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Table 7 Whole blood to plasma partitioning

From: An in vitro toolbox to accelerate anti-malarial drug discovery and development

Compound

B/Pa

Haematocrit (Gender)

Ionized or partially ionized bases at physiological pH

 Cycloguanil

0.71 ± 0.07

0.48 (M)

 Doxycyclin

0.78 ± 0.06

0.43 (M)

 Pyronaridine

9.0 ± 0.83

0.48 (M)

 Proguanil

3.30 ± 0.14

0.46 (M)

 Primaquine

0.82 ± 0.07

0.44 (M)

 Chloroquine

3.5 ± 0.09

0.42 (F)

 Chlorproguanil

3.3 ± 0.38

0.43 (M)

 Azithromycin

1.6 ± 0.19

0.48 (M)

 AQ-13

3.15 ± 0.20

0.42 (M)

 Desethylamodiaquine

3.26 ± 0.35

0.50 (M)

 Quinine

0.67 ± 0.02

0.44 (M)

 Clindamycin

0.61 ± 0.04

0.42 (M)

 KAF156

1.3 ± 0.02

0.42 (F)

 M5717

1.3 ± 0.02

0.42 (F)

 OZ277

1.10 ± 0.10

0.46 (M)

 Mefloquine

1.1 ± 0.07

~ 0.43 (M)

 Amodiaquine

1.1 ± 0.18

~ 0.43 (M)

 NPC1161B

1.09 ± 0.07

0.44 (M)

 Ferroquine

1.6 ± 0.15

~ 0.43 (M)

 Naphthoquine

1.14 ± 0.10

~ 0.43 (M)

 Tafenoquine

1.3 ± 0.04

~ 0.43 (M)

 MMV253

1.0 ± 0.05

~ 0.43 (M)

 MMV052

1.6 ± 0.14

~ 0.43 (M)

 Piperaquine

0.57 ± 0.05

~ 0.43 (M)

 Halofantrine

0.68 ± 0.06

0.43 (M)

 TDD-E209

0.51 ± 0.08

0.44 (M)

 Lumefantrine

0.48 ± 0.09

0.48 (M)

Ionized acids at physiological pH

 Sulfadoxine

0.57 ± 0.03

0.46 (M)

 Sulfamethoxazole

0.65 ± 0.07

0.43 (M)

 Artesunate

CNDb

0.44 (M)

 Atovaquone

0.52 ± 0.03

0.44 (M)

Zwitterionic or partially zwitterionic at physiological pH

 P218

0.56 ± 0.03

~ 0.43 (M)

 JPC3210

0.54 ± 0.04

~ 0.43 (M)

Neutral at physiological pH

 Dapsone

1.1 ± 0.06

0.43 (M)

 Dihydroartemisinin

CNDb

0.42 (M)

 DSM421

0.53 ± 0.03

0.44 (M)

 Pyrimethamine

0.84 ± 0.03

0.43 (M)

 MMV048

0.77 ± 0.03

0.42 (F)

 Artemisone

CNDb

0.44 (M)

 Artemether

CNDb

0.42 (M)

 SJ733

0.72 ± 0.02

0.42 (F)

 DSM265

0.54 ± 0.02

0.44 (M)

 KAE609

0.66 ± 0.04

0.42 (F)

 OZ439

0.78 ± 0.05

0.44 (M)

 ELQ300

0.53 ± 0.05

0.44 (M)

  1. aMean ± SD, n = 3–4 measurements
  2. bCND = could not determine, unstable in blood and plasma