Table II.
Parameter | G5.0-OH (29 kDa) | G6.0-OH (58 kDa) | G7.0-OH (117 kDa) | HPMA copolymer (26 kDa) | HPMA copolymer (52 kDa) | HPMA copolymer (131 kDa) |
---|---|---|---|---|---|---|
Clearance (mL/h) | ||||||
Elimination Clearance (E.CL) | 10.50 ± 1.30 | 5.00 ± 1.00 | 0.79 ± 0.21 | 7.24 ± 0.58 | 6.02 ± 0.82 | 0.17 ± 0.03 |
Renal Clearance (CLR) | 0.266 | 0.087 | 0.007 | 1.179 | 0.807 | 0.041 |
Dose normalized Exposure | ||||||
AUCplasma(0–24h) (mg.h/mg.mL) | 0.1 ± 0.01 | 0.2 ± 0.04 | 1.27 ± 0.34 | 0.14 ± 0.01 | 0.13 ± 0.02 | 5.88 ± 0.97 |
AUCtumor(0–168h) (mg.h/mg.g) | 0.48 | 0.82 | 7.99 | 0.21 | 0.23 | 3.48 |
AUCtumor/AUCplasma | 5.06 | 4.12 | 6.31 | 1.52 | 1.70 | 0.59 |
Elimination clearance and plasma exposure were computed by two-compartmental analysis with bolus input. Renal clearances were computed from urine data. Tumor AUCs were computed from area under the tumor concentration profile curve. Data is presented as mean ± standard error.