Summary statistics pharmacokinetic parameters from the SAD study
| SAD Study Panel | Participants | Cmax | Tmax | AUC0–t | AUC0–∞ | t1/2a | CLT/F |
|---|---|---|---|---|---|---|---|
| GM (CV%) | Median (Minimum–Maximum) | GM (CV%) | GM (CV%) | Mean (S.D.) | GM (CV%) | ||
| n | ng/ml | h | ng⋅h/ml | h | l/h | ||
| Panel 1 (10 mg) | 6 | 11 (50) | 3 (1.5–5) | 128 (76) | 153 (89) | 16 (15) | 66 (60) |
| Panel 2 (30 mg) | 6 | 49 (52) | 4 (3–5) | 895 (45) | 982 (5) | 19 (9) | 31 (65) |
| Panel 3 (100 mg) | 6 | 280 (42) | 4 (2–5) | 4586 (39) | 5143 (52) | 23 (9) | 19 (40) |
| Panel 4 (300 mg, fasted) | 6 | 325 (52) | 3.5 (2–5) | 8574 (46) | 8749 (48) | 20 (10) | 34 (54) |
| Panel 4 (300 mg, high-fat meal) | 6 | 721 (45) | 5 (4–12) | 19,426 (34) | 20,352 (41) | 28 (14) | 15 (31) |
| Panel 5 (600 mg famotidine) | 6 | 512 (57) | 3 (2–5) | 9750 (59) | 10,073 (63) | 23 (14) | 30 (47) |
| Panel 6 (900 mg) | 6 | 748 (32) | 4 (2–5) | 21,878 (33) | 21,440 (37) | 20 (8) | 28 (31) |
| Panel 7 (1200 mg) | 6 | 1597 (29) | 4 (3–6) | 50,104 (58) | 52,245 (56) | 22 (7) | 23 (51) |
| Panel 8 (900 mg; elderly) | 9 | 2870 (24) | 5 (3–12) | 134,138 (38) | 155,797 (43) | 63 (20) | 6 (38) |
| Panel 9 (900 mg; plasma) | 10 | 876 (42) | 4.5 (4–18) | 42,576 (26) | 439,701 (26) | 32 (21) | 20 (24) |
| Panel 9 (900 mg; CSF) | 10 | 6.5 (40) | 6 (4–18) | 97 (41) |
AUC0–t, area under the concentration-time curve from zero to the last quantifiable time; CLT/F, apparent total body clearance; GM (CV%), geometric mean and coefficient of variation.
↵a Calculated at day 25 for 200 mg in the MAD study.