Multi-laboratory comparisons of manual patch clamp hERG data generated using standardized protocols and following ICH S7B Q&A 2.1 best practices

Abstract Acute block of hERG channels is the most common mechanism underlying drug-induced QTC prolongation and potentially fatal Torsade de Pointes arrhythmia. Updates to ICH E14 Q&As now allow for using negative nonclinical data, including hERG, to support QTC risk assessment in late-stage cli...

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Main Authors: Claudia Alvarez Baron, Jun Zhao, Huimei Yu, Ming Ren, Nicolas Thiebaud, Donglin Guo, Giri Vegesna, Cheng-Hui Hsiao, Ryan DePalma, Sabyasachy Mistry, Isra Tariq, Md Shadiqur Rashid Roni, Omnia A. Ismaiel, Murali K. Matta, Vikram Patel, Manni Mashaee, Jose Vicente, Lars Johannesen, Jiansong Sheng, Simon Hebeisen, James Kramer, Andrew Bruening-Wright, Koji Nakano, Hiroshi Matsukawa, Jennifer Beck Pierson, Wendy W. Wu
Format: Article
Language:English
Published: Nature Portfolio 2025-08-01
Series:Scientific Reports
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Online Access:https://doi.org/10.1038/s41598-025-15761-8
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author Claudia Alvarez Baron
Jun Zhao
Huimei Yu
Ming Ren
Nicolas Thiebaud
Donglin Guo
Giri Vegesna
Cheng-Hui Hsiao
Ryan DePalma
Sabyasachy Mistry
Isra Tariq
Md Shadiqur Rashid Roni
Omnia A. Ismaiel
Murali K. Matta
Vikram Patel
Manni Mashaee
Jose Vicente
Lars Johannesen
Jiansong Sheng
Simon Hebeisen
James Kramer
Andrew Bruening-Wright
Koji Nakano
Hiroshi Matsukawa
Jennifer Beck Pierson
Wendy W. Wu
author_facet Claudia Alvarez Baron
Jun Zhao
Huimei Yu
Ming Ren
Nicolas Thiebaud
Donglin Guo
Giri Vegesna
Cheng-Hui Hsiao
Ryan DePalma
Sabyasachy Mistry
Isra Tariq
Md Shadiqur Rashid Roni
Omnia A. Ismaiel
Murali K. Matta
Vikram Patel
Manni Mashaee
Jose Vicente
Lars Johannesen
Jiansong Sheng
Simon Hebeisen
James Kramer
Andrew Bruening-Wright
Koji Nakano
Hiroshi Matsukawa
Jennifer Beck Pierson
Wendy W. Wu
author_sort Claudia Alvarez Baron
collection DOAJ
description Abstract Acute block of hERG channels is the most common mechanism underlying drug-induced QTC prolongation and potentially fatal Torsade de Pointes arrhythmia. Updates to ICH E14 Q&As now allow for using negative nonclinical data, including hERG, to support QTC risk assessment in late-stage clinical development. To interpret the hERG results, understanding hERG assay reproducibility or hERG data variability is pivotal. Protocol and best practice recommendations have been provided with the goal of minimizing lab-to-lab data differences, but the impact remains unclear. To fill this knowledge gap, hERG data from a HESI-coordinated multi-laboratory study were leveraged. Using standardized protocol and following best practices for patch clamp studies, five laboratories tested 28 drugs using the manual patch clamp technique. Systematic differences in block potencies were observed for data generated by one laboratory for the first 21 drugs, and these differences disappeared for the last seven drugs. Exposure, pharmacological sensitivity of the cell lines, and cell/data qualities were ruled out as the factors underlying systematic differences. All laboratories retested two drugs and obtained results within 1.6X of the initial testings, except for another laboratory that obtained data for one drug that differed from its initial testing by 7.6X. Descriptive statistics and meta-analysis were applied to the dataset to estimate what the distribution in hERG block potencies would be if a laboratory were to test the same drug repeatedly. This measure, or hERG data variability, was ~ 5X. Based on these results, hERG block potency values within 5X of each other should not be considered different, since these values are within the natural data distribution of the hERG assay; laboratory-specific safety margin threshold may be required to account for systematic data differences.
