Table 3.
RDI-OTtumor pharmacokinetic parameters for CMA and SM agents
| Agent | RDI-OTtumor AUC0-lasta | (SM RDI-OTtumor AUC0-last)/(CMA RDI-OTtumor AUC0-last) | RDI-OTtumor AUC0-6 ha | (SM RDI-OTtumor AUC0-6 h)/(CMA RDI-OTtumor AUC0-6 h) |
|---|---|---|---|---|
| CMA | ||||
| SPI-077 | 131.3 | 0.02 | 0.02 | 98.7 |
| S CKD-602 | 18.6 | 2.1 | 0.04 | 149.3 |
| XMT-1001 | 6,488.0 | 0.03 | 0.1 | 76.1 |
| PRINT docetaxel 200X200 nm | 24,010.9 | 0.5 | 2.4 | 59.2 |
| PRINT docetaxel 80X320 nm | 7,152.7 | 1.6 | 2.5 | 55.8 |
| CS0201 | 1,131.3 | 1.3 | 0.2 | 59.5 |
| Folate-CS0201 | 2,860.5 | 0.5 | 0.2 | 63.6 |
| IHL-305 | 3.0 | 1.5 | 0.1 | 63.8 |
| BTM-docetaxel | 109.9 | 0.2 | 0.3 | 26.7 |
| BTM-paclitaxel | 1,268.2 | 2.6 | 0.1 | 129.9 |
| NK012 | 741,095.9 | 9.3 × 10−5 | 0.1 | 87.3 |
| SP1049C | 767.9 | 0.8 | 5.2 | 2.8 |
| ENZ-2208 | 368.5 | 2.2 × 10−3 | 0.3 | 3.1 |
| PLD | 273.8 | 1.3 | N/A | N/A |
| Liposomal daunorubicin | 414.7 | 13.4 | 0.8 | 45.4 |
| Liposomal doxorubicin | 791.9 | 0.1 | 1.0 | 12.5 |
| OSI-211 | 31.3 | 2.0 | 0.5 | 45.5 |
| Mean ± SD | 46,289.3 ± 179,143.8 | 1.7 ± 3.1 | 0.87 ± 1.40b | 61.2 ± 41.4 |
| Median (Range) | 767.9 (3.0-741,095.9) | 0.9 (0.00009-13.4) | 0.25 (0.02-5.2) | 59.4 (2.8-149.3) |
| SM | ||||
| Cisplatin (SPI-077) | 2.3 | 2.3 | ||
| CKD-602 (S CKD-602) | 39.0 | 6.6 | ||
| CPT-11 (XMT-1001) | 219.4 | 11.1 | ||
| Docetaxel (PRINT docetaxel | 11,057.7 | 141.9 | ||
| 200 × 200 nm/80 × 320 nm) | ||||
| Cisplatin (CS0201/folate-CS0201) | 1,443.1 | 11.0 | ||
| CPT-11 (IHL-305) | 4.5 | 4.5 | ||
| Docetaxel (BTM-docetaxel) | 22.5 | 6.7 | ||
| Paclitaxel (BTM-paclitaxel) | 3,292.0 | 11.3 | ||
| SN-38 (NK012) | 68.9 | 9.3 | ||
| Doxorubicin (SP1049C) | 628.2 | 14.5 | ||
| SN-38 (ENZ-2208) | 0.8 | 0.8 | ||
| Doxorubicin (PLD) | 366.5 | N/A | ||
| Daunorubicin (liposomal daunorubicin) | 5,568.4 | 34.9 | ||
| Doxorubicin (liposomal doxorubicin) | 700.0 | 12.9 | ||
| Lurtotecan (OSI-211) | 61.6 | 24.0 | ||
| Mean ± SD | 1,565.0 ± 3,053.6 | 20.8 ± 36.0 | ||
| Median (Range) | 144.1 (0.8-11,057.7) | 11.1 (0.8-141.9) |
All SM docetaxel is Taxotere®. SM paclitaxel is Taxol®. Liposomal daunorubicin is DaunoXome®. Liposomal doxorubicin is Myocet®
PLD pegylated liposomal doxorubicin, SM small molecule, CMA carrier mediated agent, SD standard deviation, RDI-OTtumot AUC0-last area under the tumor relative distribution index-over time versus time curve from 0 h to last pharmacokinetic time point, RDI-OTtumor AUC0-6 h area under the tumor relative distribution index-over time versus time curve from 0 to 6 h
a
Units: (ng*g−1/ng*mL−1)*h
b
Different from SM (P < 0.05)