Table 4.
Tissue RDI-OT pharmacokinetic parameters for CMA and SM agents
| Agent | RDI-OTliver AUC0-lasta | RDI-OTliver AUC0-6 ha | RDI-OTspleen AUC0-6 ha | RDI-OTspleen AUC0-6 ha |
|---|---|---|---|---|
| CMA | ||||
| SPI-077 | 392.9 | 0.1 | 1,117.7 | 0.1 |
| S CKD-602 | 11.62 | 0.4 | 46.1 | 0.3 |
| XMT-1001 | 26,188 | 1.0 | 14,915.0 | 0.4 |
| PRINT docetaxel 200X200 | 11,917.6 | 3.0 | 112,966.7 | 21.9 |
| PRINT docetaxel 80X320 | 526.5 | 1.6 | 2,292.0 | 9.8 |
| CS0201 | 488 | 0.6 | 3,428.0 | 0.7 |
| Folate-CS0201 | 5,707 | 1.4 | 4,130.0 | 0.8 |
| IHL-305 | 4.5 | 0.3 | 9.3 | 0.4 |
| BTM-docetaxel | 906.9 | 13.3 | 303.7 | 6.3 |
| BTM-paclitaxel | 42,118.5 | 1.2 | 56,669.6 | 1.4 |
| NK012 | 2,833,721.1 | 0.9 | 5,152,753.6 | 0.7 |
| SP1049C | 1,167.2 | 50.0 | N/A | N/A |
| ENZ-2208 | N/A | N/A | N/A | N/A |
| PLD | 367.0 | N/A | N/A | N/A |
| Liposomal daunorubicin | N/A | N/A | N/A | N/A |
| Liposomal doxorubicin | N/A | N/A | N/A | N/A |
| OSI-211 | 38.4 | 1.8 | 204.2 | 2.5 |
| Mean ± SD | 208,825.4 ± 755,599.6 | 5.8 ± 13.7b | 445,736.3 ± 1,482,716.5 | 3.8 ± 6.43b |
| Median (Range) | 1,416,862.8 (4.5-2,833,721.1) | 1.2 (0.1-50.0) | 2,860.0 (9.3-5,152,753.6) | 0.75 (0.1-21.9) |
| SM | ||||
| Cisplatin (SPI-077) | 8.9 | 9.0 | 1.7 | 1.7 |
| CKD-602 (S CKD-602) | 96.0 | 40.0 | 22.1 | 10.6 |
| CPT-11 (XMT-1001) | 490.6 | 68.8 | 917.7 | 83.0 |
| Docetaxel (PRINT docetaxel 200 × 200 nm/80 × 320 nm) | 127.8 | 22.4 | 186.2 | 42.0 |
| Cisplatin (CS0201/folate-CS0201) | 2,743.0 | 17.0 | 647.0 | 2.1 |
| CPT-11 (IHL-305) | 14.4 | 28.4 | 27.7 | 34.5 |
| Docetaxel (BTM-docetaxel) | 83.3 | 39.0 | 535.7 | 201.5 |
| Paclitaxel (BTM-paclitaxel) | 2,240.0 | 42.4 | 969.8 | 9.3 |
| SN-38 (NK012) | 107.9 | 26.1 | 10.3 | 2.2 |
| Doxorubicin (SP1049C) | 1,534.7 | 72.5 | N/A | N/A |
| SN-38 (ENZ-2208) | N/A | N/A | N/A | N/A |
| Doxorubicin (PLD) | 409.8 | N/A | N/A | N/A |
| Daunorubicin (liposomal doxorubicin) | N/A | N/A | N/A | N/A |
| Doxorubicin (liposomal doxorubicin) | N/A | N/A | N/A | N/A |
| Lurtotecan (OSI-211) | 271.0 | 85.4 | 230.6 | 100.4 |
| Mean ± SD | 677.3 ± 949.6 | 41 ± 24.6 | 354.9 ± 382.7 | 48.73 ± 64.1 |
| Median (Range) | 199.4 (8.9-2,743.0) | 39 (9.0-85.4) | 208.4 (1.7-969.8) | 22.6 (1.7-201.5) |
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-OTtumor 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)