Pharmacokinetic and toxicokinetic summary of AZ’0908

DoseNo. of AnimalsAnticipated AUCtherDay 1Day 14
Cmax ParentAUC0–24 ParentCmax M1AUC0–24 M1AUC0–24 M1/AUC0–24 Parent (ratio)AUC0–24 Parent/DoseCmax ParentAUC0–24 ParentAUC0–24 Parent/AUCther (ratio)AUC0–24 Parent/Dose
10 μmol/kg311811580.6110.25.8NANANANA
435 μmol/kg51183752220NANANA5.14152520215.8
900 μmol/kg51185405030NANANA5.64805000425.6
  • AUC0–24, area under the curve for 24 hours; AUCther, area under plasma concentration time curve needed for therapeutic effect; NA, not available.

  • a AUCther was based on the assumption that a steady-state concentration (Css) average corresponding to 10 times the AZ’0908 whole blood assay IC50 values was needed.