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Table 5 PR-104 and PR-104A plasma pharmacokinetic parameters for cycle 1 day 1

From: A phase I trial of PR-104, a pre-prodrug of the bioreductive prodrug PR-104A, given weekly to solid tumour patients

    Cmax(μM) AUC (μM.h) t1/2(h) Cl (L/h/m2) Vdss(L/m2)
Dose-level (mg/m2)   n PR-104 PR-104A PR-104 PR-104A PR-104 PR-104A PR-104 PR-104
135   2 4.08 3.49 2.85 3.22 0.06 0.34 128 38.7
270   6 7.63 (3.13) 6.81 (2.15) 4.15 (1.69) 6.61 (2.88) 0.07 (0.05) 0.42 (0.16) 129 (49.4) 39.1 (9.83)
540   6 14.2 (6.51) 13.7 (2.94) 9.34 (4.17) 14.0 (2.70) 0.07 (0.03) 0.42 (0.16) 130 (119) 44.7 (38.5)
675   7 18.1 (9.9) 15.5 (6.1) 12.9 (7.0) 17.7 (5.6) 0.14 (0.10) 0.55 (0.11) 92.7 (52.2) 27.3 (14.4)
900   4 20.8 (5.71) 23.3 (4.64) 15.2 (4.97) 29.5 (8.44) 0.15 (0.10) 0.68 (0.14) 64.8 (22.9) 24.2 (10.5)
  1. Values are the mean (SD)