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. Author manuscript; available in PMC: 2011 Oct 1.
Published in final edited form as: Pharmacogenet Genomics. 2010 Oct;20(10):575–585. doi: 10.1097/FPC.0b013e32833b04af

Fig. 4.

Fig. 4

Characterization of exemestane-17-O-glucuronide by UPLC/MS/MS and kinetic analysis of the glucuronidation of 17-dihydroexemestane by UGToverexpressing cells. Panel (a), Representative UPLC trace using 250 μg human liver microsome (HLM) and 300 μmol/l 17-dihydroexemestane incubated for 2 h (top trace); representative UPLC trace using 250 μg HLM and 300 μmol/l 17-dihydroexemestane incubated with β-glucuronidase for 16 h (middle trace) and representative UPLC trace using 250 μg UGT2B17 cell homogenates and 300 μmol/l 17-dihydroexemestane incubated for 2 h (bottom trace). Panel (b), Mass spectrum of peak at retention time of 2.59 min. Peak at retention time of 3.61 min is 17-dihydroexemestane. Panel (c), Representative concentration curve for exemestane-17-O-glucuronide formation from UGT2B17-overexpressing cell homogenates. The concentrations of 17-dihydroexemestane used were: 4.7, 9.4, 18.8, 37.5, 75, and 150 μmol/l. Panel (d), Representative concentration curve for exemestane-17-O-glucuronide formation from UGT1A10-overexpressing cell homogenates. The concentrations of 17-dihydroexemestane used were: 4.7, 9.4, 18.8, 37.5, 75, 150, and 300 μmol/l. All other conditions are described in the Materials and methods section.