TABLE 2

PK parameters for piperaquine in the presence and absence of KAE609

ParameterValue for treatment group receiving:
75 mg KAE609 + 320 mg PPQ (n = 25)a1,280 mg PPQ + 25 mg KAE609 (n = 24)b320 mg PPQ (n = 24)c1,280 mg PPQ (n = 12)d
Cmax (mean ± SD [%CV]) (ng/ml)24.2 ± 16.8 (69.4)299 ± 191 (63.7)20.4 ± 8.40 (41.2)219 ± 124 (56.6)
Tmax (median [range]) (h)3.00 (1.00–46.5)3.00 (2.00–6.00)3.00 (1.00–12.0)3.00 (1.00–4.00)
AUC0–24 (mean ± SD [%CV]) (μg · h/ml)0.27 ± 0.14 (53.0)2.30 ± 1.00 (43.2)0.243 ± 0.09 (38.9)1.84 ± 0.84 (45.8)
AUC0–168 (mean ± SD [%CV]) (μg · h/ml)0.84 ± 0.40 (47.4)5.15 ± 1.89 (36.8)0.850 ± 0.33 (38.2)4.15 ± 1.47 (35.4)
AUC0–672 (mean ± SD [%CV]) (μg · h/ml)1.72 ± 0.92 (53.4)8.49 ± 2.84 (33.5)1.74 ± 0.68 (39.4)6.70 ± 2.13 (31.8)
AUClast (mean ± SD [%CV]) (μg · h/ml)2.07 ± 1.28 (61.6)10.8 ± 3.53 (32.7)2.16 ± 0.98 (45.4)8.36 ± 2.64 (31.5)
AUCinf (mean ± SD [%CV]) (μg · h/ml)2.60 ± 1.49 (57.2)12.0 ± 3.70 (30.9)2.82 ± 1.13 (40.1)8.99 ± 2.86 (31.8)
t1/2 (mean ± SD [%CV]) (h)510 ± 339 (66.6)485 ± 113 (23.3)551 ± 284 (51.5)536 ± 172 (32.1)
Vz/F (mean ± SD [%CV]) (liters)99,300 ± 49,500 (49.9)83,400 ± 35,000 (41.9)96,700 ± 44,500 (46.0)125,000 ± 71,700 (57.5)
CL/F (mean ± SD [%CV]) (liters/h)155 ± 80.9 (52.4)120 ± 50.0 (41.7)131 ± 59.9 (45.6)155 ± 46.1 (29.8)
  • a n = 22 for AUClast, n = 21 for t1/2 and Vz/F, and n = 19 for AUCinf.

  • b n = 21 for AUClast, AUCinf, t1/2, and Vz/F.

  • c n = 22 for AUCinf, t1/2, and Vz/F.

  • d n = 9 for AUClast and n = 7 for AUCinf, t1/2, and Vz/F.