Table 2:
Pharmacokinetic parameters of ART-123 during the first 24 hours.
| Dose | 380 U/kg | 130 U/kg | ||||||
|---|---|---|---|---|---|---|---|---|
| Group 1 | Group 2 | Group 3 | Group 4 | Group 1 | Group 2 | Group 3 | Group 4 | |
| Ccr < 10.0 | 10.0 ≤ Ccr < 30.0 | 30.0 ≤ Ccr < 60.0 | 60.0 ≤ Ccr | Ccr < 10.0 | 10.0 ≤ Ccr < 30.0 | 30.0 ≤ Ccr < 60.0 | 60.0 ≤ Ccr | |
| Number of patients | 9 | 6 | 6 | 10 | 4 | 3 | 0 | 1 |
| CLtot (ml/hour/kg) | 2.39 ± 0.988 | 2.76 ± 0.731 | 2.29 ± 0.515 | 3.56 ± 0.697 | 2.40 ± 0.720 | 2.16 ± 0.605 | - | 4.85 |
| Vd (ml/kg) | 82.7 ± 15.3 | 68.2 ± 24.3 | 71.4 ± 12.2 | 80.8 ± 16.8 | 75.0± 7.20 | 59.4± 8.04 | - | 97.7 |
| Cmax (ng/ml) | 828 ± 156 | 1,110 ± 460 | 987 ± 294 | 807 ± 160 | 287 ± 41.6 | 390 ± 95.0 | - | 221 |
| AUC0–24 (ng·hour/ml) | 12,900 ± 2,910 | 14,400 ± 4,480 | 14,300 ± 3,010 | 11,100 ± 1,700 | 4,580 ± 847 | 5,580 ± 1,000 | - | 2,910 |
| t1/2 (hours) | 27.3 ± 12.0 | 16.8 ± 2.03 | 22.0 ± 2.93 | 16.2 ± 3.52 | 23.0 ± 5.72 | 19.9 ± 4.25 | - | 14.0 |
| fe0–24 (%) | 1.03 ± 0.895 | 4.58 ± 3.29 | 6.90 ± 3.41* | 13.7 ± 4.77 | 1.04 ± 0.651 | 5.38 ± 1.29 | - | 18.2 |
Ccr, 24-hour creatinine clearance; CLtot, total body clearance; Vd, volume of distribution; Cmax, maximum plasma concentration; AUC0–24, area under plasma concentration-time curve from time 0 to 24 hours post dose; t1/2, elimination half-life; fe0–24, fractional excretion in urine from time 0 to 24 hours after dosing (Day 1 urine excretion rate); Data are represented as mean ± SD.
* fe0–24 was calculated using data for 5 patients, one patient was excluded from the analysis of fe0–24 owing to a urine collection error.