Table 2.
CMAX (ng/ml) | TMAX (hr) | AUC0-t(ng-hr/ml) | AUC0-inf(ng-hr/ml) | AUCExtrap(%) | λ(1/hr) | Half-life, t1/2(hr) | Cl/F(L/hr/kg) | |
---|---|---|---|---|---|---|---|---|
| ||||||||
Pimavanserin | ||||||||
Pimavanserin(mg/kg; s.c.) | ||||||||
0.5 | 12.17 ± 0.38 | 0.29 ± 0.04 | 14.40 ± 0.31 | 15.02 ± 0.32 | 3.89 ± 1.42 | 0.76 ± 0.14 | 1.29 ± 0.45 | 33.40 ± 0.73 |
1 | 30.13 ± 2.17 | 0.25 ± 0.00 | 41.27 ± 2.64 | 41.72 ± 2.7 | 1.09 ± 0.28 | 0.79 ± 0.04 | 0.89 ± 0.05 | 24.55 ± 1.81 |
3 | 79.52 ± 3.76 | 0.38 ± 0.06 | 189.33 ± 7.75 | 197.5 ± 8.33 | 4.26 ± 0.68 | 0.59 ± 0.03 | 1.18 ± 0.05 | 15.28 ± 0.65 |
10 | 213.17 ± 15.86 | 0.96 ± 0.25 | 857.50 ± 54.72 | 1290.17 ± 112.09 | 32.22 ± 4.18 | 0.21 ± 0.02 | 3.63 ± 0.54 | 8.10 ± 0.83 |
Pim + Lora(mg/kg; s.c.) | ||||||||
0.5 + 0.5 | 12.03 ± 1.97 | 0.25 ± 0.00 | 13.88 ± 3.32 | 14.34 ± 3.47 | 2.90 ± 0.69 | 0.80 ± 0.09 | 0.93 ± 0.12 | 41.15 ± 5.30 |
1 + 1 | 26.87 ± 5.04 | 0.25 ± 0.00 | 38.18 ± 11.19 | 39.05 ± 11.56 | 1.90 ± 0.44 | 0.68 ± 0.05 | 1.05 ± 0.08 | 28.00 ± 7.26 |
Lorcaserin | ||||||||
Lorcaserin(mg/kg; s.c.) | ||||||||
0.5 | 15.63 ± 0.74 | 0.29 ± 0.04 | 29.03 ± 0.53 | 33.43 ± 1.31 | 12.68 ± 2.45 | 0.31 ± 0.03 | 2.39 ± 0.33 | 15.07 ± 0.56 |
1 | 34.35 ± 3.19 | 0.25 ± 0.00 | 58.52 ± 3.41 | 63.70 ± 3.91 | 8.06 ± 0.47 | 0.39 ± 0.02 | 1.80 ± 0.09 | 15.97 ± 0.85 |
3 | 106.33 ± 14.74 | 0.42 ± 0.05 | 183.50 ± 7.71 | 199.17 ± 8.24 | 7.97 ± 0.50 | 0.38 ± 0.01 | 1.83 ± 0.07 | 15.18 ± 0.66 |
Pim + Lora(mg/kg; s.c.) | ||||||||
0.5 + 0.5 | 14.74 ± 0.71 | 0.30 ± 0.05 | 26.46 ± 1.80 | 28.48 ± 1.88 | 7.14 ± 0.75 | 0.40 ± 0.02 | 1.74 ± 0.11 | 17.9 ± 1.29 |
1 + 1 | 26.62 ± 1.69 | 0.35 ± 0.06 | 48.88 ± 2.71 | 52.82 ± 2.84 | 7.55 ± 0.52 | 0.41 ± 0.02 | 1.71 ± 0.07 | 19.12 ± 0.99 |
Pimavanserin administered 15 min prior to lorcaserin; CMAX, maximum serum concentration; TMAX, time to reach CMAX; AUC0-t, area under plasma drug concentration-time curve (AUC) up to time ‘t’; AUC0-inf, extrapolated AUC to infinity; AUCExtrap, effect of extrapolated AUC on AUC0-inf estimation; λ, individual estimate of terminal elimination rate constant; t1/2, elimination half-life; Cl/F, apparent total body clearance.