Table 5. PK Parameters of LEN Following Subcutaneous Administration of LEN in a PEG/Water Solution Formulation to Male Beagle Dogsabc.
| group ID | dose (mg/kg) | dose volume (mL/kg) | AUC0–72 h (μM·h) | AUC0–672 h (μM·h) | AUClast (μM·h) | AUCinf (μM·h) | Cmax (μM) | Tmax (h) | t1/2 (h) | % of AUCinf on day 3 | % of AUCinf on day 28 | mean F%b |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 31 | 6 | 0.02 | 0.738 ± 0.037 | 15.8 ± 5.3 | 50.2 ± 3.6 | 53.2 ± 2.9 | 0.050 ± 0.006 | 728 ± 194 | 421 ± 95 | 1.1 | 16 | 47 ± 3 |
| 32 | 12 | 0.04 | 6.02 ± 2.90 | 101 ± 69 | 166 ± 11 | 233c | 0.267 ± 0.176 | 296 ± 231 | 620c | 3.0 | 50 | 103c |
a
Values are the mean ± SD from 3 animals. AUC0–72 h = 3-day AUC; AUC0–672 h = 28-day AUC; SD = standard deviation.
b
F% = Total fraction dose released = 100 × dose-normalized SC AUCinf-to-IV AUCinf ratio.
c
Terminal slope defined in two animals; only mean value reported.