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Table 2 Pharmacokinetic comparison of tafenoquine (TQ) and primaquine (PQ) in plasma and liver tissue following single intravenous at dose of 5 mg/kg and intragastric at dose of 20 mg/kg administrations in male mice (n = 3)

From: Assessment of the prophylactic activity and pharmacokinetic profile of oral tafenoquine compared to primaquine for inhibition of liver stage malaria infections

PK parameters Tafenoquine (TQ) Primaquine (PQ)
  Plasma Liver Plasma Liver
Intravenous (5 mg/kg)     
Cmax (μg/mL or g) 0.66 ± 0.13 44.76 ± 29.95 1.21 ± 0.21 3.99 ± 0.53
Tmax (hours) 1.36 ± 1.11 3.69 ± 2.29 0.08 ± 0.0 0.39 ± 0.53
AUClast (μg · h/mL or g) 29.63 ± 6.74 2493.82 ± 1361.10 1.20 ± 0.13 6.06 ± 1.39
AUCinfininty (μg · h/mL or g) 30.14 ± 6.65 2544.96 ± 1348.03 1.26 ± 0.14 6.14 ± 1.38
t1/2 elimination (h) 66.28 ± 10.32 70.02 ± 4.35 0.63 ± 0.08 1.32 ± 0.06
Vz (liter/kg) 16.76 ± 6.44 - 3.85 ± 0.71 -
Cl (liter/h/kg) 0.17 ± 0.04 - 4.19 ± 0.42 -
MRT (h) 55.92 ± 3.86 66.11 ± 19.19 0.68 ± 0.02 1.27 ± 0.11
AUCinf ratio (liver/plasma) - 87.24 ± 44.29 - 3.91 ± 0.54
Intragastric (20 mg/kg)     
Cmax (μg/mL) 2.04 ± 0.59 56.90 ± 26.09 0.53 ± 0.07 8.15 ± 0.29
Tmax (hours) 11.33 ± 5.37 1.17 ± 0.76 0.50 ± 0.0 0.50 ± 0.0
AUClast (μg · h/mL) 137.91 ± 24.38 5140.52 ± 1794.60 1.26 ± 0.40 27.45 ± 1.84
AUCinfininty (μg · h/mL) 139.18 ± 24.92 5391.86 ± 1898.51 1.31 ± 0.41 27.67 ± 1.75
t1/2 elimination (h) 50.87 ± 4.23 75.48 ± 12.06 1.84 ± 0.45 4.28 ± 1.30
Vz (liter/kg) 10.60 ± 1.22 - 154.66 ± 61.83 -
Cl (liter/h/kg) 0.15 ± 0.03 - 57.94 ± 20.52 -
MRT (h) 62.08 ± 2.30 88.67 ± 12.98 2.28 ± 0.10 4.49 ± 0.25
AUCinf ratio (liver/plasma) - 48.91 ± 22.67 - 22.26 ± 6.73
Absolute bioavailability (%) 100.77 ± 37.49   28.32 ± 6.93  
  1. Vz = Volume of distribution based on the terminal phase; MRT = mean residence time, D = Day.