TABLE 7.
Summary of the steady-state PK parameters of TPV, RFB, and 25-O-desacetyl-RFBa
| PK parameterb | Result for TPV in regimen of:
|
Result for RFB in regimen of:
|
Result for 25-O-desacetyl-RFB in regimen of:
|
|||
|---|---|---|---|---|---|---|
| TPV/r alone (day 14) (n = 21) | TPV/r + RFB (day 15) (n = 21) | RFB alone (day 1) (n = 20) | RFB + TPV/r (day 15) (n = 20) | RFB alone (day 1) (n = 20) | RFB + TPV/r (day 15) (n = 20) | |
| AUC | 955 (980, 537-1,444) | 953 (996, 586-1,761) | 2,217 (2,157, 895-6,032) | 6,441 (6,206, 4,160-10,426) | 182 (175, 64-560) | 3,775 (3,716, 2,518-6405) |
| Cmax | 140.6 (141.1, 84.5-213.1) | 139.7 (143.7, 87.0-284.7) | 162.0 (156.5, 55.9-435.0) | 275.5 (283.0, 173.0-455.0) | 18.7 (20.4, 7.5-38.3) | 59.8 (56.1, 34.1-109.0) |
| Cmin | 35.2 (38.8, 10.5-79.2) | 41.0 (41.4, 16.5-97.6) | 46.7 (49.0, 23.7-116.0) | 100.1 (99.3, 70.0-161.0) | 5.4 (4.9, 2.4-15.1) | 42.2 (43.8, 22.7-71.3) |
| Tmax (h) | 2.8 (3.0, 2.0-4.0) | 2.6 (3.0, 1.5-4.0) | 3.5 (3.0, 2.0-6.0) | 4.1 (4.0, 2.0-6.0) | 3.6 (3.0, 2.0-6.0) | 5.8 (6.0, 4.0-8.0) |
| t1/2 (h) | 4.7 (4.5, 2.5-8.0) | 5.5 (5.8, 3.0-11.1) | 41.3 (51.8, 11.7-84.8) | 65.1 (71.2, 42.5-91.6) | 6.5 (6.1, 3.5-14.1) | 64.2 (68.9, 37.3-84.6) |
| CL/F (liters/h) | 0.87 (0.85, 0.57-1.54) | 0.87 (0.47, 0.83-1.42) | 67.7 (69.6, 24.9-167.6) | 23.3 (24.2, 14.4-36.1) | NA | NA |
| V (liters) | 5.9 (6.1, 3.6-9.1) | 7.0 (7.3, 3.6-9.8) | 4,028 (4,368, 1,542-8,638) | 2,188 (2,318, 909-3205) | NA | NA |
a
Data are given as the geometric mean (median, range). NA, not applicable.
b
Unless otherwise indicated, parameters and units of measurement are as follows: for RFB, AUC0-∞ (ng·h/ml), Cmax (ng/ml), and Cp12h (Cmin; ng/ml); and for TPV, AUC0-12 (μM·h), Cmax (μM), and Cp12h (Cmin; μM).