Update on drug-drug interaction at organic cation transporters: mechanisms, clinical impact, and proposal for advanced in vitro testing

Characterization of CYP2D6 drugs as substrates of human organic cation transporters (OCTs) and multidrug and toxin extrusion proteins (MATEs)

(2021) Claudia Neul et al.   BRITISH JOURNAL OF PHARMACOLOGY

Jiaotai Pill (交泰丸) Alleviates Insomnia through Regulating Monoamine and Organic Cation Transporters in Rats

(2021) Zhi-hui Li et al.   Chinese Journal of Integrative Medicine

Evaluation of in vitro absorption, distribution, metabolism, and excretion and assessment of drug-drug interaction of rucaparib, an orally potent poly(ADP-ribose) polymerase inhibitor

(2020) Mingxiang Liao et al.   XENOBIOTICA

A drug–drug interaction study to evaluate the impact of peficitinib on OCT1- and MATE1-mediated transport of metformin in healthy volunteers

(2020) Mai Shibata et al.   EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY

L-tetrahydropalmatine attenuates cisplatin-induced nephrotoxicity via selective inhibition of organic cation transporter 2 without impairing its antitumor efficacy

(2020) Cui Li et al.   BIOCHEMICAL PHARMACOLOGY

Organic cation transporter 3 and the dopamine transporter differentially regulate catecholamine uptake in the basolateral amygdala and nucleus accumbens

(2020) Katherine M. Holleran et al.   EUROPEAN JOURNAL OF NEUROSCIENCE

Tucatinib Inhibits Renal Transporters OCT2 and MATE Without Impacting Renal Function in Healthy Subjects

(2020) Ariel R. Topletz‐Erickson et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Clinical Aspects of Transporter-Mediated Drug-Drug Interactions

(2019) Arne Gessner et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Interplay of the Organic Cation Transporters OCT1 and OCT2 with the Apically Localized Export Protein MATE1 for the Polarized Transport of Trospium

(2019) Birgit Deutsch et al.   MOLECULAR PHARMACEUTICS

A systematic in vitro investigation of the inhibitor preincubation effect on multiple classes of clinically relevant transporters

(2019) Peter Tatrai et al.   DRUG METABOLISM AND DISPOSITION

Drug-drug interaction between crizotinib and entecavir via renal secretory transporter OCT2

(2019) Wenying Shu et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Organic Cation Transporters in Health and Disease

(2019) Hermann Koepsell   PHARMACOLOGICAL REVIEWS

Assay Conditions Influence Affinities of Rat Organic Cation Transporter 1: Analysis of Mutagenesis in the Modeled Outward-Facing Cleft by Measuring Effects of Substrates and Inhibitors on Initial Uptake

(2018) Valentin Gorboulev et al.   MOLECULAR PHARMACOLOGY

Assessment of Substrate Dependent Ligand Interactions at the Organic Cation Transporter OCT2 Using Six Model Substrates

(2018) Philip J Sandoval et al.   MOLECULAR PHARMACOLOGY

Multiple binding sites in organic cation transporters require sophisticated procedures to identify interactions of novel drugs

(2018) Hermann Koepsell   BIOLOGICAL CHEMISTRY

Transporters in Drug Development: 2018 ITC Recommendations for Transporters of Emerging Clinical Importance

(2018) Maciej J. Zamek-Gliszczynski et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Rat Organic Cation Transporter 1 Contains Three Binding Sites for Substrate 1-Methyl-4-phenylpyridinium per Monomer

(2018) Thorsten Keller et al.   MOLECULAR PHARMACOLOGY

Irinotecan Alters the Disposition of Morphine Via Inhibition of Organic Cation Transporter 1 (OCT1) and 2 (OCT2)

(2018) Peng Zhu et al.   PHARMACEUTICAL RESEARCH

OCTN: A Small Transporter Subfamily with Great Relevance to Human Pathophysiology, Drug Discovery, and Diagnostics

(2018) Lorena Pochini et al.   SLAS Discovery

Beyond drug-drug interactions: effects of transporter inhibition on endobiotics, nutrients and toxins

(2017) Eve-Irene Lepist et al.   Expert Opinion on Drug Metabolism & Toxicology

Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1)

