3a.
Single Dose (Part 1): Pharmacokinetic Parameters for MC4-NN2-0453
| 0.03 mg/kg (n = 6) | 0.06 mg/kg (n = 5)a | 0.15 mg/kg (n = 6) | 0.30 mg/kg (n = 6) | 0.60 mg/kg (n = 6) | 1.00 mg/kg (n = 6) | 1.50 mg/kg (n = 5)b | |
|---|---|---|---|---|---|---|---|
| Cmax (ng/mL) | 195 (23.1) | 309 (39.1) | 672 (108) | 1,590 (358) | 3,200 (616) | 4,880 (1,020) | 6,540 (909) |
| tmax (hour) | 61.3 (14.9) | 60.8 (31.3) | 100 (27.1) | 61.3 (56.0) | 50.7 (6.5) | 53.3 (9.7) | 70.7 (26.5) |
 (hour) |
234 (48.8) | 268 (46.9) | 270 (35.8) | 268 (28.6) | 259 (30.2) | 260 (77.6) | 274 (61.1) |
| AUC0–24h (h ng/mL) | 2,080 (431) | 2,990 (960) | 6,730 (1,280) | 15,500 (5,220.2) | 44,500 (11,200) | 59,300 (12,700) | 68,500 (14,100) |
| AUClast (h ng/mL) | 51,400 (6,640) | 98,200 (16,700) | 212,000 (36,500) | 454,000 (70,683.8) | 912,000 (164,000) | 1,470,000 (299,000) | 1,980,000 (385,000) |
| AUC0–∞ (h ng/mL) | 67,600 (11,300) | 138,000 (30,100) | 313,000 (77,800) | 633,000 (113,315.6) | 1,240,000 (237,000) | 2,050,000 (534,000) | 2,650,000 (329,000) |
| CL/F (L/h/kg) | 0.0005 (0.0001) | 0.0005 (0.0001) | 0.0005 (0.0001) | 0.0005 (0.0001) | 0.0005 (0.0001) | 0.0005 (0.0001) | 0.0006 (0.0001) |
| Vz/F (L/kg) | 0.15 (0.02) | 0.17 (0.03) | 0.19 (0.02) | 0.19 (0.02) | 0.18 (0.03) | 0.18 (0.04) | 0.23 (0.07) |
Data are mean (standard deviation).
a
Except for AUC0–24h which was calculated based on n = 6.
b
Except for Cmax, tmax, and AUC0–24h which were calculated based on n = 6.