TABLE 2.
Summary of HTL0009936 exposures after IV infusion in part A, mean (%CV) or [range]
| Dose (mg) | Observed C mean (ng/mL) | T max (hr) | C max (ng/mL) | AUC0–24 (hr.ng/mL) | AUC0‐∞ (hr.ng/mL) | t½ (hr) | CLp (L/hr) | CLr (L/hr) |
|---|---|---|---|---|---|---|---|---|
| 10 a | n/a | 0.50 [0.33–0.58] | 59.5 (35) | 120 (24) | 124 (24) | 2.2 (12) | 81 (24) | 8.7 (27) |
| 49.2 b | 97 (22) | 0.50 [0.17–5.5] | 125 (33) | 684 (24) | 691 (24) | 2.3 (35) | 71 (24) | 7.2 (41) |
| 83 c | 172 (17) | 2.0 [2.0–3.0] | 197 (20) | 1130 (17) | 1140 (16) | 2.4 (25) | 73 (17) | 7.8 (25) |
Geometric mean and (geometric %CV) except T max median [minimum − maximum] for n = 6 per dose except n = 5 at 83 mg. AUC0‐∞, area under the plasma concentration–time curve from zero extrapolated to infinity; AUC0–24, area under the plasma concentration–time curve from zero to 24 hours post dose; C max, maximum plasma concentration; C mean, mean plasma concentration during maintenance infusion; CLp, total plasma clearance; CLr, renal clearance; T max, time to C max; t½, apparent terminal half‐life.
a
10 mg over 0.5 hr at 33.2 mL/h.
b
14.1 mg over 0.5 hr at 47 mL/hr + 35.1 mg over 4.5 hr at 13 mL/hr.
c
43 mg over 2 hr at 64.8 mL/hr + 40 mg over 3 hr at 40.2 mL/hr.