Functional imaging of pharmacological action of SGLT2 inhibitor ipragliflozin via PET imaging using ¹¹C‐MDG

Sodium‐dependent glucose cotransporter 2 (SGLT2) is a pharmacological target of type 2 diabetes mellitus. The aim of this study was to noninvasively visualize the pharmacological action of a selective SGLT2 inhibitor ipragliflozin in the kidney using positron emission tomography (PET) imaging with ¹¹C‐methyl‐d‐glucoside (¹¹C‐MDG), an SGLT‐specific radio‐labeled substrate. PET imaging with ¹¹C‐MDG in vehicle‐treated rats demonstrated that intravenously injected ¹¹C‐MDG substantially accumulated in the renal cortex, reflecting that the compound was reabsorbed by SGLTs. In contrast, ipragliflozin‐treated rats showed significantly lower uptake of ¹¹C‐MDG in renal cortex in a dose‐related manner, suggesting that ipragliflozin inhibited the renal reabsorption of ¹¹C‐MDG. This method of visualizing the mode of action of an SGLT2 inhibitor in vivo has demonstrated the drug's mechanism in reducing renal glucose reabsorption in kidney in living animals.

DOI: 10.1002/prp2.244

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