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Table 4 Pharmacokinetic parameters of PEP02 at each dose level

From: A phase I dose-escalation study of PEP02 (irinotecan liposome injection) in combination with 5-fluorouracil and leucovorin in advanced solid tumors

  Dose of PEP02
(mg/m2)
C max
CPT-11
(μg/mL)
SN-38
(ng/mL)
T max
(hr)
AUC0→169.5
CPT-11
(hr-μg/mL)
SN-38
(hr-ng/mL)
AUC0→∞
CPT-11
(hr-μg/mL)
SN-38
(hr-ng/mL)
V ss
(L/m2)
Cl
(mL/hr/m2)
t 1/2
(hr)
Total CPT-11 60, N = 3 28.9 ± 15.8 2.4 ± 0.7 1047 ± 1210 1047 ± 1210 2.80 ± 1.59 136 ± 116 21.1 ± 11.7
80, N = 6 29.2 ± 5.2 2.1 ± 0.7 1096 ± 834 1151 ± 880 3.39 ± 0.74 124 ± 106 33.3 ± 15.1
100, N = 5 44.1 ± 7.7 4.0 ± 3.8 2237 ± 1090 2289 ± 1119 2.86 ± 0.75 58 ± 37 43.17 ± 4.8
120, N = 2 47.9 ± 16.2 2.3 ± 0.9 1254 ± 553 1254 ± 553 3.95 ± 0.83 106 ± 47 54.4 ± 17.4
SN-38 60, N = 3 7.02 ± 5.64 13.1 ± 11.7 364 ± 222 1370 ± 1122 NA NA 183.8 ± 172.3
80, N = 6 7.98 ± 4.39 13.3 ± 18.3 343 ± 133 505 ± 165 NA NA 57.5 ± 17.8
100, N = 5 7.39 ± 1.68 12.2 ± 12.3 539 ± 368 840 ± 433 NA NA 73.4 ± 18.3
120, N = 2 7.26 ± 3.90 37.8 ± 17.2 353 ± 164 305 NA NA 30.8
  Irinotecana 26.3 ± 11.9 NA 229 ± 108 NA NA NA 10.4 ± 3.1
  1. Mean ± STD; C max , peak concentration in plasma; T max , time to achieve peak plasma concentration; AUC0→169.5 and AUC0→∞, area under the plasma concentration-time curve from time zero to 169.5 h and infinity, respectively; V ss , volume of distribution at steady state; t 1/2 , plasma terminal elimination half-life; Cl, total clearance of drug from plasma; NA, not available
  2. aIrinotecan 125 mg/m2, package inset of Campto®