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. 2015 Oct 13;15:685. doi: 10.1186/s12885-015-1672-4

Table 1.

Plasma and Brain Tumor Concentrations after Administration of Irinotecan or NKTR-102

Treatment NKTR-102 Conventional Irinotecan
Time (hr) 6 24 72 168 2 6 12 24
Irinotecan Equivalent Concentration ± SEM (ng/mL or ng/g) Irinotecan Concentration ± SEM (ng/mL or ng/g)
Plasma 72450 ± 48790 210 ± 126 14 ± 7.5 5.0 ± 0.09 1100 ± 306 2.9 ± 1.4 0.7 ± 0.3 2.3 ± 1.8
Tumor 3200 ± 3700 2572 ± 1323 1207 ± 904 833 ± 240 554 ± 667 7.7 ± 5.8 2.8 ± 1.2 7.4 ± 5.2
Tumor/Plasma 0.4 12 80 170 0.5 2.7 3 4
SN38 Concentration ± SEM (ng/mL or ng/g)
Plasma 63 ± 50 34 ± 13 2.2 ± 1.4 0.65 ± 0.08 36 ± 12 2.4 ± 1.3 0.7 ± 0.1 0.4 ± 0.4
Tumor 13 ± 16 208 ± 126 60 ± 78 23 ± 28 29 ± 46 0.8 ± 0.4 0.6 ± 0.4 1.1 ± 1.1
Tumor/Plasma 0.2 6 27 31 0.8 0.3 0.9 2.8

Plasma and brain tumor concentrations for parent drug and active metabolite SN38 after a 50 mg/kg IV bolus injection of either NKTR-102 or irinotecan to NU/NU mice with established, orthotopic MDA-MB-231Br brain tumors. Results are expressed as mean ± SEM (N = 5 per time point)