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spelling doaj-art-101fb0bef1454abdbb818bbca248877a2025-08-20T03:47:07ZengNature PortfolioScientific Reports2045-23222025-08-0115112010.1038/s41598-025-15761-8Multi-laboratory comparisons of manual patch clamp hERG data generated using standardized protocols and following ICH S7B Q&A 2.1 best practicesClaudia Alvarez Baron0Jun Zhao1Huimei Yu2Ming Ren3Nicolas Thiebaud4Donglin Guo5Giri Vegesna6Cheng-Hui Hsiao7Ryan DePalma8Sabyasachy Mistry9Isra Tariq10Md Shadiqur Rashid Roni11Omnia A. Ismaiel12Murali K. Matta13Vikram Patel14Manni Mashaee15Jose Vicente16Lars Johannesen17Jiansong Sheng18Simon Hebeisen19James Kramer20Andrew Bruening-Wright21Koji Nakano22Hiroshi Matsukawa23Jennifer Beck Pierson24Wendy W. Wu25Division of Applied Regulatory Science, Office of Clinical Pharmacology, Center for Drug Evaluation and Research, US Food and Drug AdministrationDivision of Applied Regulatory Science, Office of Clinical Pharmacology, Center for Drug Evaluation and Research, US Food and Drug AdministrationDivision of Applied Regulatory Science, Office of Clinical Pharmacology, Center for Drug Evaluation and Research, US Food and Drug AdministrationDivision of Applied Regulatory Science, Office of Clinical Pharmacology, Center for Drug Evaluation and Research, US Food and Drug AdministrationDivision of Applied Regulatory Science, Office of Clinical Pharmacology, Center for Drug Evaluation and Research, US Food and Drug AdministrationDivision of Cardiology and Nephrology, Office of Cardiology, Hematology, Endocrinology and Nephrology, Office of New Drugs, Center for Drug Evaluation and Research, US Food and Drug AdministrationDivision of Applied Regulatory Science, Office of Clinical Pharmacology, Center for Drug Evaluation and Research, US Food and Drug AdministrationDivision of Applied Regulatory Science, Office of Clinical Pharmacology, Center for Drug Evaluation and Research, US Food and Drug AdministrationDivision of Applied Regulatory Science, Office of Clinical Pharmacology, Center for Drug Evaluation and Research, US Food and Drug AdministrationDivision of Applied Regulatory Science, Office of Clinical Pharmacology, Center for Drug Evaluation and Research, US Food and Drug AdministrationDivision of Applied Regulatory Science, Office of Clinical Pharmacology, Center for Drug Evaluation and Research, US Food and Drug AdministrationDivision of Applied Regulatory Science, Office of Clinical Pharmacology, Center for Drug Evaluation and Research, US Food and Drug AdministrationDivision of Applied Regulatory Science, Office of Clinical Pharmacology, Center for Drug Evaluation and Research, US Food and Drug AdministrationDivision of Applied Regulatory Science, Office of Clinical Pharmacology, Center for Drug Evaluation and Research, US Food and Drug AdministrationDivision of Applied Regulatory Science, Office of Clinical Pharmacology, Center for Drug Evaluation and Research, US Food and Drug AdministrationDivision of Applied Regulatory Science, Office of Clinical Pharmacology, Center for Drug Evaluation and Research, US Food and Drug AdministrationDivision of Cardiology and Nephrology, Office of Cardiology, Hematology, Endocrinology and Nephrology, Office of New Drugs, Center for Drug Evaluation and Research, US Food and Drug AdministrationDivision of Cardiology and Nephrology, Office of Cardiology, Hematology, Endocrinology and Nephrology, Office of New Drugs, Center for Drug Evaluation and Research, US Food and Drug AdministrationCiPA LabB’SYS GmbHCharles River LaboratoriesCharles River LaboratoriesDrug Safety Testing Center Co., Ltd., Higashimatsuyama LaboratoriesDrug Safety Testing Center Co., Ltd., Higashimatsuyama LaboratoriesHealth and Environmental Science InstituteDivision of Applied Regulatory Science, Office of Clinical Pharmacology, Center for Drug Evaluation and Research, US Food and Drug AdministrationAbstract Acute block