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. 2015 May 19;112(12):1874–1881. doi: 10.1038/bjc.2015.144

Table 5. Pharmacokinetics of irinotecan and SN-38.

  Irinotecan
SN-38
  Day 1 (test) Day 15 (reference) Day 1 (test) Day 15 (reference)
Cmax (ngml−1)
N 10 8 10 8
Median 2070 2120 20.4 15.1
Range 1590–3060 1760–2840 11.4–37.6 9.28–37.5
Tmax (h)
N 10 8 10 8
Median 1.5 1.54 1.5 1.6
Range 1.25–2.50 1.50–2.50 1.50–2.25 1.50–2.50
AUC(0–t) (ngml−1·h)
N 10 8 10 8
Median 10500 12700 150 146
Range 7130–18500 7040–17900 35.4–380 42.5–380
AUC(0–∞) (ngml−1·h)
N 9 8 10 7
Median 10600 13600 198 206
Range 7650–20600 7330–20400 102–550 64.7–508
T1/2 (h)
N 9 8 10 7
Median 6.43 6.21 13.6 15.7
Range 5.32–7.63 5.54–8.77 7.10–21.5 4.63–34.2
CL/f (lh−1)
N 9 8    
Median 29.4 23.5 NC NC
Range 16.4–47.0 15.6–46.8    
Vz/f (l)
N 9 8    
Median 297 212 NC NC
Range 147–455 143–382    
Ratio of Cmax test/reference
N   8   8
Median   0.973   1.11
Range   0.623–1.13   0.912–2.04
Ratio of AUC(0–∞) test/reference
N   8   7
Median   0.911   0.91
Range   0.577–1.08   0.825–1.58

Abbreviations: AUC0–t=area under the concentration–time curve from time zero to the time of last observation; AUC0–∞=area under the concentration–time curve from time zero to infinity; CL/f=apparent oral clearance; Cmax=maximal concentration; NC=not calculated; t1/2=apparent half-life; Tmax=time of maximum concentration; Vz/f=apparent oral volume of distribution.

Pharmacokinetics of irinotecan and its active metabolite SN-38 following single 180 mg m−2 doses on day 1 administered concomitantly with pimasertib (test) and following single 180 mg m−2 doses on day 15 administered alone (reference).