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. 2014 Apr 14;13:143. doi: 10.1186/1475-2875-13-143

Table 7.

Pharmacokinetics of test compounds in Plasmodium falciparum -infected humanized mice

Compound Target dose (mg/kg) C max (μg/mL) t max (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)

NA, not available; DNAUC, dose-normalized value of AUC(0–t).

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.

aNote that the experimental doses were 6.4 and 15.0 mg/kg (versus target doses of 10 and 30 mg/kg, respectively).

bNote that the experimental doses were 8.3 and 22.0 mg/kg (versus target doses of 10 and 30 mg/kg, respectively).

cNote that the experimental dose was 36 mg/kg (versus target dose of 50 mg/kg).

Study performed by GlaxoSmithKline.

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