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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