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Table 3 PK parameters for KAF156 in the presence and absence of piperaquine

From: A phase 1 evaluation of the pharmacokinetic/pharmacodynamic interaction of the anti-malarial agents KAF156 and piperaquine

PK parametera (unit)

800 mg KAF156 + 1280 mg PPQ

N = 23 (mean, SD, CV%)

800 mg KAF156

N = 24 (mean, SD, CV%)

Cmax (ng/mL)

2270 ± 496 (21.8%) [n = 23]

1850 ± 401 (21.7%) [n = 24]

AUClast (h µg/mL)

48.2 ± 14.4 (30.0%) [n = 22]

44.4 ± 12.7 (28.7%) [n = 24]

AUCinf (h µg/mL)

50.1 ± 15.0 (29.9%) [n = 21]

46.2 ± 13.9 (30.0%) [n = 24]

AUC0-24 h (h µg/mL)

22.8 ± 5.41 (23.7%) [n = 22]

19.1 ± 4.86 (25.4%) [n = 24]

AUC0-72 h (h µg/mL)

38.2 ± 10.2 (26.6%) [n = 22]

33.0 ± 8.67 (26.2%) [n = 24]

AUC0-168 h (h µg/mL)

47.0 ± 13.7 (29.0%) [n = 21]

42.2 ± 11.8 (27.9%) [n = 24]

Tmax (h)

3.00 (2.00–4.02) [n = 23]

3.00 (2.00–6.00) [n = 24]

T1/2 (h)

52.4 ± 11.1 (21.2%) [n = 21]

57.9 ± 10.5 (18.2%) [n = 24]

CL/F (mL/h)

17,500 ± 5760 (32.9%) [n = 21]

18,700 ± 5210 (27.8%) [n = 24]

Vz/F (L)

1360 ± 689 (50.7%) [n = 21]

1530 ± 417 (27.2%) [n = 24]

  1. AUC0-t h, The area under the plasma concentration–time curve from time zero to time ‘t’ where t is a defined time point after administration
  2. AUCinf, The area under the plasma concentration–time curve from time zero to infinity
  3. AUClast, The area under the plasma concentration–time curve from time zero to the time of the last quantifiable concentration
  4. Cmax, The observed maximum plasma concentration following drug administration
  5. CL/F, The apparent systemic (or total body) clearance from plasma following extravascular administration
  6. T1/2, The terminal elimination half-life
  7. Tmax, The time to reach the maximum concentration after drug administration
  8. Vz/F, The apparent volume of distribution during the terminal elimination phase following extravascular administration
  9. aAll PK parameter values are presented as mean ± SD (CV %) [n] except Tmax which is presented as median (range) [n]. n is number of subjects providing reliable estimate of the parameter
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Malaria Journal

ISSN: 1475-2875

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