TABLE 3.
Summary of plasma PK parameters of SPR719 following single oral dose administration of SPR720 in healthy volunteers
| SPR720 treatment (n) | Mean (% CV)a |
||||||
|---|---|---|---|---|---|---|---|
| Cmax (ng/ml) | Tmax (h) | t1/2 (h) | AUClast (h ⋅ ng/ml) | AUC0–24 (h ⋅ ng/ml) | AUCinf (h ⋅ ng/ml) | AUCext (%) | |
| 100 mg (6) | 278 (58.3) | 3 (1–4) | 3.15 (65.4)b | 1,360 (95.6) | 1,620 (174.6)b | 1,650 (184.0)b | 3.82 (132.0)b |
| 250 mg (6) | 1,220 (74.1) | 2.75 (1–4) | 2.92 (23.4)c | 6,060 (44.7) | 6,900 (41.3)c | 6,940 (40.8)c | 2.68 (93.7)c |
| 500 mg (6) | 2,860 (28.4) | 4 (2–4) | 3.59 (42.7)d | 16,000 (58.3) | 21,000 (35.6)d | 21,600 (39.9)d | 1.04 (88.7)d |
| 1,000 mg (6) | 4,730 (22.1) | 4 (1.5–4) | 3.96 (15.2)d | 56,500 (22.6) | 54,700 (21.6) | 56,800 (22.3)d | 0.234 (211.8)d |
| 1,000 mg (6) | 4,000 (16.4) | 6 (4–8) | 4.31 (25.2) | 45,100 (27.4) | 43,300 (25.7) | 45,200 (27.3) | 0.242 (76.3) |
| 1,500 mg (6) | 5,990 (39.8) | 8 (1–12) | 4.50 (24.2)d | 75,700 (49.5) | 72,300 (47.3) | 81,600 (37.8)d | 0.161 (107.7)d |
| 2,000 mg (6) | 8,240 (33.6) | 4 (2–8) | 3.96 (18.0) | 111,000 (27.6) | 106,000 (27.4) | 112,000 (27.5) | 0.215 (87.7) |
| 500 mg, elderly (6) | 1,760 (73.8) | 4 (2–8) | 3.36 (40.6)e | 11,400 (75.0) | 18,300 (55.0)b | 24,900 (8.8)e | 0.307 (36.6)e |
AUC0–24, area under the concentration-time curve from time zero to 24 h; AUCext, area under the concentration-time curve extrapolated to infinity; AUCinf, area under the concentration-time curve from time zero to infinity; AUClast, area under the concentration-time curve to the last measured time point; Cmax, maximum concentration; t1/2, elimination half-life; Tmax, time of maximum observed concentration. Cmax and AUC values are expressed as geometric means (% coefficient of variation [CV%]), Tmax values are expressed as medians (ranges), and half-life (t1/2) values are expressed as arithmetic means. The lower limit of quantitation is 10 ng/ml; BQL assigned a value of missing.
n = 3.
n = 5.
n = 4.
n = 2.