Metronidazole is an effective inhibitor of OAT3 with IC50 of 6.51 +/- 0.99 µM, Ki of 6.48 µM [1]. Also as a nitroimidazole antibiotic medication, metronidazole is used targeting anaerobic bacteria and protozoa [2].Human Organ anion/cation transporters (OATs) are important membrane transporters, which are responsible for the cellular influx of drugs in human key tissues. Inhibitors affecting the cellular intake of transporter could make dysfunction of transporters, causing drug-drug interactions (DDIs) and bring poor effect and /or side reactions.Transport functional assay indicated that Metronidazole potently inhibited the transport activity of OAT3 with IC50 of 6.51 +/- 0.99 µM, Ki of 6.48 µM. Metronidazole could also reduce methotrexate influx via OATs and OATP1A2 consistently [1].Reference:[1]. Lu X, Chan T, Zhu L, et al. The inhibitory effects of eighteen front-line antibiotics on the substrate uptake mediated by human Organic anion/cation transporters Organic anion transporting polypeptides and Oligopeptide transporters in in vitro models [J]. European Journal of Pharmaceutical Sciences. 2018, 115(30): 132-143.[2]. Scully BE. Metronidazole. Medical Clinic of North America. 1988, 72(3): 613-621.
