Skip to main content

Table 8 Rat pharmacokinetic parameters of S733 and SJ311 after oral administration

From: Selecting an anti-malarial clinical candidate from two potent dihydroisoquinolones

  (+)-SJ733 (+)-SJ311
Dose (mg/kg) 19.9 ± 0.2 50 100 200 20.9, 20.4a 50 100 200
Formulation Solution Suspension Suspension Suspension Suspension Suspension Suspension Suspension
Half life (h) 8.0 ± 0.6 7.7 ± 3.2 10.3 ± 6.9 7.7 ± 3.3 7.9, 7.9 3.5 ± 0.4 4.3 ± 2.2 4
Cmax (µM) 11.6 ± 2.1 11.1 ± 1.2 16.6 ± 3.2 27.9 ± 3.8 4.7, 5.0 4.4 ± 2.0 7.1 ± 0.81 9.4 ± 5.4
Tmax (h) 3.0 ± 0.9 4 3.0 ± 1.7 4.0 ± 3.5 1.0, 2.5 1.2 ± 0.8 4 3.2 ± 4.2
AUCinf (h µM) 76.1 ± 5.6 96.3 ± 5.8 180 ± 23.2 330 ± 78.4 26.5, 27.1 34.1 ± 8.7 61.9 ± 11.5 65.8 ± 12.6
CL/F (L/h/kg) ND 1.1 ± 0.1 1.2 ± 0.1 1.3 ± 0.3 1.6, 1.7 3.4 ± 1.0 3.6 ± 0.7 6.7 ± 0.5
V/F(L/kg) 12 ± 5.0 17 ± 9.0 15 ± 9.0 19.6, 18.7 17 ± 7.0 21 ± 8.0 38
F% 122 ± 10 74.5 69.6 63.8 38.0, 39.9 20.5 18.6 9.9
Dose in urine (%) 2.8 ± 1.0 ND 0.2 ± 0.1 14.9, 10.7 ND 1.1 ± 0.4
  1. an = 2; for all other PK studies, data are presented as mean ± SD (n = 3). AUC = AUCinf and was used to calculate F%. ND = not determined
\