TABLE 8.
Summary statistics for ertapenem single- and multiple-dose PK parameters in urine by treatment groupa,b,c
| Urine PK Parameters | WCK 6777 2 g | ERT 2 g | WCK 6777 4 g | ERT 3 g | WCK 6777 6 g |
|---|---|---|---|---|---|
| Ertapenem single-dose urine PK parameters | |||||
| Ae,urine (mg) 0–4 h | 339.62 (97.70, 605.00) | 748.60 (573.00, 995.00) | 794.50 (414.00, 1,620.00) | 768.60 (451.00, 1,090.00) | 670.13 (87.80, 1,630.00) |
| Ae,urine (mg) 4–8 h | 159.23 (74.20, 268.00) | 275.67 (105.00, 414.00) | 202.67 (163.00, 272.00) | 713.50 (393.00, 1,850.00) | 605.83 (246.00, 1,390.00) |
| Ae,urine (mg) 8–12 h | 64.30 (19.80, 83.80) | 122.38 (58.80, 204.00) | 128.93 (77.50, 202.00) | 173.50 (128.00, 227.00) | 192.00 (112.00, 305.00) |
| Ae,urine (mg) 12–24 h | 49.80 (25.60, 66.50) | 84.22 (49.90, 150.00) | 54.38 (19.20, 106.00) | 149.15 (84.50, 235.00) | 106.95 (58.50, 158.00) |
| Ae,urine(0–24) (mg) | 594.00 (204.00, 856.00) | 1,085.67 (321.00, 1,490.00) | 1,181.83 (711.00, 2,190.00) | 1,676.67 (1,200.00, 2,160.00) | 1,572.17 (843.00, 2,400.00) |
| fe,urine (%) 0–4 h | 33.96 (9.77, 60.50) | 37.46 (28.70, 49.80) | 39.75 (20.70, 81.20) | 25.60 (15.00, 36.20) | 22.33 (2.93, 54.30) |
| fe,urine (%) 4–8 h | 15.92 (7.42, 26.80) | 13.78 (5.27, 20.70) | 10.14 (8.14, 13.60) | 23.77 (13.10, 61.60) | 20.16 (8.18, 46.20) |
| fe,urine (%) 8–12 h | 6.43 (1.98, 8.38) | 6.12 (2.94, 10.20) | 6.45 (3.88, 10.10) | 5.79 (4.28, 7.57) | 6.41 (3.74, 10.20) |
| fe,urine (%) 12–24 h | 4.98 (2.56, 6.65) | 4.21 (2.49, 7.48) | 2.72 (0.96, 5.32) | 4.97 (2.82, 7.83) | 3.57 (1.95, 5.28) |
| fe,urine0–24 (%) | 59.40 (20.40, 85.60) | 54.32 (16.10, 74.70) | 58.98 (35.50, 109.00) | 55.85 (40.10, 71.80) | 52.43 (28.10, 79.90) |
| CLR0–24 (L/h) | 0.75 (61) | 0.78 (57) | 0.79 (41) | 0.76 (19) | 0.73 (42) |
| Ertapenem multiple-dose urine PK parameters | |||||
| Ae,urine (mg) 0–4 h,ss | 357.83 (208.00, 525.00) | 702.30 (39.50, 1,270.00) | 777.80 (433.00, 1,490.00) | 1,010.40 (655.00, 1,530.00) | 998.17 (467.00, 1,670.00) |
| Ae,urine (mg) 4–8 h,ss | 113.37 (10.10, 205.00) | 344.17 (132.00, 911.00) | 234.94 (97.70, 473.00) | 603.40 (186.00, 1,100.00) | 417.33 (209.00, 727.00) |
| Ae,urine (mg) 8–12 h,ss | 54.95 (7.16, 88.10) | 136.54 (21.70, 198.00) | 88.86 (48.10, 153.00) | 171.80 (137.00, 217.00) | 113.88 (54.00, 150.00) |
| Ae,urine (mg) 12–24 h,ss | 43.04 (26.70, 68.20) | 29.69 (9.35, 72.20) | 65.46 (55.00, 81.10) | 113.98 (85.60, 159.00) | 96.03 (61.50, 167.00) |
| Ae,urine0–24,SS (mg) | 552.83 (325.00, 778.00) | 1,067.33 (340.00, 1,700.00) | 1,166.60 (652.00, 2,200.00) | 1,898.00 (1,060.00, 3,000.00) | 1,624.50 (887.00, 2,320.00) |
| fe,urine (%) 0–4 h,ss | 35.78 (20.80, 52.50) | 35.09 (1.97, 63.30) | 38.94 (21.70, 74.60) | 33.68 (21.80, 51.00) | 33.28 (15.60, 55.80) |
| fe,urine (%) 4–8 h,ss | 11.34 (1.01, 20.50) | 17.19 (6.62, 45.50) | 11.72 (4.89, 23.60) | 20.08 (6.19, 36.50) | 13.91 (6.96, 24.20) |
| fe,urine (%) 8–12 h,ss | 5.50 (0.72, 8.81) | 6.83 (1.08, 9.91) | 4.45 (2.41, 7.67) | 5.73 (4.57, 7.23) | 3.80 (1.80, 5.01) |
| fe,urine (%) 12–24 h,ss | 4.30 (2.67, 6.82) | 1.48 (0.47, 3.61) | 3.27 (2.75, 4.06) | 3.80 (2.85, 5.30) | 3.20 (2.05, 5.56) |
| fe,urine0–24,SS (%) | 55.28 (32.50, 77.80) | 53.35 (17.00, 84.90) | 58.36 (32.60, 110.00) | 63.28 (35.50, 100.00) | 54.20 (29.60, 77.40) |
| CLR(0–24),SS (L/h) | 0.74 (28) | 0.78 (53) | 0.84 (48) | 0.92 (37) | 0.90 (44) |
a
Times are relative to time of dosing.
b
Values of mean (min, max) are shown, except for CLR, for which values of GM (CV%) are shown.
c
Ae, amount excreted in urine; CLR, renal clearance; CV, coefficient of variation; ERT, ertapenem; fe, fraction of dose excreted unchanged in urine; GM, geometric mean; WCK 6777, ertapenem/zidebactam; ss, steady state.