(2017) Eugene C. Chen et al.   JOURNAL OF MEDICINAL CHEMISTRY

OCT1 mediates hepatic uptake of sumatriptan and loss-of-functionOCT1polymorphisms affect sumatriptan pharmacokinetics

(2016) J Matthaei et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

The plasma membrane monoamine transporter (PMAT): Structure, function, and role in organic cation disposition

(2016) J Wang   CLINICAL PHARMACOLOGY & THERAPEUTICS

The Effect of Dolutegravir on the Pharmacokinetics of Metformin in Healthy Subjects

(2016) Ivy H. Song et al.   JAIDS-JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES

Evaluation and Quantitative Prediction of Renal Transporter-Mediated Drug-Drug Interactions

(2016) Bo Feng et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Metformin Action: Concentrations Matter

(2015) Ling He et al.   Cell Metabolism

The Effect of Famotidine, a MATE1-Selective Inhibitor, on the Pharmacokinetics and Pharmacodynamics of Metformin

(2015) Jennifer E. Hibma et al.   CLINICAL PHARMACOKINETICS

A Comprehensive Review of Drug–Drug Interactions with Metformin

(2015) Tore Bjerregaard Stage et al.   CLINICAL PHARMACOKINETICS

Steady-state pharmacokinetics of metformin is independent of the OCT1 genotype in healthy volunteers

(2015) Mette Marie Hougaard Christensen et al.   EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY

Role of organic cation transporters in drug–drug interaction

(2015) Hermann Koepsell   Expert Opinion on Drug Metabolism & Toxicology

Role of organic cation transporters (OCTs) in the brain

(2015) Thomas Couroussé et al.   PHARMACOLOGY & THERAPEUTICS

Global genetic analyses reveal strong inter-ethnic variability in the loss of activity of the organic cation transporter OCT1

(2015) Tina Seitz et al.   Genome Medicine

Verapamil decreases the glucose-lowering effect of metformin in healthy volunteers

(2014) Sung Kweon Cho et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Pharmacokinetic Evaluations of the Co-Administrations of Vandetanib and Metformin, Digoxin, Midazolam, Omeprazole or Ranitidine

(2014) Susanne Johansson et al.   CLINICAL PHARMACOKINETICS

Association of Organic Cation Transporter 1 With Intolerance to Metformin in Type 2 Diabetes: A GoDARTS Study

(2014) Tanja Dujic et al.   DIABETES

N1-methylnicotinamide as an endogenous probe for drug interactions by renal cation transporters: studies on the metformin–trimethoprim interaction

(2014) Fabian Müller et al.   EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY

Brain organic cation transporter 2 controls response and vulnerability to stress and GSK3β signaling

(2014) T Couroussé et al.   MOLECULAR PSYCHIATRY

Revisiting Serotonin Reuptake Inhibitors and the Therapeutic Potential of “Uptake-2” in Psychiatric Disorders

(2013) Lynette C. Daws et al.   ACS Chemical Neuroscience

Morphine is a substrate of the organic cation transporter OCT1 and polymorphisms in OCT1 gene affect morphine pharmacokinetics after codeine administration

(2013) Mladen V. Tzvetkov et al.   BIOCHEMICAL PHARMACOLOGY

Role of organic cation transporter OCT2 and multidrug and toxin extrusion proteins MATE1 and MATE2-K for transport and drug interactions of the antiviral lamivudine

(2013) Fabian Müller et al.   BIOCHEMICAL PHARMACOLOGY

Trimethoprim-metformin interaction and its genetic modulation by OCT2 and MATE1 transporters

(2013) Barbara Grün et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Effect of Concomitant Administration of Trospium Chloride Extended Release on the Steady-State Pharmacokinetics of Metformin in Healthy Adults

(2013) Michael G. Oefelein et al.   CLINICAL DRUG INVESTIGATION

Clinical Pharmacokinetic, Pharmacodynamic and Drug-Interaction Profile of the Integrase Inhibitor Dolutegravir

(2013) Mackenzie L. Cottrell et al.   CLINICAL PHARMACOKINETICS

Profiling Solute Carrier Transporters in the Human Blood–Brain Barrier

(2013) E G Geier et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Emerging Transporters of Clinical Importance: An Update From the International Transporter Consortium

(2013) K M Hillgren et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Combinatorial Pharmacophore Modeling of Organic Cation Transporter 2 (OCT2) Inhibitors: Insights into Multiple Inhibitory Mechanisms

