Mean pharmacokinetic parameters on day 1 for emixustat and its major metabolites (ACU-5116, ACU-5124, and ACU-5149) in subjects with geographic atrophy
| Analyte | Cmax ± S.D. (N) | Tmax ± S.D. (N) | t1/2 ± S.D. (N) | AUC0–24 ± S.D. (N) | AUC0–∞ ± S.D. (N) | |
|---|---|---|---|---|---|---|
| ng/ml | h | h | ng⋅h/ml | ng⋅h/ml | ||
| 2.5 mg QD emixustat | ||||||
| Emixustat | 0.637 ± 0.279 (17) | 4.31 ± 1.83 (17) | 5.84 ± 1.83 (16) | 6.42 ± 3.39 (15) | 7.15 ± 3.82 (12) | |
| ACU-5116 | 5.96 ± 2.28 (17) | 2.59 ± 0.895 (17) | 5.38 ± 1.96 (17) | 46.1 ± 16.1 (10) | 50.0 ± 21.8 (8) | |
| ACU-5124 | 7.29 ± 3.89 (17) | 4.14 ± 0.956 (17) | 5.72 ± 1.84 (16) | 76.8 ± 42.2 (9) | 80.3 ± 52.7 (8) | |
| ACU-5149 | 5.68 ± 3.02 (17) | 3.72 ± 0.966 (17) | 5.44 ± 1.76 (16) | 53.1 ± 41.6 (9) | 59.0 ± 49.3 (8) | |
| 5.0 mg QD emixustat | ||||||
| Emixustat | 1.61 ± 0.832 (18) | 3.47 ± 1.91 (18) | 6.35 ± 1.05 (17) | 14.0 ± 6.15 (18) | 15.0 ± 6.96 (17) | |
| ACU-5116 | 12.0 ± 5.91 (18) | 2.24 ± 1.35 (18) | 5.78 ± 2.66 (18) | 81.4 ± 34.9 (17) | 94.2 ± 44.7 (17) | |
| ACU-5124 | 13.6 ± 6.79 (18) | 3.61 ± 1.10 (18) | 5.57 ± 1.08 (18) | 129 ± 72.8 (18) | 143 ± 79.6 (17) | |
| ACU-5149 | 11.0 ± 6.18 (18) | 3.42 ± 1.27 (18) | 5.41 ± 1.72 (18) | 101 ± 70.9 (18) | 110 ± 79.9 (17) | |
| 10.0 mg QD emixustat | ||||||
| Emixustat | 2.79 ± 1.18 (18) | 3.14 ± 1.49 (18) | 6.78 ± 1.40 (18) | 27.4 ± 12.5 (18) | 30.8 ± 15.3 (18) | |
| ACU-5116 | 23.4 ± 9.04 (18) | 2.66 ± 1.08 (18) | 6.60 ± 2.18 (18) | 168 ± 61.7 (18) | 188 ± 70.6 (16) | |
| ACU-5124 | 25.3 ± 9.84 (18) | 4.04 ± 1.14 (18) | 6.29 ± 1.36 (18 | 263 ± 122 (18) | 288 ± 133 (18) | |
| ACU-5149 | 21.1 ± 10.9 (18) | 3.87 ± 1.25 (18) | 6.12 ± 1.42 (18) | 204 ± 117 (18) | 223 ± 128 (18) |
AUC0-24, area under the plasma concentration-time curve from time 0 to 24 hours; AUC0-∞ area under the plasma concentration-time curve from time 0 to infinity; Cmax, maximum observed plasma concentration; N, number of subjects; QD, once daily; t1/2, terminal half-life; Tmax, time to reach Cmax.