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. 2023 Jun 12;39(5):332–346. doi: 10.1089/jop.2022.0184

Table 5.

Plasma Pharmacokinetic Parameters for QLS-101 and Levcromakalim in Beagle Dogs Dosed Topically with QLS-101 Eyedrops for 28 Days

QLS-101
Day Gender Dose (mg/eye/dose) Tmax (h) Cmax (ng/mL) tlast (h) AUC0–24h (h × ng/mL) T1/2 (h)
1 Male 0.8 1 (1–2) 36.5 ± 17.2 12 (12–12) 231 ± 108 3.69 ± ID
    1.6 1 (1–2) 73.7 ± 50.5 12 (12–24) 520 ± 274 4.26 ± ID
3.2 2 (2–2) 166 ± 32.0 24 (24–24) 1,520 ± 115 4.82 ± 0.872
Female 0.8 2 (2–2) 55.5 ± 26.5 12 (12–24) 496 ± 371 4.12 ± ID
  1.6 2 (2–2) 129 ± 39.7 24 (24–24) 1,220 ± 207 6.18 ± 1.37
3.2 2 (1–2) 156 ± 79.0 24 (12–24) 1,480 ± 832 4.92 ± 0.558
28 Male 0.8 1 (1–2) 47.0 ± 7.44 12 (12–12) 272 ± 24.1 3.44 ± 0.252
    1.6 1 (1–2) 57.3 ± 36.3 12 (12–12) 381 ± 180 3.32 ± ID
3.2 2 (2–2) 147 ± 37.9 24 (24–24) 1,260 ± 205 5.08 ± 1.23
Female 0.8 2 (1–2) 80.2 ± 14.0 12 (12–24) 545 ± 81.9 3.68 ± 1.17
  1.6 2 (2–2) 201 ± 105 24 (24–24) 1,750 ± 890 4.95 ± 0.654
3.2 2 (1–2) 139 ± 66.0 24 (24–24) 1,200 ± 462 5.15 ± 1.06
Levcromakalim
Day Gender Dose (mg/eye/dose) Tmax (h) Cmax (ng/mL) tlast (h) AUC0–24h (h × ng/mL) T1/2 (h)
1
 Male
 0.8
 2 (1–2)
 25.3 ± 5.05
 12 (8–12)
 99.8 ± 4.28
 3.64 ± ID
 
  
 1.6
 4 (2–4)
 24.4 ± 15.0
 12 (12–12)
 133 ± 51.0
 3.24 ± ID
3.2
 2 (2–2)
 76.0 ± 26.9
 24 (12–24)
 361 ± 105
 3.44 ± 0.10
Female
 0.8
 2 (2–2)
 25.1 ± 6.32
 12 (12–12)
 92.7 ± 8.00
 2.65 ± 1.05
 
 1.6
 2 (2–4)
 23.2 ± 6.76
 12 (12–24)
 125 ± 58.0
 3.61 ± ID
3.2
 2 (1–2)
 72.2 ± 42.5
 12 (12–24)
 294 ± 180
 2.73 ± 0.42
28
 Male
 0.8
 2 (2–4)
 10.6 ± 1.79
 12 (8–12)
 49.1 ± 7.85
 2.35 ± ID
   
 1.6
 2 (2–8)
 15.5 ± 12.7
 12 (12–12)
 70.7 ± 35.5
 3.12 ± ID
3.2
 2 (1–4)
 31.0 ± 13.0
 12 (12–24)
 166 ± 67.1
 3.38 ± 1.15
Female
 0.8
 2 (2–2)
 18.4 ± 3.55
 12 (8–12)
 80.1 ± 4.94
 2.51 ± ID
  1.6
 2 (2–4)
 19.9 ± 2.80
 12 (12–12)
 105 ± 6.57
 2.06 ± ID
3.2 2 (2–4) 32.9 ± 22.6 24 (12–24) 154 ± 76.5 4.90 ± 2.44