Table 1.
Pharmacokinetic (PK) parameters measured in preclinical species after i.v. bolus administration of a novel phosphorothioate backbone 13-mer locked nucleic acid oligonucleotide-targeting miRNA-221 (LNA-i-miR-221).
| Species | Dose (i.v. Bolus) |
C0/Dose | AUC 1 | AUC/Dose | CL | Terminal Half-Life |
Vd Terminal |
|---|---|---|---|---|---|---|---|
| mg/kg | ng/mL/mg | (h·ng/mL) | (h·ng/mL)/mg | mL/min/kg | h | mL/Kg | |
| Rat | 12.5 | 4462 | 27192 | 2160 | 7.9 | 3.9 | 2626 |
| Mouse 2 | 25 | 82 | 3226 | 129 | 129 | 1.5 | 16443 |
| Monkey | 8.75 | 7017 | 49300 | 5634 | 3.0 | 12.8 | 3286 |
1 for mouse and rat AUC was the corresponding AUC0–∞ after a single dose; for monkey, the AUC value corresponds to AUC0–48 h after single dose. 2 mouse PK parameters here reported should be considered only as indicative.