Table 3.
SAR103168 plasma pharmacokinetics parameters (course 1).
| Plasma SAR103168, mean ± SD (geometric mean) [CV%] | ||||||
|---|---|---|---|---|---|---|
| 1.2 mg/m2 | 1.7 mg/m2 | 2.4 mg/m2 | 4.8 mg/m2 | 9.6 mg/m2 | 14.4 mg/m2 | |
| Day 1 | n = 5 | n = 4 | n = 5 | n = 3 | n = 5 | n = 4 |
| Cmax (ng/mL) | 69.4 ± 29.4 (61.9) [42.4] | 78.3 ± 15.6 (77.0) [19.9] | 140 ± 70.4 (125) [50.2] | 204 ± 83.2 (194) [40.7] | 259 ± 43.8 (256) [16.9] | 533 ± 198 (501) [37.2] |
| tmax* (h) | 0.92 (0.50–7.00) | 0.50 (0.50–0.83) | 0.92 (0.50–0.92) | 0.92 (0.50–0.92) | 1.00 (0.67–1.42) | 0.88 (0.50–0.92) |
| AUClast (ng.h/mL) | 109 ± 60.1† (96.0) [55.1] | 75.5 ± 21.6 (73.4) [28.7] | 283 ± 340 (164) [120.3] | 217 ± 66.3 (211) [30.6] | 744 ± 800 (543) [107.5] | 822 ± 265 (784) [32.3] |
| Day 5 | n = 7 | n = 4 | n = 5 | n = 3 | n = 5 | n = 4 |
| Cmax (ng/mL) | 63.9 ± 47.8 (51.9) [74.8] | 170 ± 144 (138) [84.8] | 350 ± 546 (156) [155.8] | 238 ± 81.5 (228) [34.3] | 291 ± 76.9 (282) [26.5] | 467 ± 255 (420) [54.6] |
| tmax* (h) | 0.92 (0.50–3.95) | 0.96 (0.92–1.33) | 1.08 (0.92–1.28) | 0.92 (0.50–0.92) | 0.92 (0.88–1.00) | 0.90 (0.50–1.00) |
| AUClast (ng.h/mL) | 45.7 ± 40.2 (31.5) [87.9] | 228 ± 171 (176) [74.8] | 468 ± 761 (193) [162.7] | 577 ± 179 (560) [31.0] | 987 ± 1140 (681) [115.5] | 992 ± 684 (3.49) [114.3] |
| T1/2z (h) | NC ± NC (NC) [NC]‡ | NC ± NC (NC) [NC]§ | 4.35 ± 5.13 (2.41) [117.8]¶ | NC ± NC (NC) [NC]‡ | 3.32 ± 2.69 (2.62) [80.9]† | 5.46 ± 6.24 (3.49) [114.3] |
Cmax, peak plasma concentration; tmax, time of peak plasma concentration; AUClast, area under the curve up to last measurement; t1/2z, terminal exponential half-life; SD, standard deviation; CV, coefficient of variation; NC, not calculated.
Median (min-max).
n = 4.
n = 1.
n = 0.
n = 2.