TABLE 2.
Summary of MK-8507 plasma PK following administration of single oral MK-8507 doses of a suspension (2 to 400 mg) or tablet (400 to 1,200 mg) with fasting and 100-mg dose of suspension following a high-fat meal in adults without HIVb
| Type of dose | Dose amt (mg) | No. of patients | AUC0-∞a (geometric mean [95% CI] [μM·h]) | AUC0–168a (geometric mean [95% CI] [μM·h]) | Cmaxa (geometric mean [95% CI] [μM]) | C168hra (geometric mean [95% CI] [μM]) | Tmax (median [min, max] [h]) | Apparent terminal t½ (geometric mean [%GVC] [h]) |
|---|---|---|---|---|---|---|---|---|
| Suspension | 2 | 6 | 3.82 (3.30–4.43) | 2.94 (2.62–3.29) | 0.05 (0.05–0.06) | 0.01(0.01–0.01) | 2.00 (2.00–2.00) | 82.9 (8.54) |
| 10 | 6 | 15.2 (13.1–17.6) | 11.9 (10.6–13.3) | 0.22 (0.19–0.25) | 0.03 (0.02–0.03) | 2.00 (1.00–4.00) | 82.0 (34.6) | |
| 30 | 6 | 52.0 (44.9–60.2) | 39.7 (35.4–44.6) | 0.79 (0.68–0.90) | 0.10 (0.08–0.13) | 2.00 (2.00–4.00) | 77.7 (9.97) | |
| 100 | 6 | 175 (151–202) | 139 (124–156) | 2.58 (2.23–2.97) | 0.30 (0.24–0.39) | 2.04 (2.00–4.00) | 75.9 (27.2) | |
| 100 (fed) | 6 | 159 (138–184) | 126 (112–141) | 1.67 (1.45–1.93) | 0.31 (0.24–0.39) | 10.00 (6.00–12.02) | 72.6 (30.6) | |
| 200 | 6 | 374 (323–433) | 287 (256–322) | 5.40 (4.68–6.23) | 0.68 (0.53–0.87) | 2.02 (2.00–4.03) | 83.5 (14.3) | |
| 400 | 6 | 770 (666–892) | 619 (552–694) | 11.5 (9.99–13.3) | 1.30 (1.02–1.67) | 4.00 (2.00–4.00) | 69.1 (29.9) | |
| Tablet | 400 | 6 | 710 (592–850) | 606 (501–732) | 9.09 (7.13–11.6) | 1.28 (0.99–1.64) | 7.00 (2.00–12.00) | 58.3 (14.9) |
| 800 | 6 | 1,230 (1,030–1,480) | 989 (818–1,190) | 15.4 (12.1–19.6) | 2.10 (1.63–2.70) | 4.00 (4.00–6.00) | 70.9 (36.5) | |
| 1,200 | 6 | 1,920 (1,600–2,300) | 1,570 (1,300–1,890) | 23.6 (18.5–30.1) | 3.59 (2.79–4.61) | 5.00 (4.00–8.00) | 68.7 (12.8) |
a
Back-transformed LSM and CI from linear mixed-effects model performed on natural log-transformed values.
b
AUC, area under the concentration-time curve; C168hr, trough concentration; CI, confidence interval; Cmax, maximum concentration; CV, coefficient of variation; GCV, geometric coefficient of variation; LSM, least-squares mean; max, maximum; min, minimum; t1/2, terminal half-life; Tmax, time to maximum concentration.