Table 2.
Plasma concentration-time profiles
| A is plasma concentration-time profiles after single dose of upacicalcet | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Step | Group | N | Cmax (ng/mL) | tmax (h) | AUC0–66h (h·ng/mL) | AUCinf (h·ng/mL) | t1/2 (h) | MRT0–t (h) | MRTinf (h) | CLp (mL/h) | Vdss (mL) |
| Step 1 | 0.025 mg | 4 | 3.20 ± 0.86 | 0.167 ± 0.000 | 85.1 ± 8.21 | 270 ± 161 | 122 ± 80.7 | 29.2 ± 0.250 | 174 ± 113 | 106 ± 43.5 | 14900 ± 741 |
| Step 2 | 0.05 mg | 4 | 6.93 ± 1.62 | 0.167 ± 0.000 | 203 ± 26.6 | 456 ± 63.3 | 77.6 ± 8.87 | 28.8 ± 0.386 | 111 ± 12.2 | 105 ± 13.5 | 11700 ± 1710 |
| Step 3 | 0.1 mg | 4 | 10.5 ± 3.79 | 0.375 ± 0.417 | 261 ± 81.8 | 506 ± 235 | 65.0 ± 30.6 | 26.8 ± 2.83 | 91.5 ± 44.8 | 211 ± 71.5 | 17700 ± 7990 |
| Step 4 | 0.2 mg | 4 | 21.9 ± 2.61 | 0.167 ± 0.000 | 675 ± 99.4 | 1480 ± 257 | 76.6 ± 8.08 | 28.6 ± 0.171 | 109 ± 11.3 | 130 ± 24.7 | 14100 ± 2060 |
| Step 5 | 0.4 mg | 4 | 56.5 ± 8.32 | 0.167 ± 0.000 | 1530 ± 320 | 3150 ± 1080 | 68.1 ± 14.1 | 28.1 ± 0.929 | 97.1 ± 20.7 | 129 ± 37.7 | 11900 ± 1530 |
| Step 6 | 0.6 mg | 4 | 74.2 ± 25.1 | 0.167 ± 0.000 | 2130 ± 542 | 5000 ± 1350 | 83.2 ± 6.88 | 29.1 ± 0.472 | 119 ± 9.42 | 120 ± 35.5 | 14200 ± 3960 |
| Step 7 | 0.8 mg | 5 | 113 ± 42.0 | 0.167 ± 0.000 | 2700 ± 1250 | 6130 ± 3530 | 72.0 ± 33.1 | 26.3 ± 6.23 | 102 ± 47.9 | 212 ± 224 | 13200 ± 4770 |
| B is plasma concentration-time profiles after multiple dose of upacicalcet | |||||
|---|---|---|---|---|---|
| Step | Group | Visit (day) | N | Ctrough (ng/mL) | Cmax (ng/mL) |
| Step 1 | 0.05 mg | 1 | 8 | – | 7.10 ± 1.84 |
| 3 | 8 | 2.21 ± 0.97 | – | ||
| 5 | 8 | 2.42 ± 1.20 | – | ||
| 8 | 8 | 1.97 ± 1.17 | – | ||
| 10 | 8 | 2.66 ± 1.23 | – | ||
| 12 | 8 | 2.46 ± 1.45 | – | ||
| 15 | 7 | 2.04 ± 1.41 | – | ||
| 17 | 7 | 2.67 ± 1.25 | 7.83 ± 1.43 | ||
| 19 | 7 | 2.84 ± 1.28 | – | ||
| 22 | 7 | 1.88 ± 1.17 | – | ||
| Step 2 | 0.1 mg | 1 | 8 | – | 15.6 ± 4.21 |
| 3 | 8 | 5.19 ± 1.02 | – | ||
| 5 | 8 | 6.43 ± 1.10 | – | ||
| 8 | 8 | 5.49 ± 1.24 | – | ||
| 10 | 8 | 6.56 ± 1.24 | – | ||
| 12 | 7 | 6.60 ± 1.29 | – | ||
| 15 | 7 | 5.38 ± 1.27 | – | ||
| 17 | 6 | 6.61 ± 0.82 | 16.7 ± 3.35 | ||
| 19 | 6 | 6.52 ± 1.15 | – | ||
| 22 | 6 | 5.68 ± 1.01 | ± | ||
| Step 3 | 0.2 mg | 1 | 10 | – | 26.3 ± 4.73 |
| 3 | 10 | 8.65 ± 1.98 | – | ||
| 5 | 10 | 10.7 ± 2.78 | – | ||
| 8 | 9 | 8.88 ± 2.83 | – | ||
| 10 | 9 | 10.5 ± 2.52 | – | ||
| 12 | 7 | 11.2 ± 3.69 | – | ||
| 15 | 7 | 9.17 ± 3.12 | – | ||
| 17 | 7 | 11.2 ± 3.35 | 26.4 ± 7.15 | ||
| 19 | 6 | 10.5 ± 3.21 | – | ||
| 22 | 4 | 11.1 ± 2.90 | – | ||
Mean ± SD