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Table 2 Calculated DDI indices of the four most potent OCT2 inhibitors

From: Proguanil and cycloguanil are organic cation transporter and multidrug and toxin extrusion substrates

Compound name

Cmax (ng/mL)a

Cmax (µM)

Unbound fraction

IC50 (µM)

DDI indexb

Amodiaquine

5.2c [45]

0.015

0.1 [46]

11

0.0001

Proguanil

306d [47]

1.2

0.25 [39]

13

0.02

Pyrimethamine

281e [48]

1.1

0.06 [49]

1.6

0.04

Quinine

11430f [50]

35

0.11g [36]

3.4

1.1

  1. a(Geometric) mean or median maximum plasma concentrations as determined in in vivo pharmacokinetic studies
  2. bDDI index calculated by dividing the unbound Cmax by the IC50 concentration. A DDI index cut-off value ≥ 0.1 is believed to indicate the requirement for future in vivo pharmacokinetic studies [18]
  3. cIn Ugandan children aged 5–13 years with uncomplicated malaria
  4. dIn Thai children with uncomplicated multidrug-resistant falciparum malaria
  5. eIn patients with acute falciparum malaria
  6. fIn adult patients with uncomplicated falciparum malaria
  7. gIn Thai patients with falciparum malaria