RSC Symposium on Transporters in Drug Discovery and Development

A recap of some of the important and promising research that was presented at the Transporters in Drug Discovery and Development symposium...

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...

Webinars

ADME 101: Efflux and Uptake Drug Transporters

Presented by Andrew Taylor, Ph.D., Services Technical Support Manager Drug transport can be thought of as the AD&E in ADME, as transporters are responsible for absorption, distribution,...
Webinars

ADME 101: Lysosomal Trapping

Presenter:  Andrew Taylor, Ph.D., Services Technical Support Manager This ADME 101 video discusses how compounds can become trapped by lysosomes, which can lead to high...
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...

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

How can in vitro and in vivo studies help me understand my drug’s clearance?

Systemic clearance, denoting how much drug is cleared from a volume of blood per unit of time, is of critical...

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?...
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

Full Title The evaluation of induction and inhibition potency of various drugs on CYP3A4 and OATP1B1/1B3 Authors Ryota Takeuchi, Rena Kusano, Tomoko Sasai, Takami Sarashina,...
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

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

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

Reduced Pricing for In Vitro Transporter Studies

We’re pleased to announce that our scientists’ ongoing dedication to enhancing our processes and discovering new efficiencies without sacrificing quality...

White Papers

Dexamethasone reduces airway epithelial Cl− secretion by rapid non-genomic inhibition of KCNQ1, KCNN

Darina Hynes (XenoTech EU Business Development Manager), Brian J.Harvey Basolateral membrane K+ channels play a key role in basal and agonist stimulated Cl− transport across airway epithelial cells...
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...

Scientific Posters

An assessment of in vitro inhibition of CYPs, UGTs and transporters by phosphodiester- or phosphorothioate-linked oligonucleotides

Full Title An assessment of in vitro inhibition of CYPs, UGTs and transporters by phosphodiester- or phosphorothioate-linked oligonucleotides Presented at the 2019 Marbach Castle Drug-Drug...
Webinars

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

Presenter: Brian Ogilvie, Ph.D., XenoTech Vice President of Scientific Consulting Synopsis: In October, 2017, the US FDA revised and split its 2012 draft guidance for industry...
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...

Webinars

Understanding P-gp & BCRP Inhibition Assay Design & Outcomes

In vitro drug transporter inhibition studies are recognized for their importance due to the major role transporters play in absorption, distribution and excretion of compounds, and the toxicological and pharmacological consequences of transporter-mediated drug-drug interactions (DDI). P-gp and BCRP transporters limit intestinal absorption and blood-brain barrier penetration, and facilitate excretion into bile and urine...
Blog

Coverage from the October 2018 PBSS DDI Workshop

The Pharmaceutical and BioScience Society (PBSS) hosted the workshop “Drug-Drug Interactions: Update on Risk Assessment, Clinical Evaluation and Regulatory Requirements” on October...

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

Strategies to improve the predictions accuracy of hepatic intrinsic clearance of three antidiabetic drugs: application of the extended clearance concept and consideration of the effect of albumin on CYP2C metabolism and OAT1B1-mediated hepatic uptake

Ryo Fujino, Kenta Hashizume, Shinsuke Aoyama, Kazuya Maeda, Kiyomi Ito, Kota Toshimoto, Wooin Lee, Shin-ichi Ninomiya, Yuichi Sugiyama The antidiabetic drugs glibenclamide, repaglinide, and nateglinide...
Blog

New Recommendation: Evaluate NMEs for OCT1 Transporter-Mediated DDI Potential

Brian Ogilvie, Ph.D., Vice President of Scientific Consulting at XenoTech, presented a case study on the importance of the hepatic OCT1...

Publications

Challenges and solutions in today’s in vitro transporter research

Dr. Joanna Barbara In vitro drug transport assays are performed throughout drug development and range from simple permeability screens to kinetic assessments in complex assay formats. Sometimes interpreting...
Blog

Challenges & Solutions in Today’s In Vitro Transporter Research

Transporters are membrane-bound proteins that govern the passage of drugs into and out of cells. These gatekeeper proteins can be...

Webinars

Challenges & Solutions In Today’s In Vitro Transporter Research Landscape

Recent changes to the FDA in vitro DDI guidance document have emphasized the need for more considered transporter study designs to better inform in vivo expectations for drugs in development. Additionally, challenges associated with some diverse compounds in what should have been straightforward in vitro transporter assays will be examined. Case studies will explore the problematic observations or data, creative methods of troubleshooting applied, and how we can learn from those experiences to better understand and address surprises in future transporter studies...
Blog

AAPS-FDA Drug Transporters

The American Association of Pharmaceutical Scientists (AAPS) and U.S. Food and Drug Administration (FDA) co-sponsored the workshop “Drug Transporters in ADME:...

Publications

An assessment of the in vitro inhibition of cytochrome P450 enzymes (CYP), UDP-glucuronsyltransferases (UGT) and transporters by phosphodiester- or phosphorothioate-linked oligonucleotides

Faraz Kazmi, Phyllis Yerino, Chase McCoy, Andrew Parkinson, David B Buckley and Brian W Ogilvie Oligonucleotides represent an expanding class of pharmacotherapeutics in development for...
Blog

XenoTech Adds US Support for MATE1 and MATE2-K Drug Transporter Studies

Transporters have become increasingly important in drug development due to the major role they play in absorption, distribution and excretion of...

