TABLE 3

Exposures of Gwt1 inhibitors following oral or i.p. dosing of prodrugs in the presence or absence of 100 mg/kg ABT pretreatmenta

ProdrugAnalyteAvg AUCb (μg · h/ml) resulting from 26-mg/kg doseRatio of AUC with ABT/AUC without ABT
p.o. dosingi.p. dosingp.o. dosing + ABTi.p. dosing + ABTp.o. dosingi.p. dosing
APX001APX001A2.76 ± 0.234.36 ± 0.1141.50 ± 8.0924.28 ± 17.7415.05.6
APX2096APX203910.66 ± 0.4811.75 ± 1.8391.28 ± 20.7597.25 ± 12.618.68.3
APX2097APX20204.49 ± 2.324.31 ± 0.9641.94 ± 6.4135.61 ± 28.229.38.3
APX2104APX20413.49 ± 0.274.68 ± 0.7349.92 ± 10.3472.62 ± 9.0714.315.5
  • a p.o., oral; i.p., intraperitoneal.

  • b Time course for the experiment: 0.083 0.5, 2, 4, 8, and 24 h postdose of 26 mg/kg prodrug (n = 3 per time point). AUC is the area under the curve of the analyte, calculated from time zero to the time of the last measurable concentration.