TABLE 5

Mean pharmacokinetic parameters on day 7 for emixustat and its major metabolites (ACU-5116, ACU-5124, and ACU-5149) in subjects with geographic atrophy

AnalyteCmax ± S.D. (N)Tmax ± S.D. (N)t1/2 ± S.D. (N)AUC0–t ± S.D. (N)Rac ± S.D. (N)
ng/mlhhng⋅h/ml
2.5 mg QD emixustat
 Emixustat0.739 ± 0.372 (17)3.92 ± 1.57 (17)6.98 ± 1.73 (16)7.33 ± 2.40 (14)1.20 ± 0.152 (12)
 ACU-51167.34 ± 3.4 (17)2.15 ± 0.949 (17)6.00 ± 3.26 (17)40.8 ± 21.7 (17)1.17 ± 0.237 (8)
 ACU-51247.41 ± 3.47 (17)4.00 ± 1.50 (17)5.89 ± 2.46 (15)62.1 ± 44.6 (17)1.09 ± 0.137 (6)
 ACU-51495.93 ± 3.77 (17)3.35 ± 1.32 (17)5.94 ± 2.09 (15)49.2 ± 43.5 (17)1.27 ± 0.392 (5)
5.0 mg QD emixustat
 Emixustat1.69 ± 0.745 (18)3.81 ± 1.41 (18)7.04 ± 1.23 (18)16.5 ± 7.55 (18)1.19 ± 0.225 (18)
 ACU-511614.23 ± 6.23 (18)2.17 ± 2.15 (18)6.78 ± 2.85 (18)91.4 ± 45.2 (18)1.31 ± 0.337 (16)
 ACU-512416.1 ± 8.96 (18)3.97 ± 1.46 (18)6.95 ± 1.82 (17)159 ± 91.0 (18)1.24 ± 0.169 (18)
 ACU-514912.6 ± 6.85 (18)3.39 ± 1.64 (18)6.36 ± 2.01 (17)116 ± 83.0 (18)1.23 ± 0.298 (17)
10.0 mg QD emixustat
 Emixustat3.48 ± 1.81 (18)3.09 ± 1.32 (18)7.05 ± 2.83 (18)32.4 ± 17.7 (18)1.17 ± 0.277 (18)
 ACU-511629.6 ± 13.o (18)2.32 ± 1.58 (18)6.90 ± 2.90 (17)209 ± 100 (18)1.27 ± 0.315 (18)
 ACU-512432.2 ± 16.6 (18)4.03 ± 1.04 (18)6.70 ± 1.64 (17)332 ± 189 (18)1.29 ± 0.176 (17)
 ACU-514923.5 ± 12.8 (18)3.75 ± 1.72 (18)6.25 ± 1.72 (17)239 ± 146 (18)1.17 ± 0.230 (18)
  • AUC0-t, area under the plasma concentration-time curve from time 0 to the last measurable plasma concentration; Cmax, maximum observed plasma concentration; N, number of subjects; QD, once daily; Rac, accumulation ratio (calculated based upon AUC0-∞ for emixustat and AUC0-24 for metabolites); t1/2, terminal half-life; Tmax, time to reach Cmax.