TABLE 1

In vitro inhibition (IC50 or Ki) of selected compounds on human OCT2, MATE1, MATE2K, OAT2, and OCT3

InhibitorsOCT2 IC50 or Ki (µM)MATE1 IC50 or Ki (µM)MATE2K IC50 or Ki (µM)OAT2 IC50 or Ki (µM)OCT3 IC50 or Ki (µM)
Probe Metformin (10 µM)aReported in the LiteraturebProbe Metformin (5 µM)aReported in the LiteraturebProbe Metformin (5 µM)aReported in the LiteraturebReported in the LiteraturebReported in the Literatureb
Cimetidine2.9 ± 0.716.6–16500.6 ± 0.050.2–16.35.6 ± 0.72.1–46.622–72.89.8–111
Pyrimethamine0.61 ± 0.044.8–23.60.02 ± 0.0020.077–0.630.045 ± 0.0030.046–0.52
Famotidine21.6 ± 3.436.1–18000.45 ± 0.030.6–0.766.6 ± 0.99.7–36.26.7–14
Ranitidine11.7 ± 1.330.5–798.2 ± 0.68.3–25.421 ± 22562–290
Trimethoprim19.8 ± 1.513.2–13270.51 ± 0.033.31–29.10.14 ± 0.020.61–28.9NI12.3
Dronedarone1.9 ± 0.30.46 ± 0.028.9 ± 1.7
DX-6190.94–1.290.82–4.320.1
Dolutegravir0.21 ± 0.040.066–1.933.6 ± 0.74.6712.5 ± 1.6>100>100>100
Cobicistat37.9 ± 4.98.24–330.98 ± 0.190.99–1.8720.5 ± 3.033.5>100>100
Ritonavir24.8 ± 3.420–250.28 ± 0.050.08–15.440.1 ± 6.523.7>20300
Ranolazine47 ± 916.8 ± 1.550 ± 8
Rilpivirine0.38 ± 0.055.130.25 ± 0.040.28 ± 0.08
Amiodarone4.7 ± 1.1>10001.0 ± 0.2>50>1000
Raltegravir>100>100>100>100>100>100
Telaprevir>1006.3562 ± 522.98>100
Vandetanib0.4 ± 0.055.5–73.40.06 ± 0.010.16–1.230. 04 ± 0.010.3–1.26
  • —, Data are not reported or available; NI, no inhibition.

  • a Data generated at Merck & Co. for inhibition of OCT2, MATE1, and MATE2K using metformin as the probe substrate in CHO-K1-OCT2, CHO-K1-MATE1, and MDCKII-MATE2K cells using the method described by Rizk et al. (2014).

  • b Data obtained from the University of Washington DDI database (https://www.druginteractioninfo.org).