Aims: The primary aim of this study was to assess the individual effects of probenecid and cimetidine on mirogabalin exposure. Methods: This phase 1, open‐label, crossover study randomized healthy adults to receive three treatment regimens, each separated by ≥5‐day washout: a single oral dose of mirogabalin 15 mg on day 2, mirogabalin 15 mg on day 2 plus probenecid 500 mg every 6 h from days 1 to 4, and mirogabalin 15 mg on day 2 plus cimetidine 400 mg every 6 h from days 1 to 4. Results: Coadministration of mirogabalin with probenecid or cimetidine increased the maximum and total mirogabalin exposure. The geometric mean ratios of Cmax and AUC(0‐t) (90% CI) with and without coadministration of probenecid were 128.7% (121.9–135.7%) and 176.1% (171.9–180.3%), respectively. The geometric mean ratios of Cmax and AUC(0‐t) (90% CI) with and without coadministration of cimetidine were 117.1% (111.0–123.6%) and 143.7% (140.3–147.2%), respectively. Mean (standard deviation) renal clearance of mirogabalin (l h–1) was substantially slower after probenecid [6.67 (1.53)] or cimetidine [7.17 (1.68)] coadministration, compared with mirogabalin alone [11.3 (2.39)]. Coadministration of probenecid or cimetidine decreased mirogabalin mean (standard deviation) apparent total body clearance [10.5 (2.33) and 12.8 (2.67) l h–1, respectively, vs. 18.4 (3.93) for mirogabalin alone]. Conclusions: A greater magnitude of change in mirogabalin exposure was observed when coadministered with a drug that inhibits both renal and metabolic clearance (probenecid) vs. a drug that only affects renal clearance (cimetidine). However, as the increase in exposure is not clinically significant (>2‐fold), no a priori dose adjustment is recommended. [ABSTRACT FROM AUTHOR]