Table S2.
Amount of uric acid, xanthine, and hypoxanthine excreted in urine
| Ae (mg) | Uric acid
|
Xanthine
|
Hypoxanthine
|
||||||
|---|---|---|---|---|---|---|---|---|---|
| Baseline | Day 1 (Day 8*) |
Day 7 | Baseline | Day 1 (Day 8*) |
Day 7 | Baseline | Day 1 (Day 8*) |
Day 7 | |
| SAD study | |||||||||
| 10 mg (n=6) | 592.1 (119.3) | 498.3 (103.7) | – | 9.4 (2.8) | 68.8 (9.0) | – | 9.0 (4.4) | 24.6 (10.1) | – |
| 25 mg (n=6) | 548.8 (111.5) | 536.7 (43.2) | – | 6.8 (0.9) | 86.1 (9.7) | – | 7.5 (1.8) | 28.7 (3.3) | – |
| 50 mg (n=8) | 611.6 (75.9) | 466.3 (47.8) | – | 8.2 (1.4) | 106.5 (14.7) | – | 8.5 (1.6) | 27.7 (6.2) | – |
| 100 mg (n=8) | 522.1 (112.1) | 436.3 (52.4) | – | 6.4 (2.2) | 134.1 (28.8) | – | 7.0 (2.0) | 36.6 (8.6) | – |
| 200 mg (n=8) (fasting) | 710.1 (91.3) | 552.8 (108.6) | – | 8.0 (1.8) | 174.0 (28.6) | – | 14.0 (4.1) | 58.7 (17.3) | – |
| 200 mg (n=8) (fed)* | – | 574.3 (64.9) | – | 148.3 (41.6) | – | 38.3 (12.4) | |||
| 400 mg (n=8) | 716.5 (204.1) | 563.8 (92.7) | – | 8.6 (2.5) | 247.9 (52.1) | – | 9.5 (2.4) | 67.0 (39.9) | – |
| 600 mg (n=8) | 563.3 (83.6) | 511. 9 (88.8) | – | 7.2 (2.0) | 197.6 (45.6) | – | 8.6 (2.5) | 40.5 (6.8) | – |
| Placebo (n=14) | 652.5 (163.0) | 653.8 (153.3) | – | 9.3 (2.0) | 7.9 (2.1) | – | 10.3 (3.7) | 10.6 (4.3) | – |
| MAD study | |||||||||
| 100 mg (n=8) | 526.5 (109.0) | 410.8 (75.3) | 187.7 (45.8) | 7.7 (1.7) | 124.0 (28.6) | 129.0 (27.3) | 8.7 (1.8) | 31.8 (7.5) | 36.5 (9.6) |
| 200 mg (n=8) | 529.7 (93.1) | 421.4 (62.9) | 124.2 (15.1) | 8.1 (2.4) | 189.0 (36.6) | 258.8 (41.6) | 8.4 (1.7) | 34.2 (6.0) | 59.6 (15.3) |
| 400 mg (n=8) | 536.9 (106.5) | 490.0 (48.3) | 99.8 (20.1) | 7.6 (1.9) | 175.5 (17.0) | 247.6 (45.2) | 9.9 (1.9) | 52.9 (11.1) | 61.8 (15.5) |
| 600 mg (n=8) | 439.5 (154.6) | 570.3 (282.2) | 79.7 (26.2) | 8.9 (10.5) | 167.1 (37.3) | 242.4 (36.2) | 8.1 (6.2) | 351. (8.2) | 49.1 (13.5) |
| 800 mg (n=6) | 510.7 (204.0) | 652.9 (134.0) | 60.7 (8.6) | 5.0 (1.8) | 182.3 (36.1) | 318.6 (86.2) | 6.2 (1.6) | 27.5 (3.8) | 61.7 (15.5) |
| Febuxostat 80 mg (n=8) | 472.6 (95.8) | 417.8 (59.9) | 182.6 (53.4) | 6.3 (2.0) | 140.0 (29.8) | 193.0 (25.6) | 8.1 (2.9) | 40.2 (18.1) | 54.3 (25.8) |
| Placebo (n=10) | 546.8 (82.8) | 602.5 (100.8) | 582.9 (108.9) | 6.7 (1.6) | 6.9 (1.6) | 6.9 (1.4) | 8.1 (2.8) | 8.9 (3.0) | 8.7 (2.6) |
Notes: All values are presented as mean (SD).
*
Data of 200 mg dose group under fed condition.
Abbreviations: Ae, cumulative amount excreted in the urine for 24 h; SAD, single ascending dose; MAD, multiple ascending dose; SD, standard deviation.