Steady-state Cmax values of the inhibitors of OCT1 and OCT2 compared with their IC50 values Reference for Cmax values: RxList, San Clemente, CA.
Compounds | Cmax, steady state | IC50 (OCT1) | IC50 (OCT2) | Application |
|---|---|---|---|---|
| μM | μM | μM | ||
| Indinavir | 12.6 ± 4 | 37 ± 6 | 275 ± 57 | p.o. 800 mg t.i.d. |
| Saquinavir | 0.29* | 37 ± 7 | 205 ± 29 | p.o. 600 mg t.i.d.** |
| Zalcitabine | 0.1 ± 0.04* | 24 ± 5 | 131 ± 12 | p.o. 1,5 mg |
| Trimethoprim | 6.8* | 20 ± 3 | 51 ± 22 | p.o. 200 mg |
| Lamivudine | 6.5 ± 2* | 17 ± 3 | 33 ± 11 | p.o. 2 mg/kg b.i.d. |
| Ritonavir | 15.5 ± 5* | 14 ± 2 | 25 ± 7 | p.o. 600 mg b.i.d. |
| Nelfinavir | 4.0 ± 0.8* | 7 ± 1 | 13 ± 3 | p.o. 1250 mg b.i.d. |
| Pentamidine | 0.5–0.8* | 0.4 ± 1 | 3.8 ± 1 | p.o. 4 mg/kg |