Examples of transporter-related DDIs involving OCT2, MATE1, and/or MATE2K and correlation with transient elevation of SCr

PerpetratorPerpetrator Dose RegimenVictimVictim Dose Regimen% Change in AUC% Change in Renal CLElevation of SCr and/or % Decrease of CLcrReferences
Cimetidine400 mg QID (8 days)Gabapentin1200 mg QD [4 days]23.7−17.8Yes; CLcr↓10%Lal et al., 2010
Cimetidine800 mg BID (6 days)Glycopyrronium100 μg inhalation SD19.2−22.1Dumitras et al., 2013
Cimetidine400 mg BID (6.5 days)Metformin500 mg SD54.2−44.6No; CLcr NSWang et al., 2008
Cimetidine400 mg BID (5 days)Metformin250 mg QD (10 days)46.2−28.3NoaSomogyi et al., 1987
Cimetidine300 mg TID (5 days)Varenicline2 mg SD29.7−25.1Yes; CLcr↓5-10%Feng et al., 2008
Dolutegravir50 mg BID (7 days)Metformin500 mg BID (12 days)145Yes; SCr ↑Zong et al., 2014
Pyrimethamine50 mg SDMetformin250 mg SD35.3−35Yes; CLcr↓20%Kusuhara et al., 2011
Ranitidine150 mg BIDProcainamide1 g SD13.7−18.5Somogyi and Bochner, 1984
Ranitidine150 mg BID (4 days)Triamterene100 mg/day QD (8 days)−24−51No; NS ClcrMuirhead et al., 1988
Trimethoprim200 mg TID (6 days)Metformin500 mg TID (10 days)37−32Yes; CLcr↓20%; SCr ↑23%Grun et al., 2013
Trimethoprim200 mg TID(5 days)Metformin850 mg QD (2 doses)29.5−26.4Yes; CLcr↓16.9%Muller et al., 2015
Vandetanib100 mg QD (three 21-day cycles)Cisplatin75 mg/m2 SD (three 21-day cycles)32.7Blackhall et al., 2010
Vandetanib800 mg SDMetformin1000 mg SD73.3−52Yes; SCr ↑ 8-29%Johansson et al., 2014
  • —, Data are not reported or available; AUC, area under the curve; BID, twice daily; NS, not significant statistically; QID, four times a day; SD, single dose; TID, three times a day.

  • a A time-dependent variation of SCr was observed.