2011
Characterization of Short-Lived Electrophilic Metabolites of the Anticancer Agent Laromustine (VNP40101M)
Nassar A, King I, Du J. Characterization of Short-Lived Electrophilic Metabolites of the Anticancer Agent Laromustine (VNP40101M). Chemical Research In Toxicology 2011, 24: 568-578. PMID: 21361357, DOI: 10.1021/tx100453t.Peer-Reviewed Original ResearchConceptsHuman liver microsomesNuclear magnetic resonance spectroscopyPhase II conjugatesN-acetylecysteinePooled human liver microsomesFragment ionsLiver microsomesPhase 1 metabolismCofactor nicotinamide adenine dinucleotide phosphateReactive intermediatesMoietyElectrophilic metabolitesMagnetic resonance spectroscopyM-4MethylformamidePhysiological pHVNP40101MResonance spectroscopyLaromustineConjugateActive moietyRearrangementAlkylating agentsH-DCysteine
2009
An in Vitro Evaluation of the Victim and Perpetrator Potential of the Anticancer Agent Laromustine (VNP40101M), Based on Reaction Phenotyping and Inhibition and Induction of Cytochrome P450 Enzymes
Nassar A, King I, Paris B, Haupt L, Ndikum-Moffor F, Campbell R, Usuki E, Skibbe J, Brobst D, Ogilvie B, Parkinson A. An in Vitro Evaluation of the Victim and Perpetrator Potential of the Anticancer Agent Laromustine (VNP40101M), Based on Reaction Phenotyping and Inhibition and Induction of Cytochrome P450 Enzymes. Drug Metabolism And Disposition 2009, 37: 1922-1930. PMID: 19520774, DOI: 10.1124/dmd.109.027516.Peer-Reviewed Original ResearchConceptsInhibition of CYP2B6Cytochrome P450 enzymesInhibition of CYP1A2Induction of cytochrome P450 enzymesPrimary cultures of human hepatocytesCultures of human hepatocytesPlasma C(maxHuman liver microsomesInduce CYP1A2Intravenous administrationClinical effectsCYP2C19P450 enzymesCYP3A4/5CYP2B6Human hepatocytesMetabolite profilesAnticancer drugsHydroxylated metabolitesIn vitro evaluationLaromustineLiver microsomesCYP3A4Reactive intermediatesCYP1A2
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