Scientific Posters

Comparison of two hepatic uptake assay methods

Full Title “Comparison of two hepatic uptake assay methods, plated and oil layer methods, using  human and preclinical species cryopreserved hepatocytes” Authors Akito Takahashi, Ryota...
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...
Publications

In Vitro Studies with Two Human Organic Anion Transporters: OAT2 & OAT7

Mathialagan S, Costales C, Tylaska L, Kimoto E, Vildhede A, Johnson J, Johnson N, Sarashina T, Hashizume K, Isringhausen CD, Vermeer LMM, Wolff AR, Rodrigues...
Blog

URI Drug Transporters Workshop Presentations

The University of Rhode Island College of Pharmacy’s 5th Annual Transporters in Drug Discovery and Development: Driving Knowledge from Laboratory...

Blog

XenoTech Adds New Drug Transporters to Portfolio

Transporters have become increasingly important in drug development due to the major role they play in absorption, distribution and excretion of...

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

Global marine pollutants inhibit P-glycoprotein: Environmental levels, inhibitory effects, and cocrystal structure

The world’s oceans are a global reservoir of persistent organic pollutants to which Humans and other animals are exposed. Although it is well known that...
Webinars

Evaluation of Ketoconazole and its Alternative Clinical CYP3A4/5 Inhibitors as Inhibitors of Drug Transporters

Presented by: Lydia Vermeer, Ph.D., Senior Scientist, Drug Transport Ketoconazole is an orally available, synthetic, broad spectrum, antifungal agent. Approved in 1982 by the FDA...
Scientific Posters

Automated High Content Drug Transport Screening with Transwell Plates for Drug Discovery

Full Title Automated High Content Drug Transport Screening with Transwell Plates for Drug Discovery Abstract The purpose of this study was to develop a method...
Scientific Posters

Comparison of Ki and IC50 Values for Prototypical Inhibitors of ABC Transporters

Full Title Comparison of Ki and IC50 Values for Prototypical Inhibitors of the Human ABC Transporters P-gp and BCRP in Membrane Vesicles Abstract P-gp (ABCB1/MDR1) and...
Scientific Posters

Evaluation of BSEP Inhibitors Using B-CLEAR® Human Hepatocytes to Predict Inhibition and Cholestasis

Full Title Evaluation of BSEP Inhibitors Using B-CLEAR® Human Hepatocytes to Predict Inhibition and Cholestasis Abstract Drug-induced liver injury (DILI) is characterized as liver injury...
Scientific Posters

Accumulation of Taurocholic Acid in B-CLEAR® Human Sandwich-Cultured Hepatocytes in the Presence of Clinically Relevant Cholestatic Agents

Full Title Accumulation of Taurocholic Acid in B-CLEAR® Human Sandwich-Cultured Hepatocytes in the Presence of Clinically Relevant Cholestatic Agents Abstract Drug induced liver injury (DILI)...
Scientific Posters

Comparison of Ki and IC50 Values for Prototypical Inhibitors of the Major Drug Uptake Transporters

Full Title Comparison of Ki and IC50 Values for Prototypical Inhibitors of the Major Drug Uptake Transporters Abstract We previously reported on the similarities and...
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...
Scientific Posters

The Use of Pooled Plated Cryopreserved Human Hepatocytes for the Determination of Metabolic Clearance, CYP Induction, and Uptake Transporter Studies

Full Title The Use of Pooled Plated Cryopreserved Human Hepatocytes for the Determination of Metabolic Clearance, CYP Induction, and Uptake Transporter Studies Abstract During early...
Publications

Drugs as Victims and Perpetrators and the Pharmacokinetic Concept of Maximum Exposure

Brian W. Ogilvie, Andrew Parkinson This article describes the dramatic but predictable impact of two perpetrators on the disposition of a victim drug. For a...
Scientific Posters

Comparing Ki and IC50 Values

Full Title Comparison of Ki and IC50 values for prototypical and clinically-relevant probe substrates of the hepatic transporters OATP1B1 and OATP1B3 Abstract Organic anion transporting polypeptides 1B1...
Scientific Posters

BCRP Transport Inhibition

Full Title System-dependent inhibition of BCRP transport by high- and low-permeable compounds in bi-directional MDCKII cells and membrane vesicles Abstract Breast cancer resistance protein (BCRP,...
Blog

Navigating the Transporter Wave of 2013

The International Transporter Consortium (ITC) issued 7 papers in the July 2013 issue of Clinical Pharmacology & Therapeutics. These 7...

Webinars

Navigating the Transporter Wave of 2013: A Review of the Seven Recent ITC Publications on Drug Transporters

Presented by: Greg Loewen, Amanda Hays and Andrea Wolff Seven papers were published by the International Transporter Consortium (ITC) in the July 2013 issue of Clinical...
Scientific Posters

Uptake and Efflux Transporters

This poster was presented at the annual AAPS conference in 2013 Full Title Comparison of IC50 Values for Prototypical and Clinically-Relevant Probe Substrates and Inhibitors...
Scientific Posters

Inhibitors of Uptake Transporters

This poster was presented at the annual AAPS conference in 2013. Full Title Comparison of Ki and IC50 Values for Prototypical Inhibitors of Uptake Transporters...
Webinars

Application of Hepatocytes for In Vitro Uptake Assays

Presented by: David Buckley, Ph.D. – CSO This webinar provides a basic review of concepts applicable to a structure-based approach for the evaluation of hepatic...