TABLE 3.
SPR206 urine PK parameters in single- and multiple-dose cohorts (PK population)
| SPR206 dose group | Mean ± SDa |
|||
|---|---|---|---|---|
| Ae (mg) | CLR (L/h) | Fe | Fe (%) | |
| SAD | ||||
| 10 mg (n = 1) | 0.75 | 0.034 | 0.007 | 0.70 |
| 25 mg (n = 5) | 1.33 ± 1.09 | 0.32 ± 0.29 | 0.05 ± 0.04 | 5.32 ± 4.38 |
| 50 mg (n = 6) | 9.01 ± 0.95 | 0.85 ± 0.10 | 0.18 ± 0.02 | 18.02 ± 1.93 |
| 100 mg (n = 6) | 26.88 ± 5.06 | 1.35 ± 0.34 | 0.27 ± 0.05 | 26.92 ± 5.06 |
| 200 mg (n = 6) | 71.36 ± 7.68 | 1.77 ± 0.20 | 0.36 ± 0.04 | 35.68 ± 3.85 |
| 400 mg (n = 6) | 213.42 ± 24.78 | 1.97 ± 0.22 | 0.53 ± 0.06 | 53.35 ± 6.21 |
| 300 mg (n = 4) | 147.54 ± 22.49 | 2.13 ± 0.43 | 0.49 ± 0.08 | 49.15 ± 7.50 |
| MAD day 1 | ||||
| 25 mg q8h (n = 5) | 1.04 ± 0.67 | 0.24 ± 0.15 | 0.04 ± 0.03 | 4.14 ± 2.70 |
| 50 mg q8h (n = 6) | 6.51 ± 1.83 | 0.82 ± 0.25 | 0.13 ± 0.04 | 13.03 ± 3.66 |
| 100 mg q8h (n = 6) | 25.28 ± 4.86 | 1.55 ± 0.38 | 0.25 ± 0.05 | 25.28 ± 4.87 |
| 150 mg q8h (n = 6) | 57.66 ± 7.86 | 2.13 ± 0.44 | 0.38 ± 0.05 | 38.42 ± 5.23 |
| 100 mg q8h (14 d) (n = 6) | 24.97 ± 8.08 | 1.58 ± 0.39 | 0.25 ± 0.08 | 24.95 ± 8.08 |
| MAD day 7 | ||||
| 25 mg q8h (n = 6) | 1.76 ± 0.73 | 0.22 ± 0.06 | 0.07 ± 0.03 | 7.03 ± 2.94 |
| 50 mg q8h (n = 6) | 8.51 ± 2.82 | 0.69 ± 0.20 | 0.17 ± 0.06 | 17.03 ± 5.64 |
| 100 mg q8h (n = 6) | 33.09 ± 13.40 | 1.25 ± 0.50 | 0.33 ± 0.13 | 33.08 ± 13.94 |
| 150 mg q8h (n = 4) | 81.17 ± 3.81 | 1.55 ± 0.17 | 0.54 ± 0.03 | 54.10 ± 1.52 |
| 100 mg q8h (14 d) (n = 6) | 36.30 ± 6.72 | 1.29 ± 0.24 | 0.36 ± 0.07 | 36.30 ± 6.73 |
a
Ae, cumulative amount of drug excreted in successive urine intervals with quantifiable urine concentrations; CLR, renal clearance; Fe, fraction of cumulative fraction of dose recovered in urine as unchanged drug in successive urine intervals with quantifiable urine concentrations; Fe (%), percentage fraction of cumulative fraction of dose recovered in urine as unchanged drug in successive urine intervals with quantifiable urine concentrations.