Introduction <p>Olorigliflozin, a selective sodium-glucose cotransporter 2 inhibitor, is in development for the treatment of type 2 diabetes mellitus (T2DM).</p> Objective <p>This trial aimed to assess the pharmacokinetics, pharmacodynamics, and safety of olorigliflozin capsules by comparing results in patients with T2DM with normal renal function and in those with mild and moderate impairment.</p> Materials and methods <p>This study administered olorigliflozin 50 mg to 32 Chinese patients with T2DM from a single medical center, of whom 16 showed no renal impairment, eight showed mild impairment, and eight showed moderate impairment. Those with mild impairment were matched to eight without impairment based on sex, age, and body mass index, whereas those with moderate impairment were matched to the remaining eight without impairment.</p> Results <p>All 32 participants completed the study. Compared with normal renal function, patients with mild renal impairment had 15.42% higher maximum plasma concentration and 16.22% higher area under the curve from time zero to time t (AUC_0–<i>t</i>), a clinically non-significant difference, with similar geometric mean AUC extrapolated from time zero to infinity (AUC_0–∞). Moderate renal impairment showed 56.71% higher AUC_0–<i>t</i> and 62.27% higher AUC_0-∞ but comparable maximum plasma concentration. Time to maximum plasma concentration was consistent across groups. Both renal impairment groups had decreased renal excretion. At 24 h post-dose, urinary glucose excretion increased: mild renal impairment (14.31–52.31 g) versus matched control (34.32–98.14 g), moderate renal impairment (5.94–38.45 g) versus matched control (9.85–72.83 g), yet absolute levels remained lower in the renal impairment groups. Adverse events (all grade 1–2) had similar rates.</p> Conclusions <p>Olorigliflozin capsules (50 mg) may be safe and effective for individuals with T2DM who show no or mild renal impairment, but they may be inappropriate for those who show moderate impairment.</p>