TABLE 1

Plasma PK parameters for KAE609 in the presence and absence of piperaquine

ParameterValue for treatment group receiving:
75 mg KAE609 + 320 mg PPQ (n = 25)a25 mg KAE609 + 1,280 mg PPQ (n = 24)25 mg KAE609 (n = 25)b
Cmax (mean ± SD [%CV]) (ng/ml)760 ± 176 (23.2)226 ± 60.0 (26.6)269 ± 57.5 (21.3)
Tmax (median [range]) (h)3.00 (1.00–46.5)3.00 (2.00–6.00)3.00 (1.00–12.0)
AUC0–24 (mean ± SD [%CV]) (μg · h/ml)9.35 ± 1.90 (20.4)2.77 ± 0.80 (28.7)2.93 ± 0.70 (23.9)
AUClast (mean ± SD [%CV]) (μg · h/ml)18.6 ± 5.53 (29.8)5.87 ± 3.97 (67.6)5.35 ± 1.44 (26.8)
AUCinf (mean ± SD [%CV]) (μg · h/ml)18.6 ± 5.55 (29.8)6.10 ± 4.54 (74.5)5.42 ± 1.45 (26.7)
t1/2 (mean ± SD [%CV]) (h)24.4 ± 6.82 (28.0)26.4 ± 13.0 (49.1)25.2 ± 9.12 (36.2)
Vz/F (mean ± SD [%CV]) (liters)149 ± 46.4 (31.2)172 ± 56.9 (33.1)170 ± 49.3 (28.9)
CL/F (mean ± SD [%CV]) (liters/h)4.34 ± 1.16 (26.6)5.01 ± 1.76 (35.1)4.98 ± 1.53 (30.7)
  • a n = 23 for AUClast, AUCinf, t1/2, and Vz/F.

  • b n = 24 for AUClast, AUCinf, t1/2, and Vz/F.