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

Table 4. PK Parameters of LEN Following Subcutaneous Administration of LEN in a PEG/Water Solution Formulation to Male WH Ratsabc.

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%c
21 50 0.12 7.86 ± 1.47 152 ± 49 774 ± 74 789 ± 61 0.469 ± 0.120 718 ± 257 1056 ± 504 0.68 13 79 ± 6
22 100 0.33 16.2 ± 6.2 216 ± 113 1330 ± 238 1340 ± 228 0.500 ± 0.138 1064 ± 257 1240 ± 281 0.71 9.4 67 ± 11
23 150 0.5 21.7 ± 3.6 282 ± 14 2160 ± 211 2190 ± 205 0.765 ± 0.092 1120 ± 194 1420 ± 403 0.63 8.2 73 ± 7
24 450 1.5 75.7 ± 12.1 926 ± 164 5360 ± 787 5400 ± 837 1.95 ± 0.306 840 ± 444 1330 ± 263 0.73 9.0 60 ± 9
25 200 0.33 × 2b 32.3 ± 4.7 507 gf± 147 2410 ± 60 2410 ± 60 1.09 ± 0.17 728 ± 256 647 ± 28 0.71 11 60 ± 1
26 300 0.5 × 2b 41.1 ± 1.3 550 ± 54 3630 ± 189 3660 ± 184 1.35 ± 0.09 896 ± 775 1110 ± 299 0.60 8.0 61 ± 3
27 900 1.5 × 2b 99.4 ± 22.2 1140 ± 239 8400 ± 1160 8620 ± 1250 2.22 ± 0.35 1288 ± 423 1360 ± 156 0.48 5.5 48 ± 7
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

Two injections, each at a distinct site

c

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