Table 8 In vitro metabolism in human liver microsomes

Ionized or partially ionized bases at physiological pH

 Cycloguanil

< 7^b

< 9.72^c

 Doxycyclin

< 7^b

< 7.53^c

 Pyronaridine

8.6

29.7

 Proguanil

< 7^b

< 21.2^c

 Primaquine

7.70

13.8

 Chloroquine

< 7^b

< 14^c

 Chlorproguanil

< 7^b

< 135^c

 Azithromycin

< 7^b

< 10^c

 AQ-13

< 7^b

< 10.6^c

 Desethylamodiaquine

13.3

CND^d

 Quinine

16.5

28.9

 Clindamycin

32.0

47.8

 KAF156

14.7

105

 M5717

11.1

22.2

 OZ277

< 7^b

< 159

 Mefloquine

< 7^b

< 140^c

 Amodiaquine

308

339

 NPC1161B

< 7^b

CND

 Ferroquine

29.2

108

 Naphthoquine

14.4

68.6

 Tafenoquine

< 7^b

< 3500^c

 MMV253

13.2

120

 MMV052

13.0

13,000

 Piperaquine

20.1

1540

 Halofantrine

26.9

13,500

 TDD-E209

25.5^e

85,000

 Lumefantrine

< 7^b

CND^d

Ionized acids at physiological pH

 Sulfadoxine

< 7^b

< 7.53

 Sulfamethoxazole

< 7^b

< 7.00

 Artesunate

146

CND^d

 Atovaquone

< 7^b

< 3500^c

Zwitterionic or partially zwitterionic at physiological pH

 P218

< 7^b

< 7.95^c

 JPC3210

9.50

328

Neutral at physiological pH

 Dapsone

< 7^b

< 8.14^c

 Dihydroartemisinin

16.6

19.1

 DSM421

< 7^b

< 9.09^c

 Pyrimethamine

< 7^b

< 13^c

 MMV048

< 7^b

< 11.5^c

 Artemisone

97.7

222

 Artemether

163

326

 SJ733

142

245

 DSM265

< 7^b,e

< 25^c

 KAE609

24.1

1270

 OZ439

72.1

72,100

 ELQ300

< 7^b

< 3500^c