Table 2.
GW766994X treatment condition | Tissue concentrations of GW766994 on day 29, ng/mL |
Plasma concentrations of GW766994, ng/mL |
||||||
---|---|---|---|---|---|---|---|---|
Retina, dosed eye | Retina, nondosed eye | Choroid, dosed eye | Choroid, nondosed eye | Day 8 | Day 15 | Day 22 | Day 29 | |
Bilateral injection, 10% w/v | 43,200 ± 12,100 | 109,000 ± 37,900 | 19.4 ± 7.0 | 11.1 ± 7.2 | 20.6 ± 13.5 | |||
Single-eye injection, 10% w/v | 46,600 ± 29,000 | 69.5 ± 29.5 | 91,500 ± 42,900 | 3490 ± 92.1 | 6.92 ± 1.27 | 4.72 ± 1.54 | 6.99 ± 2.82 | |
Bilateral implant, 0.1 mg | 374 ± 97.2 | 796 ± 283 | 0.232 ± 0.043 | 0.112 ± 0.020 | 0.081 ± 0.017 | 0.071 ± 0.015 | ||
Bilateral implant, 0.3 mg | 440 ± 188 | 1170 ± 524 | 0.349 ± 0.033 | 0.201 ± 0.028 | 0.164 ± 0.020 | 0.158 ± 0.020 | ||
Bilateral topical, 10 mg/mL | 295 ± 442 | 3490 ± 921 | 3.81 ± 0.886 | 2.48 ± 0.882 | 2.45 ± 0.728 | 1.71 ± 0.925 |
Intravitreal injections were administered at 5 mg/eye per dose on days 8 and 22. The implant preloaded with approximately 0.1 mg and 0.3 mg of GW766994 were intended to release approximately 0.002 and 0.010 mg per day, respectively. Both devices were implanted on day 1. Animals dosed topically were given eye drops twice daily (0.5 mg/eye per dose), with doses approximately 8 hours apart, on days 1 to 29. n = 6 eyes analyzed for each bilateral treatment, n = 3 eyes analyzed for the single-eye treatment.