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Table 2 Pharmacokinetic profiles of CatK inhibitors in rabbits[13, 25]

From: Cathepsin K inhibitors increase distal femoral bone mineral density in rapidly growing rabbits

Compound Dose (mg/kg) AUC (μm*hr) Cmax(nM) Cmin(nM) Cl (mL/min/kg) [Cmin]/bone res IC50 IC50(nM)
        Rabbit CatK Rabbit bone resorption assay
L-833905 10 1.9 163 29 0.2 33 ± 2 149 ± 20
  30 6.1 651 60 0.4   
L-006235 1 0.3 74 9 113 1.8 0.5 5 ± 1
  3 1.0 337 15 3.0   
  10 5.0 2436 8 1.6   
L-873724 1 0.5 78 <LOD* 26 ≤0.1 0.8 13 ± 1
  3 3.1 490 28 2.2   
  10 7.8 1370 32 2.5   
ODN 0.3 0.7 33 35 6 1.5 1.0 23 ± 6
  1 2.2 130 37 1.6   
  3 4.1 270 88   3.8   
  1. * ~ 1 nM.
  2. AUC = area under the curve, CatK = Cathepsin K, Cl = clearance, Cmax = maximum concentration after dosing, Cmin = minimum concentration after dosing, IC50 = half maximal inhibitory concentration, LOD = limit of detection, ODN = odanacatib, res = resorption.
  3. Reprinted (adapted) with permission from Falgueyret et al. 2005 [13].
  4. Reprinted (adapted) with permission from Gauthier et al. 2008 [25].