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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.
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Malaria Journal

ISSN: 1475-2875

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