The multikinase inhibitor axitinib in the treatment of advanced hepatocellular carcinoma: the current clinical applications and the molecular mechanisms

H Jiang, J Liao, L Wang, C Jin, J Mo… - Frontiers in …, 2023 - frontiersin.org
Advanced hepatocellular carcinoma (HCC) is a formidable public health problem with
limited curable treatment options. Axitinib, an oral tyrosine kinase inhibitor, is a potent and …

Loperamide toxicity: recommendations for patient monitoring and management

W Eggleston, R Palmer, PA Dubé, S Thornton… - Clinical …, 2020 - Taylor & Francis
Who: This position statement is a collaborative effort by the American Academy of Clinical
Toxicology (AACT) and the American Association of Poison Control Centers (AAPCC) and …

Plasticizer interaction with the heart: chemicals used in plastic medical devices can interfere with cardiac electrophysiology

R Jaimes III, D McCullough, B Siegel… - Circulation …, 2019 - Am Heart Assoc
Background: Phthalates are used as plasticizers in the manufacturing of flexible, plastic
medical products. Patients can be subjected to high phthalate exposure through contact with …

[HTML][HTML] A systematic strategy for estimating hERG block potency and its implications in a new cardiac safety paradigm

BJ Ridder, DJ Leishman, M Bridgland-Taylor… - Toxicology and Applied …, 2020 - Elsevier
Introduction hERG block potency is widely used to calculate a drug's safety margin against
its torsadogenic potential. Previous studies are confounded by use of different patch clamp …

The potential mechanisms behind loperamide-induced cardiac arrhythmias associated with human abuse and extreme overdose

HR Lu, BP Damiano, M Kreir, J Rohrbacher… - Biomolecules, 2023 - mdpi.com
Loperamide has been a safe and effective treatment for diarrhea for many years. However,
many cases of cardiotoxicity with intentional abuse of loperamide ingestion have recently …

[HTML][HTML] hERG block potencies for 5 positive control drugs obtained per ICH E14/S7B Q&As best practices: Impact of recording temperature and drug loss

CA Baron, N Thiebaud, M Ren… - … of Pharmacological and …, 2022 - Elsevier
According to the ICH S7B guideline, drug candidates are screened for hERG block prior to
first-in-human testing to predict the likelihood of delayed repolarization associated with a …

Molecular determinants of loperamide and N-desmethyl loperamide binding in the hERG cardiac K+ channel

RJ Vaz, J Kang, Y Luo, D Rampe - Bioorganic & Medicinal Chemistry …, 2018 - Elsevier
Abuse of the common anti-diarrheal loperamide is associated with QT interval prolongation
as well as development of the potentially fatal arrhythmia torsades de pointes. The …

Quantitative systems pharmacology models for a new international cardiac safety regulatory paradigm: an overview of the comprehensive in vitro proarrhythmia assay …

Z Li, C Garnett, DG Strauss - CPT: Pharmacometrics & Systems …, 2019 - Wiley Online Library
As a relatively new discipline, quantitative systems pharmacology has seen a significant
increase in the application and utility of drug development. One area that could greatly …

Electrocardiographic changes in loperamide toxicity: Case report and review of literature

T Teigeler, H Stahura, R Alimohammad… - Journal of …, 2019 - Wiley Online Library
Introduction Loperamide, an antidiarrheal agent, is a µ‐opioid receptor agonist increasingly
abused to prevent opioid withdrawal or to produce euphoric effects. At supra‐therapeutic …

Functional characteristics of CYP3A4 allelic variants on the metabolism of loperamide in vitro

QM Lin, YH Li, Q Liu, NH Pang, RA Xu… - Infection and Drug …, 2019 - Taylor & Francis
Background Cytochrome P450 3A4 (CYP3A4) appears to be genetically polymorphic, which
in turn contributes to interindividual variability in response to therapeutic drugs. Loperamide …