(2013) Yuan Xu et al.   MOLECULAR PHARMACEUTICS

Substrate- and Cell Contact-Dependent Inhibitor Affinity of Human Organic Cation Transporter 2: Studies with Two Classical Organic Cation Substrates and the Novel Substrate Cd2+

(2013) Frank Thévenod et al.   MOLECULAR PHARMACEUTICS

Effects of genetic variants in SLC22A2 organic cation transporter 2 and SLC47A1 multidrug and toxin extrusion 1 transporter on cisplatin-induced adverse events

(2012) Kazufumi Iwata et al.   Clinical and Experimental Nephrology

Renal drug–drug interactions: what we have learned and where we are going

(2012) Eve-Irene Lepist et al.   Expert Opinion on Drug Metabolism & Toxicology

Discovery of Potent, Selective Multidrug and Toxin Extrusion Transporter 1 (MATE1, SLC47A1) Inhibitors Through Prescription Drug Profiling and Computational Modeling

(2012) Matthias B. Wittwer et al.   JOURNAL OF MEDICINAL CHEMISTRY

Association of genetic variation in the organic cation transporters OCT1, OCT2 and multidrug and toxin extrusion 1 transporter protein genes with the gastrointestinal side effects and lower BMI in metformin-treated type 2 diabetes patients

(2012) Linda Tarasova et al.   Pharmacogenetics and Genomics

Effects of a MATE Protein Inhibitor, Pyrimethamine, on the Renal Elimination of Metformin at Oral Microdose and at Therapeutic Dose in Healthy Subjects

(2011) H Kusuhara et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Pharmacokinetics and Tolerability of Vandetanib in Chinese Patients With Solid, Malignant Tumors: An Open-Label, Phase I, Rising Multiple-Dose Study

(2011) Li Zhang et al.   CLINICAL THERAPEUTICS

Organic cation transporter 2 controls brain norepinephrine and serotonin clearance and antidepressant response

(2011) A Bacq et al.   MOLECULAR PSYCHIATRY

Selective Transport of Monoamine Neurotransmitters by Human Plasma Membrane Monoamine Transporter and Organic Cation Transporter 3

(2010) H. Duan et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

OCT2 polymorphisms and in-vivo renal functional consequence: studies with metformin and cimetidine

(2010) Zhi-Jun Wang et al.   Pharmacogenetics and Genomics

Effects of OCT1 polymorphisms on the cellular uptake, plasma concentrations and efficacy of the 5-HT3 antagonists tropisetron and ondansetron

(2010) M V Tzvetkov et al.   PHARMACOGENOMICS JOURNAL

Contribution of Organic Cation Transporter 2 (OCT2) to Cisplatin-Induced Nephrotoxicity

(2009) K K Filipski et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

The Effects of Genetic Polymorphisms in the Organic Cation Transporters OCT1, OCT2, and OCT3 on the Renal Clearance of Metformin

(2009) M V Tzvetkov et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Expression of organic cation transporters OCT1 (SLC22A1) and OCT3 (SLC22A3) is affected by genetic factors and cholestasis in human liver

(2009) Anne T. Nies et al.   HEPATOLOGY

Involvement of Human Multidrug and Toxin Extrusion 1 in the Drug Interaction between Cimetidine and Metformin in Renal Epithelial Cells

(2009) M. Tsuda et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Transport of Lamivudine [(-)- -L-2',3'-Dideoxy-3'-thiacytidine] and High-Affinity Interaction of Nucleoside Reverse Transcriptase Inhibitors with Human Organic Cation Transporters 1, 2, and 3

(2009) G. Minuesa et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Five Amino Acids in the Innermost Cavity of the Substrate Binding Cleft of Organic Cation Transporter 1 Interact with Extracellular and Intracellular Corticosterone

(2009) C. Volk et al.   MOLECULAR PHARMACOLOGY

Genetic Variants of the Organic Cation Transporter 2 Influence the Disposition of Metformin

(2008) IS Song et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Structural Requirements for Drug Inhibition of the Liver Specific Human Organic Cation Transport Protein 1

(2008) Gustav Ahlin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Organic cation transporter 3: Keeping the brake on extracellular serotonin in serotonin-transporter-deficient mice

(2008) N. L. Baganz et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA