TABLE 1.
Pharmacokinetic parameters for single-dose administration of ensitrelvir (part 1; cohorts A–E, and J) in the fasted statea
| Parameters | Ensitrelvir (cohort/dose) |
|||||
|---|---|---|---|---|---|---|
| A/20 mg | B/70 mg | C/250 mg | D/500 mg | E/1000 mg | J/2000 mg | |
| n | 6 | 6 | 8 | 6 | 6 | 6 |
| Cmax (μg/mL) | 1.70 (15.0) | 5.20 (18.5) | 15.2 (23.6) | 32.6 (19.0) | 63.8 (39.1) | 96.9 (16.5) |
| Tmax (h) | 2.50 (1.00, 4.00) |
1.50 (1.00, 4.00) |
2.50 (1.00, 12.00) |
2.00 (1.00, 4.00) |
2.75 (1.00, 6.00) |
4.00 (1.50, 8.00) |
| AUC0-last (μg·h/mL) | 82.00 (19.5) | 289.1 (15.4) | 906.8 (15.8) | 1975 (15.9) | 3,341 (35.2) | 6,311 (22.0) |
| AUC0-inf (μg·h/mL) | 91.44 (24.3) | 291.0 (15.7) | 913.7 (16.2) | 1987 (16.1) | 3,370 (35.5) | 6,346 (22.2) |
| t1/2,z (h) | 42.6 (18.6) | 45.7 (11.9) | 43.1 (20.2) | 42.2 (14.6) | 48.1 (11.3) | 43.1 (15.6) |
| MRT (h) | 61.8 (18.7) | 67.3 (13.4) | 73.4 (12.7) | 68.2 (9.0) | 70.3 (9.3) | 67.4 (8.4) |
| CL/F (L/h) | 0.219 (24.3) | 0.241 (15.7) | 0.274 (16.2) | 0.252 (16.1) | 0.297 (35.5) | 0.315 (22.2) |
| Vz/F (L) | 13.5 (10.2) | 15.9 (9.0) | 17.0 (8.8) | 15.3 (13.5) | 20.6 (26.2) | 19.6 (21.7) |
| Feu0-144 (%) | 12.9 (14.6) | 14.7 (27.4) | 16.0 (16.6) | 21.8 (15.4) | 19.4 (29.5) | NA |
| CLR (L/h) | 0.0314 (25.0) | 0.0401 (34.9) | 0.0507 (21.2) | 0.0624 (15.4) | 0.0668 (24.7) | NA |
a
Geometric means (percentage coefficient of variation) are presented, except for Tmax, for which medians (minimum, maximum) are presented. NA, not applicable.