TABLE 3.
PK parameters of keverprazan, M9, and vonoprazan on day 1 and day 7 upon consecutive drug administration for 7 days.
| Parameters | Keverprazan | M9 | Vonoprazan | ||
|---|---|---|---|---|---|
| 20 mg | 40 mg | 20 mg | 40 mg | 20 mg | |
| N | 8 | 8 | 8 | 8 | 4 |
| Day 1 | |||||
| t 1/2, h | 6.27 ± 1.21 | 6.52 ± 1.10 | 4.77 ± 0.798 | 5.21 ± 1.00 | 6.47 ± 1.17 |
| T max, h | 2.00 (1.25, 2.00) | 1.50 (1.00, 3.00) | 2.00 (1.50, 3.00) | 2.00 (2.00, 3.00) | 1.25 (1.25, 1.50) |
| C max, ng/mL | 28.8 ± 11.8 | 59.3 ± 31.5 | 238 ± 65.3 | 419 ± 170 | 23.2 ± 4.63 |
| AUC0–24h, h·ng/mL | 230 ± 100 | 467 ± 235 | 1462 ± 297 | 2634 ± 903 | 168 ± 21.9 |
| AUC0–∞, h·ng/mL | 249 ± 114 | 512 ± 268 | 1507 ± 302 | 2732 ± 905 | 182 ± 26.1 |
| V z/F, L | 849 ± 390 | 967 ± 707 | — | — | 1030 ± 158 |
| CL/F, L/h | 96.1 ± 45.4 | 101 ± 59.5 | — | — | 112 ± 17.4 |
| AUC0–t_M9/AUC0–t_ keverprazan | — | — | 7.76 ± 4.50 | 7.65 ± 5.89 | — |
| Day 7 | |||||
| t 1/2, h | 6.23 ± 0.776 | 7.01 ± 1.10 | 7.21 ± 0.828 | 7.32 ± 0.918 | 7.71 ± 1.70 |
| T max, h | 1.25 (1.00, 3.00) | 3.00 (1.00, 3.00) | 2.00 (1.25, 2.00) | 2.00 (1.50, 3.00) | 1.63 (1.25, 3.00) |
| C max, ng/mL | 43.1 ± 14.9 | 93.2 ± 71.2 | 232 ± 67.0 | 392 ± 163 | 27.2 ± 6.59 |
| T min, h | 10.3 ± 12.8 | 9.00 ± 12.4 | 3.43 ± 9.07 | 6.0 ± 11.1 | 6.00 ± 12.0 |
| C min, ng/mL | 2.94 ± 2.39 | 10.7 ± 13.0 | 8.80 ± 4.09 | 18.5 ± 9.60 | 1.89 ± 0.811 |
| C AVSS | 15.0 ± 7.19 | 41.6 ± 40.4 | 67.9 ± 15.3 | 121 ± 35.4 | 9.02 ± 2.20 |
| AUC0–24h, h·ng/mL | 361 ± 173 | 998 ± 971 | 1631 ± 366 | 2915 ± 850 | 216 ± 52.8 |
| AUC0–t , h·ng/mL | 390 ± 198 | 1117 ± 1116 | 1730 ± 398 | 3145 ± 905 | 239 ± 60.4 |
| AUC0–∞, h·ng/mL | 393 ± 201 | 1131 ± 1137 | 1744 ± 405 | 3175 ± 915 | 244 ± 62.4 |
| V z/F, L | 609 ± 333 | 656 ± 428 | — | — | 1056 ± 251 |
| CLss/F, L/h | 69.5 ± 39.3 | 66.3 ± 40.3 | — | — | 96.9 ± 24.8 |
| DF, % | 287 ± 56.1 | 230 ± 59.5 | 327 ± 60.3 | 302 ± 76.7 | 287 ± 68.8 |
| R AUC0–24h | 1.51 ± 0.447 | 1.94 ± 0.849 | 1.10 ± 0.104 | 1.13 ± 0.171 | 1.28 ± 0.194 |
| R Cmax | 1.51 ± 0.637 | 1.59 ± 0.684 | 0.970 ± 0.0539 | 0.935 ± 0.0917 | 1.17 ± 0.0581 |
| AUC0‐t_M9/AUC0‐t_keverprazan | — | — | 5.63 ± 3.60 | 4.99 ± 3.69 | — |
Abbreviations: AUC, area under the concentration curve; C AVSS, average value of the steady‐state concentration; CL/F, apparent total body clearance; CLss/F, oral clearance; C max, peak concentration; C min, trough concentration; DF, degree of fluctuation; R, accumulation ratio; t 1/2, elimination half‐life; T max, time to reach C max; T min, time to reach C min; V z/F, volume of distribution.