Table 6.
Results of Phase I pharmacokinetic study and toxicity of HPMA-PTX in cancer patients [12].
| Pharmacokinetics of HPMA-PTX | |||||
|---|---|---|---|---|---|
|
| |||||
| Pharmacokinetics of total paclitaxelb | |||||
|
| |||||
| Dose (mg/m2)a | N | AUC(h·μM) | Cmax(μM) | t1/2 (h) | CLtotal (L/h) |
| 80 | 3 | 318 ± 99 | 40.1 ± 5.1 | 6.5 ± 0.3 | 0.54 ± 0.22 |
| 100 | 3 | 268 ± 56 | 44.1 ± 10.1 | 5.7 ± 0.6 | 0.87 ± 0.21 |
| 140 | 3 | 413 ± 107 | 61.2 ± 9.3 | 6.5 ± 0.7 | 0.76 ± 0.19 |
| 196 | 3 | 450 ± 19 | 74.9 ± 4.3 | 6.6 ± 0.8 | 0.84 ± 0.96 |
| Toxicity of HPMA-PTX | |||||
|---|---|---|---|---|---|
|
| |||||
| Dose (mg/m2)a | N | Grade 3 or greater | |||
|
| |||||
| Hematological toxicities | Neuromuscular toxicities | ||||
|
| |||||
| Anemiac | Neutropenia | granulo-cytopeniad | Peripheral neuropathy | ||
| 80 | 3 | 0 | 0 | 0 | 0 |
| 100 | 3 | 1 | 0 | 0 | 0 |
| 140 | 3 | 0 | 0 | 0 | 0 |
| 196 | 3 | 0 | 0 | 0 | 1 |
a
As paclitaxel equivalents.
b
Pharmacokinetics of polymer-drug micelles was determined during the first course.
c
One more patient experienced anemia grade 3, but dose not specified.
d
One patient experienced granulocytopenia grade 3, but dose not specified.