of hERG channels is the most common mechanism underlying drug-induced QTC prolongation and potentially fatal Torsade de Pointes arrhythmia. Updates to ICH E14 Q&As now allow for using negative nonclinical data, including hERG, to support QTC risk assessment in late-stage clinical development. To interpret the hERG results, understanding hERG assay reproducibility or hERG data variability is pivotal. Protocol and best practice recommendations have been provided with the goal of minimizing lab-to-lab data differences, but the impact remains unclear. To fill this knowledge gap, hERG data from a HESI-coordinated multi-laboratory study were leveraged. Using standardized protocol and following best practices for patch clamp studies, five laboratories tested 28 drugs using the manual patch clamp technique. Systematic differences in block potencies were observed for data generated by one laboratory for the first 21 drugs, and these differences disappeared for the last seven drugs. Exposure, pharmacological sensitivity of the cell lines, and cell/data qualities were ruled out as the factors underlying systematic differences. All laboratories retested two drugs and obtained results within 1.6X of the initial testings, except for another laboratory that obtained data for one drug that differed from its initial testing by 7.6X. Descriptive statistics and meta-analysis were applied to the dataset to estimate what the distribution in hERG block potencies would be if a laboratory were to test the same drug repeatedly. This measure, or hERG data variability, was ~ 5X. Based on these results, hERG block potency values within 5X of each other should not be considered different, since these values are within the natural data distribution of the hERG assay; laboratory-specific safety margin threshold may be required to account for systematic data differences.https://doi.org/10.1038/s41598-025-15761-8Cardiac safetyDelayed ventricular repolarizationExperimental uncertaintyConcentration-inhibitionAssay reproducibilitySafety margin
spellingShingle Claudia Alvarez Baron
Jun Zhao
Huimei Yu
Ming Ren
Nicolas Thiebaud
Donglin Guo
Giri Vegesna
Cheng-Hui Hsiao
Ryan DePalma
Sabyasachy Mistry
Isra Tariq
Md Shadiqur Rashid Roni
Omnia A. Ismaiel
Murali K. Matta
Vikram Patel
Manni Mashaee
Jose Vicente
Lars Johannesen
Jiansong Sheng
Simon Hebeisen
James Kramer
Andrew Bruening-Wright
Koji Nakano
Hiroshi Matsukawa
Jennifer Beck Pierson
Wendy W. Wu
Multi-laboratory comparisons of manual patch clamp hERG data generated using standardized protocols and following ICH S7B Q&A 2.1 best practices
Scientific Reports
Cardiac safety
Delayed ventricular repolarization
Experimental uncertainty
Concentration-inhibition
Assay reproducibility
Safety margin
title Multi-laboratory comparisons of manual patch clamp hERG data generated using standardized protocols and following ICH S7B Q&A 2.1 best practices
title_full Multi-laboratory comparisons of manual patch clamp hERG data generated using standardized protocols and following ICH S7B Q&A 2.1 best practices
title_fullStr Multi-laboratory comparisons of manual patch clamp hERG data generated using standardized protocols and following ICH S7B Q&A 2.1 best practices
title_full_unstemmed Multi-laboratory comparisons of manual patch clamp hERG data generated using standardized protocols and following ICH S7B Q&A 2.1 best practices
title_short Multi-laboratory comparisons of manual patch clamp hERG data generated using standardized protocols and following ICH S7B Q&A 2.1 best practices
title_sort multi laboratory comparisons of manual patch clamp herg data generated using standardized protocols and following ich s7b q a 2 1 best practices
topic Cardiac safety
Delayed ventricular repolarization
Experimental uncertainty
Concentration-inhibition
Assay reproducibility
Safety margin
url https://doi.org/10.1038/s41598-025-15761-8
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