Table 2.
Pharmacokinetic parameters of pridopidine and its metabolite TV‐45065 after single and multiple daily doses of 45 mg pridopidine to subjects with mild renal impairment and normal renal function
| Single dose | Steady‐state | ||||||
|---|---|---|---|---|---|---|---|
| Pridopidine | |||||||
| Parameter | Mild renal impairment (n = 12) | Healthy control of mild renal impairment (n = 12) | Mild renal impairment (n = 12) | Healthy control of mild renal impairment (n = 12) | |||
| AUC (ng ml–1 h) * | 2365 ± 1120 | 2365 ± 1264 | 3999 ± 1390 | 3851 ± 1557 | |||
| Cmax (ng ml–1) | 276 ± 66.6 | 263 ± 71.1 | 358 ± 87.3 | 426 ± 128 | |||
| tmax (h) † | 1.0 (0.5–3.0) | 1.2 (1.0–2.0) | 1.5 (0.5–3.0) | 1.3 (0.5–4.0) | |||
| t1/2 (h) | 6.9 ± 3.3 | 7.6 ± 3.6 | 9.1 ± 2.2 | 9.6 ± 3.0 | |||
| Vz/F (l) | 201 ± 42.3 | 219 ± 55.8 | 173 ± 45.55 | 156 ± 30.5 | |||
| CL/F (ml min–1) | 397 ± 185 | 388 ± 155 | 211 ± 75.6 | 232 ± 116 | |||
| CLR (ml min–1) | 101 ± 30.0 | 106 ± 32.1 | 99 ± 32.8 | 116 ± 31.1 | |||
| fe (%) | 29.8 ± 16.7 | 30.6 ± 14.7 | 49 ± 12.5 | 55 ± 16.3 | |||
| Rac | – | – | 2.04 ± 0.5 | 1.90 ± 0.3 | |||
| TV‐45065 | |||||||
| AUC (ng ml–1 h) * | 932 ± 305 | 804 ± 279 | 651 ± 255 | 514 ± 243 | |||
| Cmax (ng ml–1) | 59.4 ± 29.9 | 54.5 ± 25.9 | 38.6 ± 15.1 | 37.5 ± 25.2 | |||
| tmax (h) † | 2.5 (1.0–8.0) | 2.5 (1.5–8.0) | 2.5 (1.0–24.0) | 1.75 (1.0–8.0) | |||
| t1/2 (h) | 10.2 ± 4.7 | 8.5 ± 3.0 | 16.1 ± 7.0 | 13.6 ± 5.7 | |||
| CLR (ml min–1) | 455.5 ± 102.9 | 496.3 ± 112.4 | 444.8 ± 108.9 | 517.8 ± 130.8 | |||
| fe (%) | 42.7 ± 13.7 | 40.7 ± 10.9 | 30.7 ± 11.6 | 28.4 ± 11.6 | |||
*
AUC(0,∞) for single dose, AUC(0,τ) for multiple dose;
†
t max presented as median (range), all other parameters are presented as arithmetic mean ± SD.