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Table 7 Pharmacokinetics of test compounds in Plasmodium falciparum -infected humanized mice

From: Repositioning: the fast track to new anti-malarial medicines?

Compound Target dose (mg/kg) Cmax(μg/mL) tmax(h) AUC(0–t)(μg · h · mL) DNAUC(0–t)(μg · h · mL−1 · day−1)
UK-112,214 100 8.61 (0.4) 4.0 (1.7) 72.1 (2.7) 0.859 (0.32)
UK-112,214 300 17.6 (6.4) 3.3 (4.0) 231 (101) 1.03 (0.45)
CEP-701a 10 0.63 (0.079) 0.78 (0.38) 2.8 (0.46) 0.44 (0.072)
CEP-701a 30 2.8 (0.84) 4.0 (1.7) 23.8 (6.8) 1.6 (0.47)
CEP-1347b 10 0.83 (0.44) 4.8 (4.0) 8.1 (1.8) 0.98 (0.22)
CEP-1347b 30 0.73 (0.20) 6.0 (NA) 9.9 (2.1) 0.45 (0.092)
PSC-833c 50 1.39 (0.20) 3.30 (1.2) 12.90 (2.97) 0.36 (0.082)
PSC-833 100 1.01 (0.53) 5.33 (3.05) 12.26 (4.25) 0.13 (0.04)
PSC-833 200 0.91 (0.47) 2 (0) 13.05 (6.05) 0.065 (0.03)
  1. NA, not available; DNAUC, dose-normalized value of AUC(0–t).
  2. Values are the mean (SD). Pharmacokinetics were estimated in whole blood after oral UK-112,214 and PSC-833 or subcutaneous CEP-701 and CEP-1347 administration to P. falciparum-infected humanized mice.
  3. aNote that the experimental doses were 6.4 and 15.0 mg/kg (versus target doses of 10 and 30 mg/kg, respectively).
  4. bNote that the experimental doses were 8.3 and 22.0 mg/kg (versus target doses of 10 and 30 mg/kg, respectively).
  5. cNote that the experimental dose was 36 mg/kg (versus target dose of 50 mg/kg).
  6. Study performed by GlaxoSmithKline.