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Table 2 Modeled Human Pharmacokinetic Parameters and JAK1/3 and JAK2 IC50 Coverage for CP-690,550

From: Anti-inflammatory activity and neutrophil reductions mediated by the JAK1/JAK3 inhibitor, CP-690,550, in rat adjuvant-induced arthritis

BID Dose mg Cmax
(nM)
24 hr AUC
(nM*h)
JAK1/3 IC50Coverage Every
12 hrsA
(rangeB)
JAK2 IC50Coverage Every
12 hrsC, D
(range)
5 167 1548 7.8 hrs (7.0-8.8) 0 hrsC (0-0)
0 hrsD
10 337 3097 10.3 hrs (9.6-11.3) 0 hrs (0-0)
0.3 hrs
15 503 4645 11.7 hrs (10.9-12.0) 0 hrs (0-0)
2.1 hrs
30 1006 9291 12.0 hrs (12.0-12.0) 0 hrs (0-0)
5.0 hrs
  1. A JAK1/3 human whole blood IC50 (IL-21 dependent pSTAT3) = 25 ± 6 nM; B range based on the upper and lower error around the IC50 where available; C JAK2 human whole blood IC50 (GM-CSF dependent pSTAT5) = 1377 ± 185 nM; D GM-CSF stimulated myelomonocytic HUO3 cell JAK2 IC50 = 324 nM [1].