Aims DWP16001 is a novel sodium–glucose cotransporter 2 inhibitor for the treatment of type 2 diabetes with selective and sustained sodium–glucose cotransporter 2 inhibition. We aimed to evaluate whether the coadministration of DWP16001 and metformin causes any changes in pharmacokinetics (PK) or pharmacodynamics (PD). Methods A randomized, open‐label, single‐ and multiple‐dose, 2‐sequence, crossover study was conducted in healthy male subjects. Subjects received the following treatments: a single oral dose of DWP16001 (DWP) 2 mg, metformin immediate release 1000 mg (MET) twice daily for 7 days and a single oral dose of DWP and MET at steady‐state for metformin (DWP+MET). Serial blood and interval urine were collected for PK and PD analyses. Safety and tolerability profiles were assessed throughout the study. Results DWP+MET displayed increased peak concentration and area under the concentration–time curve from time 0 to time of the last quantifiable concentration compared with DWP (per standard bioequivalence boundaries, 0.8–1.25); the geometric mean ratios (GMRs) and their 90% confidence intervals (CIs) were 1.22 (1.13–1.31) and 1.09 (1.05–1.14), respectively. DWP+MET and MET showed similar peak concentration and area under the concentration–time curve within a dosing interval at steady state for metformin; the GMRs and 90% CIs were 0.98 (0.90–1.06) and 1.05 (0.98–1.13), respectively. The amount of urinary glucose excretion from time 0 to 144 h was also comparable between DWP+MET and DWP (GMR and 90% CI; 0.99, 0.94–1.05). Conclusion The results suggest that DWP16001 and metformin could be coadministered without clinically relevant PK and PD interactions.