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. 2023 Nov 2;20(12):6213–6225. doi: 10.1021/acs.molpharmaceut.3c00626

Table 3. PK Parameters of LEN Following Subcutaneous Administration of LEN in an Aqueous Suspension Formulation to Male Beagle Dogsabcd.

group ID dose (mg/kg)b 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%d
11 3 0.03 3.0 ± 2.1 18.6 ± 9.0 25.4 ± 7.5 28.0 ± 6.4 0.056 ± 0.037 72 ± 83 525 ± 147 11 66 49 ± 11
12 6 0.06 20.8 ± 7.4 117 ± 37 128 ± 41 129 ± 42 0.410 ± 0.141 40 ± 28 322 ± 51 16 91 114 ± 37
13 6 0.03 × 2c 18.8 ± 2.4 85.0 ± 7.0 88.4 ± 6.2 88.9 ± 6.2 0.417 ± 0.014 64 ± 28 174 ± 38 21 96 78 ± 5
14 6 0.03 6.6 ± 3.4 63.9 ± 27.3 75.9 ± 34.6 79.1 ± 32.2 0.175 ± 0.068 96 ± 63 354 ± 329 8 96 70 ± 28
15 30 0.30 145 ± 9 496 ± 49 497 ± 51 497 ± 51 2.96 ± 0.30 40 ± 14 66 ± 5 29 100 88 ± 9
16 100 1.0 340 ± 76 1336 ± 504 1356 ± 500 1357 ± 500 7.24 ± 1.28 32 ± 14 94 ± 59 25 100 72 ± 26
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

Formulation concentration at 100 mg/mL LEN (groups 11–13; 15, 16) and at 200 mg/mL LEN (group 14).

c

Two injections, each at a distinct site.

d

F% = Total fraction dose released = 100 × dose-normalized SC AUCinf-to-IV AUCinf ratio.