Table 7. Pharmacokinetics of 15c in Preclinical Species.
| intravenous
PK parameters (IV, n = 3) | |||||
|---|---|---|---|---|---|
| species | dose (mg/kg)a | Clpb | Vd (L/kg) | T1/2 (h) | AUC (μM·h) |
| rat | 3 | 29.1 ± 7.7 | 5.8 ± 3.1 | 7.5 ± 1.0 | 3.4 ± 0.8 |
| dog | 1 | 9.4 ± 2.3 | 2.4 ± 0.63 | 10.4 ± 2.4 | 3.46 ± 0.80 |
| monkey | 1c | 16.4 ± 2.30 | 5.80 ± 0.76 | 12.9 ± 2.05 | 1.92 ± 0.27 |
| oral
PK parameters (PO, n = 3) | |||||
|---|---|---|---|---|---|
| species | dose (mg/kg) | Cmax (μM) | Tmax (h) | AUC (μM·h) | Foral |
| rat | 10d | 2.07 ± 1.59 | 0.58 ± 0.38 | 6.77 ± 3.19 | 61 ± 29 |
| dog | 2e | 2.47 ± 0.67 | 0.42 ± 0.14 | 8.51 ± 3.09 | 121 ± 44 |
| rhesus | 10e | 5.69 ± 2.02 | 0.42 ± 0.14 | 6.76 ± 1.78 | 28 ± 7.6 |
a
20% hydroxypropyl-beta-cyclodextrin with 100 mM sodium phosphate (pH 8).
b
mL/min/kg.
c
5% dimethyl sulfoxide/30% propylene glycol/30% polyethylene glycol 300/35% (40% hydroxypropyl-beta-cyclodextrin).
d
0.5% methyl cellulose/0.2% sodium laurel sulfate/5 mM HCI.
e
0.4% hydroxypropyl methylcellulose.