Characterization of dasatinib and its structural analogs as CYP3A4 mechanism-based inactivators and the proposed bioactivation pathways

Drug Metabolism and Disposition

Volumn 37, Issue 6, 2009, Pages 1242-1250

  Li, Xiaohai ^a   He, Yuanjun ^a   Ruiz, Claudia H ^a   Koenig, Marcel ^a   Cameron, Michael D ^a  

^a SCRIPPS RESEARCH INSTITUTE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CARBAMAZEPINE; CYTOCHROME P450 3A4; DASATINIB; DRUG METABOLITE; GLUTATHIONE; IMINE METHIDE; KETOCONAZOLE; MIDAZOLAM; PIPERAZINE; PYRIMIDINE DERIVATIVE; QUINONE IMINE; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CHEMICAL MODIFICATION; CHRONIC MYELOID LEUKEMIA; DOSE TIME EFFECT RELATION; DRUG ACTIVATION; DRUG MECHANISM; DRUG METABOLISM; ENZYME INACTIVATION; HUMAN; HUMAN CELL; HYDROXYLATION; LIVER MICROSOME METABOLISM; MOUSE; NONHUMAN; OXIDATION; PRIORITY JOURNAL; RAT; STRUCTURE ACTIVITY RELATION;

CHROMATOGRAPHY, HIGH PRESSURE LIQUID; CYTOCHROME P-450 CYP3A; DICLOFENAC; ENZYME ACTIVATION; ENZYME INHIBITORS; GLUTATHIONE; HUMANS; K562 CELLS; MICROSOMES, LIVER; PIPERAZINES; PROTEIN KINASE INHIBITORS; PYRIMIDINES; SPECTROMETRY, MASS, ELECTROSPRAY IONIZATION; THIAZOLES;

EID: 66649132811     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.108.025932     Document Type: Article

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