Table 3.
Pharmacokinetics of topically delivered TG100801 in rabbits
| Tissue | Concentration (nM) | Ratio TG100801: TG100572 |
||
|---|---|---|---|---|
| TG100801 | TG100572 | Sum | ||
| Conjunctiva | 609 | 3,980 | 4,589 | 1:6.5 |
| Cornea | 38 | 3,280 | 3,318 | 1:86 |
| Aqueous humor | 0.5 | 0 | 0.5 | NA |
| Iris | 9 | 45 | 54 | 1:5 |
| Ciliary Body | 65 | 73 | 138 | 1:1.1 |
| Lens | <LOD | <LOD | NA | NA |
| Sclera | 100 | 249 | 349 | 1:2.5 |
| Choroid | 34 | 169 | 203 | 1:5 |
| Retina | 46 | 41 | 87 | 1:0.9 |
| Vitreous humor | 11 | 11 | 22 | 1:1 |
| Plasma | <LOD | <LOD | NA | NA |
Dutch Belted rabbits were dosed topically with a single 40 µL drop of 0.6% TG100801 and 2 hours later they were euthanized and ocular tissues were dissected and homogenized. Mass spectroscopy was used to measure the concentrations of TG100801, TG100572, or both (sum) in tissue homogenates. Assay level of detection (LOD) was 1 ng/mL (<2 nM). NA: not applicable.