Table 1.
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)