TABLE 1.
Parameter and garenoxacin dose (mg) | Result fora:
|
||
---|---|---|---|
Day 1 | Day 7 | Day 14 | |
Cmax, μg/ml [geometric mean (% CV)] | |||
100 | 1.2 (23.2) | 1.5 (23.1) | 1.6 (37.0) |
200 | 2.4 (15.2) | 2.9 (15.9) | 3.0 (9.2) |
400 | 4.6 (14.8) | 5.2 (15.8) | 5.6 (17.6) |
800 | 9.5 (12.8) | 12.6 (32.2) | 14.4 (40.4) |
1,200 | 16.3 (31.8) | 21.5 (37.9) | 24.0 (34.8) |
AUC∞, μg/ml [geometric mean (% CV)] | |||
100 | 15.1 (24.4) | N/Ad | N/A |
200 | 29.6 (20.4) | N/A | N/A |
400 | 55.2 (18.5) | N/A | N/A |
800 | 130.3 (16.5) | N/A | N/A |
1,200 | 230.0 (33.1) | N/A | N/A |
AUGτ,b μg/ml [geometric mean (% CV)] | |||
100 | 11.5 (21.3) | 15.6 (18.6) | 15.7 (20.5) |
200 | 23.3 (19.0) | 31.0 (17.6) | 32.7 (17.3) |
400 | 45.2 (15.6) | 58.5 (23.1) | 58.6 (19.9) |
800 | 100.7 (10.7) | 157.9 (44.5) | 180.8 (48.8) |
1,200 | 179.8 (30.0) | 271.0 (36.5) | 307.3 (31.2) |
t1/2, h [mean (SD)] | |||
100 | N/A | N/A | 17.8 (3.3) |
200 | N/A | N/A | 15.5 (4.4) |
400 | N/A | N/A | 13.3 (2.2) |
800 | N/A | N/A | 15.5 (4.0) |
1,200 | N/A | N/A | 15.4 (3.4) |
Tmax, h [median (minimum to maximum)] | |||
100 | 1.25 (0.75-2.00) | 1.13 (0.75-4.00) | 1.13 (0.50-4.00) |
200 | 1.75 (1.00-2.00) | 1.50 (1.00-3.00) | 1.75 (1.00-2.00) |
400 | 1.75 (0.75-2.00) | 1.25 (0.50-1.50) | 1.50 (0.75-2.00) |
800 | 1.75 (1.00-4.00) | 1.50 (0.75-3.00) | 2.50 (1.50-4.00) |
1,200 | 2.50 (2.00-4.00) | 2.50 (1.50-4.00) | 2.00 (1.50-4.00) |
MRT, h [mean (SD)] | |||
100 | 16.9 (3.0) | 18.8 (5.1) | 19.4 (2.8) |
200 | 15.6 (2.4) | 16.0 (5.1) | 18.2 (3.5) |
400 | 13.9 (1.1) | 15.6 (1.7) | 17.1 (1.8) |
800 | 16.0 (2.7) | 20.0 (5.7) | 21.2 (5.5) |
1,200 | 16.0 (2.9) | 17.3 (2.2) | 20.4 (2.7) |
% UR [mean (SD)] | |||
100 | 37.3 (8.3) | 50.7 (9.0) | 52.0 (19.7)c |
200 | 28.0 (6.4) | 44.4 (6.0) | 44.3 (13.1) |
400 | 23.2 (7.7) | 37.6 (9.8) | 43.6 (3.2) |
800 | 21.1 (3.5)c | 36.6 (9.1) | 33.1 (6.0) |
1,200 | 25.4 (2.8) | 36.5 (4.1) | 40.9 (3.6) |
CLR, ml/min [mean (SD)] | |||
100 | 56.1 (19.9) | 55.2 (15.2) | 55.7 (11.7) |
200 | 40.6 (11.5) | 48.4 (11.5) | 46.9 (18.5) |
400 | 34.9 (13.2) | 44.6 (17.1) | 50.4 (11.0) |
800 | 27.0 (5.6) | 33.3 (17.8) | 25.6 (10.0) |
1,200 | 29.4 (10.1) | 28.0 (8.5) | 27.5 (8.2) |
n = 6 for all groups but the 400-mg dose group.
AUCτ is 24 h.
n = 5.
N/A, not applicable.