… 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 …

… 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 …

… 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 …

… to abacavir metabolism has not been fully characterized. The pharmacogenetic study of …
Monitoring abacavir bioactivation in humans: screening for an aldehyde metabolite. Toxicol. …

… predictable during preclinical testing and predisposing factors … (metabolite) binds covalently
to protein, and drug(metabolite)-… Abacavir binds endogenously deep within the MHC peptide …

… 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 …

… , abacavir, lamivudine, and tenofovir on isolated human peripheral … aldehyde dehydrogenases
catalyze the phase I metabolism … significant impacts on the bioactivation and disposition of …

… 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 …

… 3-Hydroxytamoxifen is reported to be bioactivated by O-sulfation to form the therapeutically
… Thus, bioactivation of hydroxylated products to toxic metabolites results from their oxidations …

… acid metabolites by aldehyde oxidase or the aldehyde … by alcohol dehydrogenase (eg,
abacavir [8]) and dealkylation of some … -reaction monitoring transition as the parent aldehyde. The …