Physical storage of formulations may result in physical composition changes that affect pharmacokinetics. Dapagliflozin, an oral sodium-glucose cotransporter 2 inhibitor used for type 2 diabetes mellitus, stored under prolonged exposure to heat converts crystalline dapagliflozin to an amorphous form. Bioequivalence of the amorphous to crystalline form and food effects of each form in the 2.5-mg formulation are unknown. Two open-label, crossover, single-dose studies in healthy participants assessed pharmacokinetics for heat-stressed (HS) and non–heat-stressed (NH) dapagliflozin 10-mg (study 1, N = 29, fasted + HS food effect) and 2.5-mg (study 2, N = 28, fasted + HS and NH food effect) tablets. The 90% confidence intervals for geometric mean ratios of area under the concentration–time curve (AUC) and peak concentration (Cmax) for HS 2.5- and 10-mg tablets were within 80–125%, indicating bioequivalence. In the fed vs. fasted state for 2.5-mg and 10-mg HS tablets, AUCs were similar, time to Cmax was prolonged by 1.25 h, and Cmax decreased by approximately 50%. No serious adverse events were reported. Given that dapagliflozin's efficacy is dependent upon AUC, it was concluded that HS and NH dapagliflozin tablets are bioequivalent in 2.5- and 10-mg doses with no clinically meaningful food effect for either form.