Drug–protein adducts: past, present, and future

TA Baillie - Medicinal Chemistry Research, 2020 - Springer
… recognized to underlie the bioactivation of many substituted … α,β-unsaturated aldehyde
metabolite of abacavir, did react … span in humans of ~120 days, also has been used to monitor

Involvement of Pazopanib and Sunitinib Aldehyde Reactive Metabolites in Toxicity and Drug–Drug Interactions in Vitro and in Patient Samples

MN Paludetto, JL Stigliani, A Robert… - Chemical Research …, 2019 - ACS Publications
… of these aldehyde RM in human plasma samples obtained during drug monitoring. Docking
… originating from the metabolic transformation, often called bioactivation, of particular …

Mitigating a Bioactivation Liability with an Azetidine-Based Inhibitor of Diacylglycerol Acyltransferase 2 (DGAT2) En Route to the Discovery of the Clinical Candidate …

R Sharma, MS Dowling, K Futatsugi… - Chemical Research in …, 2023 - ACS Publications
… mitigated the formation of the electrophilic aldehyde metabolite, and was a more potent …
In vitro metabolism studies were conducted on human tissue acquired from a third party that …

Biotransformation: impact and application of metabolism in drug discovery

J Shanu-Wilson, L Evans, S Wrigley… - ACS Medicinal …, 2020 - ACS Publications
… of metabolic liabilities, identification of any bioactivation to reactive … , and metabolic stability
testing of metabolites during lead … However, a proposed aldehyde oxidase metabolite of one …

Pharmacogenomics of antiretroviral drug metabolism and transport

ZJ Yu, EP Mosher, NN Bumpus - Annual review of …, 2021 - annualreviews.org
… to abacavir metabolism has not been fully characterized. The pharmacogenetic study of …
Monitoring abacavir bioactivation in humans: screening for an aldehyde metabolite. Toxicol. …

[HTML][HTML] What's been Hapten-ing over the last 88 years?

P Thomson, S Hammond, X Meng… - Medicinal Chemistry …, 2023 - Springer
… predictable during preclinical testing and predisposing factors … (metabolite) binds covalently
to protein, and drug(metabolite)-… Abacavir binds endogenously deep within the MHC peptide …

The Role of Drug Metabolism in Toxicity

UM HANUMEGOWDA, C DAVIS - Drug Metabolism Handbook …, 2022 - Wiley Online Library
… in the bioactivation of a xenobiotic and/or its metabolite(s) to … or organ systems may require
a tailored screening paradigm. … Metabolic activation of abacavir to an aldehyde intermediate …

Important roles of transporters in the pharmacokinetics of anti-viral nucleoside/nucleotide analogs

M Yang, X Xu - Expert opinion on drug metabolism & toxicology, 2022 - Taylor & Francis
… , abacavir, lamivudine, and tenofovir on isolated human peripheral … aldehyde dehydrogenases
catalyze the phase I metabolism … significant impacts on the bioactivation and disposition of …

Critical Examination of Selected Aspects of the ToxTracker In Vitro Genotoxicity Assay: Evaluation of S9 Metabolic Activation Protocols and Quantitative Interpretation …

L Boisvert - 2020 - ruor.uottawa.ca
screened for genotoxic activity. To this end, Toxys BV developed the in vitro ToxTracker®
assay, which detects (geno)toxicity by monitoring … ; reporter induction is monitored using flow …

Development of Long-acting Nanoformulated Abacavir ProTides

Z Lin, HE Gendelmant - 2019 - digitalcommons.unmc.edu
… In a mass balance study using [(14)C] abacavir, ABC and its two major metabolites
Monitoring abacavir bioactivation in humans: screening for an aldehyde metabolite. Toxicol …