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. 2013 Mar;57(3):1209–1217. doi: 10.1128/AAC.01263-12

Table 1.

Derived plasma pharmacokinetic parameters for GS-9851, GS-566500, and GS-331007

Parameter Mean (SD) value for day and dose [na]b
Day 1
 Day 3
50 mg 100 mg 200 mg 400 mg 50 mg 100 mg 200 mg 400 mg
GS-9851
    AUC0–t (h · ng/ml) 37.4 (19.9) [8] 84.4 (87.6) [8] 149.5 (139.8) [8] 234.0 (127.6) [8] 30.8 (24.2) [7] 102.6 (96.0) [8] 148.9 (185.3) [8] 185.2 (135.7) [8]
    AUC0–24 (h · ng/ml) 45.7 (24.7) [8] 90.2 (91.6) [8] 162.1 (144.3) [8] 236.4 (130.5) [8] 35.1 (25.2) [7] 113.2 (101.0) [8] 159.7 (184.8) [8] 191.5 (136.3) [8]
    Cmax (ng/ml) 23.1 (8.9) [8] 61.2 (72.5) [8] 75.4 (38.5) [8] 165.6 (130.4) [8] 21.5 (15.4) [7] 81.0 (117.2) [8] 77.1 (74.9) [8] 81.7 (65.3) [8]
    t1/2 (h) 0.8 (0.4, 1.2) [2] 2.1 (1.1, 4.2) [3] 1.0 (1.0, 1.1) [2] 1.0 (0.9, 1.2) [2] 1.3 (0.6, 2.1) [2] 1.0 (0.6, 1.3) [2]
    tmax (h) 1.8 (1.0, 3.0) [8] 1.0 (0.8, 1.8) [8] 1.0 (1.0, 1.6) [8] 1.3 (1.0, 2.4) [8] 2.0 (1.0, 2. 0) [7] 1.5 (1.0, 1.5) [8] 1.0 (0.8, 1.3) [8] 1.0 (0.8, 1.5) [8]
    AUC extrapolated (%) 7.4 (1.93) [2) 21.9 (15.0) [3)
GS-566500
    AUC0–t (h · ng/ml) 16.6 (17.7) [7] 82.1 (70.2) [5] 125.8 (135.7) [7] 286.9 (260.7) [8)] 15.8 (10.2) [4] 81.3 (110.7) [7] 93.3 (107.3) [8] 201.6 (157.5) [8]
    AUC0–24 (h · ng/ml) 24.4 (23.4) [7] 97.3 (70.5) [5] 138.5 (136.8) [7] 301.4 (268.8) [8] 21.3 (11.8) [4] 91.5 (113.2) [7] 105.7 (110.2) [8] 215.0 (162.9) [8]
    Cmax (ng/ml) 13.4 (4.3) [7] 36.7 (24.1) [5] 38.2 (24.1) [7] 72.2 (61.5) [8] 13.3 (0.8) [4] 32.8 (32.6) [7] 29.1 (17.3) [8] 46.2 (31.9) [8]
    t1/2 (h) 2.4 (2.4, 2.4) [2] 2.0 (1.9, 3.8) [4] 3.1 (2.7, 3.5) [7] 2.3 [1] 3.3 (2.3, 4.3) [2] 3.7 (2.9, 5.0) [3]
    tmax (h) 3.0 (1.5, 3.1) [7] 2.0 (1.0, 3.0) [5] 1.5 (1.5, 4.0) [7] 1.9 (1.5, 3.0) [8] 1.8 (1.5, 2.5) [4] 2.0 (2.0, 3.0) [7] 2.0 (1.3, 3.0) [8] 2.0 (1.3, 3.3) [8]
    AUC extrapolated (%) 29.6 (15.5) [2] 27.0 (13.8) [4] 19.4 (9.8) [7]
GS-331007
    AUC0–t (h · ng/ml) 899.9 (357.5) [8] 1,256.4 (617.4) [8] 2,554.1 (919.2) [8] 2,854.4 (1,069.3) [8] 918.9 (393.8) [7] 2,100.8 (562.1) [8] 3,196.4 (1,364.7) [8] 5,311.0 (3,182.8) [8]
    AUC0–24 (h · ng/ml) 942.7 (364.1) [8) 1,277.4 (600.6) [8) 2,555.5 (919.4) [8) 2,856.4 (1,070.6) [8) 951.5 (390.3) [7) 1,719.9 (372.13) [8) 2,947.7 (1,097.4) [8) 3,554.4 (1,380.1) [8)
    AUC0–∞ (h · ng/ml) 1,115.3 (300.6) [7] 1,488.9 (564.4) [7] 2,943.5 (1,053.1) [6] 4,179.1 (1,615.0) [5]
    Cmax (ng/ml) 129.8 (47.2) [8) 174.2 (80.1) [8] 318.5 (100.4) [8] 335.1 (98.3) [8) 117.7 (41.9) [7] 218.9 (52.2) [8] 336.6 (68.5) [8] 340.4 (109.5) [8]
    t1/2 (h) 4.1 (2.9, 7.9) [7] 5.8 (5.4, 7.7) [7] 6.8 (6.6, 9.0) [6] 11.7 (11.1, 12.0) [5] 6.0 (3.2, 7.0) [5] 10.3 (8.1, 14.9) [4] 7.2 (5.5, 9.6) [7] 17.9 (15.4, 21.4) [3]
    tmax (h) 3.5 (3.0, 4.0) [8] 3.5 (3.0, 4.0) [8] 3.5 (3.0, 4.0) [8] 3.0 (2.5, 4.0) [8] 4.0 (3.0, 4.0) [7] 3.0 (2.5, 3.5) [8] 3.5 (3.0, 5.0) [8] 3.0 (2.5, 3.5) [8]
    GS-331007/GS-9851 AUC0–t ratioc 71.0 (66.2) 93.0 (108.2) 55.7 (32.9) 37.6 (28.4) 113.6 (87.5) 91.5 (81.3) 64.2 (23.5) 84.7 (68.2)
a

n, no. of subjects.

b

Data for t1/2 and tmax are presented as median (first quartile, third quartile).

c

Ratio calculated after conversion of GS-331007 AUC0–t into nanogram equivalents of GS-9851 · h/ml.