TABLE 2

Pharmacokinetic parameters of PR-104 metabolites in mouse and human plasma after intravenous administration of 975 mg/m2 (bolus) and 1100 mg/m2 (60-min infusion), respectively

MouseHuman*
AUC0-inft1/2AUC0-inft1/2
μmol-h/lminμmol-h/lmin
PR-10480.73.419.0 (1.6)7.1 (1.0)
PR-104A81.616.834.9 (4.2)39.7 (1.4)
PR-104H (M22)3.023.91.75 (0.2)41.5 (3.3)
PR-104M (M23)10.220.50.29 (0.04)60.6 (5.5)
PR-104S1 (M8)19.324.70.78 (0.17)53.0 (4.5)
PR-104G (M1)2.713.144.6 (16.2)35.3 (2.1)
  • * The PK for PR-104 and PR-104A are in good agreement with the values reported elsewhere (Jameson et al., 2009), for 6 of the same 10 subjects, using a different analytical method.