Table 3.
Pharmacokinetic parameters of pridopidine and its metabolite TV‐45065 after single and multiple daily doses of 45 mg pridopidine to subjects with moderate renal impairment and normal renal function
| Single dose | Steady‐state | ||||||
|---|---|---|---|---|---|---|---|
| Pridopidine | |||||||
| Parameter | Moderate renal impairment (n = 12) | Healthy control of moderate renal impairment (n = 12) | Moderate renal impairment (n = 12) | Healthy control of moderate renal impairment (n = 12) | |||
| AUC (ng ml–1 h) * | 3087 ± 1667 | 2059 ± 711 | 7007 ± 4555 | 3853 ± 1459 | |||
| Cmax (ng ml–1) | 252 ± 53.8 | 278 ± 36.5 | 497 ± 215 | 375 ± 82.9 | |||
| tmax (h) † | 1.5 (0.5–4.0) | 1.0 (0.5–1.5) | 2.0 (0.5–2.5) | 1.5 (0.5–4.0) | |||
| t1/2 (h) | 9.6 ± 4.0 | 5.7 ± 1.3 | 13.6 ± 5.1 | 9.0 ± 2.4 | |||
| Vz/F (l) | 214 ± 48.47 | 192 ± 46.58 | 161 ± 39.0 | 161 ± 35.7 | |||
| CL/F (ml min–1) | 312 ± 148 | 410 ± 150 | 137 ± 56.5 | 218 ± 70.6 | |||
| CLR (ml min–1) | 72.8 ± 32.6 | 75.0 ± 21.3 | 67 ± 27.3 | 90 ± 32.4 | |||
| fe (%) | 24.6 ± 10.9 | 19.3 ± 6.4 | 50 ± 9.8 | 42 ± 11.9 | |||
| Rac | – | – | 2.8 ± 0.8 | 2.0 ± 0.3 | |||
| TV‐45065 | |||||||
| AUC (ng ml–1 h) * | 1728 ± 734 | 1066 ± 218 | 1116 ± 535 | 679 ± 259 | |||
| Cmax (ng ml–1) | 81.3 ± 45.0 | 79.8 ± 25.6 | 60.3 ± 23.8 | 43.0 ± 16.3 | |||
| tmax (h) † | 3.5 (1.5–12.0) | 2.25 (1.0–4.0) | 3.5 (1.0–12.0) | 3.25 (1.5–8.0) | |||
| t1/2 (h) | 12.5 ± 5.0 | 7.4 ± 1.8 | 21.8 ± 9.0 | 14.6 ± 4.9 | |||
| CLR (ml min–1) | 306.4 ± 160.7 | 391.2 ± 96.2 | 274.4 ± 127.1 | 415.8 ± 128.5 | |||
| fe (%) | 47.5 ± 10.0 | 43.9 ± 7.6 | 29.5 ± 7.8 | 28.9 ± 7.2 | |||
*
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.