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

Table 2. PK Parameters of LEN Following Subcutaneous Administration of LEN in Aqueous Suspension to Male WH Ratsabcde.

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 F%e
1 10 0.10 32.5 + 20.8 194 + 14 236 + 36 236 + 36 0.671 + 0.198 25 + 23 219 + 81 14 82 118 ± 18
2 30 0.30 20.6 ± 3.9 343 ± 63 663 ± 83 664 ± 83 0.724 ± 0.222 224 ± 97 263 ± 31 3 52 110 ± 14
3 100 1.0 68.0 ± 27.2 900 ± 89 1545c 1554c 1.91 ± 0.33 224 ± 97 397c 4 58c 78c
4 200 1.0 × 2d 180 ± 93 1498 ± 223 2499 ± 188 2517 ± 194 3.81 ± 1.08 120 ± 83 403 ± 50 7 60 63 ± 5
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.

c

Only mean value was reported because one animal died at 2112 h postdose. This animal had appeared normal at the daily regular check time of 2088 h.

d

Two injections, each at a distinct site.

e

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