Table 3.
Mean maraviroc pharmacokinetics for 12-day multiple-dose study (study 2)
| Maraviroc dose | Day (n) | AUCτ*,† (ng ml−1 h) Mean (CV%) | AUC* (ng ml−1 h) Mean (CV%) | Cmax* (ng ml−1) Mean (CV%) | Tmax‡ (h) Mean (SD) | t1/2‡ (h) Mean (SD) |
|---|---|---|---|---|---|---|
| 3 mg b.i.d. | 1 (5) | nc | nc | 0.67 (52) | 0.9 (0.4) | nc |
| 7 (5) | 6.6 (32) | nc | 1.32 (31) | 1.1 (0.2) | nc | |
| 12 (4) | 4.2 (69) | nc | 0.83 (35) | 0.6 (0.3) | nc | |
| 10 mg b.i.d. | 1 (5) | 11.8 (33) | nc | 2.26 (37) | 1.8 (1.4) | nc |
| 7 (5) | 19.0 (25) | nc | 2.71 (35) | 1.9 (2.3) | nc | |
| 12 (5) | 22.2 (24) | 44.8 (8.6) | 3.33 (41) | 1.3 (1.5) | 15.2 (3.1) | |
| 25 mg b.i.d. | 1 (9)§ | 46.1 (51) | 74.6 (50) | 8.72 (62) | 3.3 (2.3) | 10.8 (2.7) |
| 7 (8) | 92.0 (47) | nc | 18.6 (51) | 3.1 (1.7) | nc | |
| 12 (8)§ | 98.6 (49) | 236 (35) | 16.2 (48) | 3.3 (2.1) | 13.9 (2.2) | |
| 100 mg b.i.d. | 1 (9) | 512 (21) | 579 (21) | 187 (43) | 2.2 (0.9) | 7.76 (0.57) |
| 7 (9) | 636 (26) | nc | 159 (42) | 2.5 (1.4) | nc | |
| 12 (9) | 686 (24) | 1018 (23) | 181 (30) | 2.5 (1.9) | 18.5 (2.5) | |
| 300 mg b.i.d. | 1 (9) | 2157 (47) | 2422 (46) | 538 (46) | 1.6 (1.4) | 8.63 (2.2) |
| 7 (9) | 2641 (43) | nc | 674 (47) | 1.5 (1.3) | nc | |
| 12 (9) | 3609 (32) | 4561 (31) | 854 (32) | 2.6 (1.5) | 16.4 (2.3) | |
| 600 mg q,d, (cohort 3) | 1 (9) | 5877 (20) | 6074 (20) | 1317 (38) | 3.3 (0.9) | 7.74 (0.99) |
| 7 (9) | 6982 (27) | 7650 (26) | 1351 (38) | 2.6 (1.3) | 15.3 (2.2) | |
| 12 (0) | – | – | – | – | – | |
| 600 mg q.d. (cohort 5) | 1 (9) | 5545 (23) | 5717(22) | 1322 (41) | 2.1 (1.4) | 7.84 (1.4) |
| 7 (9) | nc | nc | 1204 (45) | 2.8 (1.8) | nc | |
| 12 (9) | 6440 (12) | 7177 (13) | 1361 (20) | 2.3 (1.1) | 17.2 (3.9) |
*
Geometric mean.
†
τ = 12 h for b.i.d. dosing and 24 h for q.d. dosing.
‡
Arithmetic mean.
§
AUC and t1/2 were only calculated for five subjects. nc, not calculated.