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. Author manuscript; available in PMC: 2017 Apr 1.
Published in final edited form as: Clin Pharmacokinet. 2016 Apr;55(4):495–506. doi: 10.1007/s40262-015-0332-9

Table 1.

In vitro potency of putative clinical inhibitors in cells expressing OCT1, OCT2, OCT3, MATE1, MATE2K and PMAT.

Drug Parameter OCT1 OCT2 OCT3 MATE1 MATE2K PMAT
moxifloxacin IC50 (μM) 47.0 >151 >151 5.12 1.19 >151
Cmax/IC50 0.13 <0.04 <0.04 1.22 5.22 <0.04
Cmax,u/IC50 0.08 <0.02 <0.02 0.74 3.16 <0.02
norfloxacin IC50 (μM) >160 >160 >160 19.9 4.74 >160
Cmax/IC50 <0.03 <0.03 <0.03 0.24 0.99 <0.03
Cmax,u/IC50 <0.02 <0.02 <0.02 0.20 0.84 <0.02
ondansetron IC50 (μM) >1.32 >1.32 >1.32 0.05 0.08 >1.32
Cmax/IC50 <0.10 <0.10 <0.10 2.47 1.57 <0.10
Cmax,u/IC50 <0.02 <0.02 <0.02 0.62 0.39 <0.02
ranitidine IC50 (μM) 26.8 15.7 93.5 4.04 4.63 >214
Cmax/IC50 0.24 0.40 0.07 1.56 1.36 <0.03
Cmax,u/IC50 0.20 0.34 0.06 1.33 1.16 <0.02
nizatidine IC50 (μM) >115 >115 41.1 52.7 7.81 >115
Cmax/IC50 <0.04 <0.04 0.11 0.08 0.56 <0.04
Cmax,u/IC50 <0.02 <0.02 0.07 0.05 0.37 <0.02

Cmax and calculated Cmax,u were obtained from literature values (see Supplemental Table 1). Cmax/IC50 and Cmax,u/IC50 values that exceed the 0.1 cut-off are bolded.

IC50, concentration at half the maximum inhibition of active transport; Cmax, maximum plasma concentration; Cmax,u, maximum plasma concentration that is not bound to plasma proteins; OCT, organic cation transporter; MATE, multidrug and toxin extrusion transporter; PMAT, plasma membrane monoamine transporter.