A critical perspective on 3D liver models for drug metabolism and toxicology studies

AS Serras, JS Rodrigues, M Cipriano… - Frontiers in cell and …, 2021 - frontiersin.org
The poor predictability of human liver toxicity is still causing high attrition rates of drug
candidates in the pharmaceutical industry at the non-clinical, clinical, and post-marketing …

Cell spheroids as a versatile research platform: formation mechanisms, high throughput production, characterization and applications

MC Decarli, R Amaral, DP Dos Santos, LB Tofani… - …, 2021 - iopscience.iop.org
Abstract Three-dimensional (3D) cell culture has tremendous advantages to closely mimic
the in vivo architecture and microenvironment of healthy tissue and organs, as well as of …

Pharmacological blockage of the AHR-CYP1A1 axis: a call for in vivo evidence

NR Coelho, AB Pimpão, MJ Correia… - Journal of Molecular …, 2022 - Springer
The aryl hydrocarbon receptor (AHR) is a ligand-activated transcription factor that can be
activated by structurally diverse compounds arising from the environment and the microbiota …

Supernatant from hepatocyte cultures with drugs that cause idiosyncratic liver injury activates macrophage inflammasomes

R Kato, J Uetrecht - Chemical research in toxicology, 2017 - ACS Publications
There is increasing evidence that most idiosyncratic drug-induced liver injury (IDILI) is
immune mediated, and in most cases, reactive metabolites appear to be responsible for the …

Green electrosynthesis of drug metabolites

R Asra, AM Jones - Toxicology Research, 2023 - academic.oup.com
In this concise review, the field of electrosynthesis (ES) as a green methodology for
understanding drug metabolites linked to toxicology is exemplified. ES describes the …

Self-assembled 3D spheroids and hollow-fibre bioreactors improve MSC-derived hepatocyte-like cell maturation in vitro

M Cipriano, N Freyer, F Knöspel, NG Oliveira… - Archives of …, 2017 - Springer
Abstract 3D cultures of human stem cell-derived hepatocyte-like cells (HLCs) have emerged
as promising models for short-and long-term maintenance of hepatocyte phenotype in vitro …

Reactive metabolite of gefitinib activates inflammasomes: implications for gefitinib-induced idiosyncratic reaction

R Kato, Y Ijiri, T Hayashi, J Uetrecht - The Journal of Toxicological …, 2020 - jstage.jst.go.jp
The epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKIs) have been
approved for non-small cell lung cancer. Although EGFR TKIs are less toxic than traditional …

Unusual biotransformation reactions of drugs and drug candidates

EM Isin - Drug Metabolism and Disposition, 2023 - ASPET
Detailed assessment of the fate of drugs in nonclinical test species and humans is essential
to ensure the safety and efficacy of medicines in patients. In this context, biotransformation of …

Unmasking efavirenz neurotoxicity: Time matters to the underlying mechanisms

NM Grilo, MJ Correia, JP Miranda, M Cipriano… - European Journal of …, 2017 - Elsevier
Efavirenz is an anti-HIV drug that presents relevant short-and long-term central nervous
system adverse reactions. Its main metabolite (8-hydroxy-efavirenz) was demonstrated to be …

Drugs of abuse from a different toxicological perspective: an updated review of cocaine genotoxicity

NG Oliveira, RJ Dinis-Oliveira - Archives of Toxicology, 2018 - Springer
Cocaine is one of the most widely consumed psychoactive substances and has been
recognized as a major public health concern for many years. While several aspects of the …