TABLE 2

Pharmacokinetic parameters of total radioactivity, emvododstat, and its metabolites in pooled plasma following oral administration of 14C-emvododstat in healthy male human subjects

DayDoseComponentTmax (h)T1/2 (h)Tlast (h)Cmax
(µg eq/mL)
AUC0–24
(µg eq·h/mL)
AUC0–240
(µg eq·h/mL)
% AUCa of TRA
616 mg/0.3 µCibTRA6NC240.305.08NA100
EmvododstatNANANANA2.59NA51.0
O-Desmethyl emvododstatNANANANA0.49NA9.6
M298NANANANA0.11NA2.2
M443NANANANA0.72NA14.1
M474NANANANA0.17NA3.4
O-Desmethyl emvododstat glucuronideNANANANA0.59NA11.7
716 mg/100 µCicTRA6NC2400.182.416.92100
Emvododstat3792400.141.582.4635.6
O-Desmethyl emvododstat6431440.0160.250.608.61
M298240NC2400.002NC0.324.66
M312240NC2400.001NC0.304.31
M443144NC2400.0050.061.0415.0
M474240NC2400.0040.020.517.41
O-Desmethyl emvododstat glucuronide6582400.0250.330.8111.7
  • AUC0–24, area under the plasma concentration-time curve from time zero to 24 hours postdose; AUC0–240, area under the plasma concentration-time curve from time zero to 240 hours postdose; NA, not applicable; NC, not calculable.

  • aAUC0–24 TRA for Day 6 and AUC0–240 TRA for Day 7.

  • bRepeat once-daily oral dosing of 16 mg/0.3 µCi or 11.1 kBq 14C-emvododstat for 6 days.

  • cSingle oral 16 mg/100 µCi or 3.7 MBq 14C-emvododstat dose on Day 7, which was preceded by repeat once-daily oral dosing of 16 mg/0.3 µCi or 11.1 kBq 14C-emvododstat for 6 days.