Why do SGLT2 inhibitors inhibit only 30-50% of renal glucose reabsorption in humans?

Jiwen Liu, Tae Weon Lee, Ralph A. DeFronzo

Research output: Contribution to journalReview article

128 Scopus citations

Abstract

Sodium glucose cotransporter 2 (SGLT2) inhibition is a novel and promising treatment for diabetes under late-stage clinical development. It generally is accepted that SGLT2 mediates 90% of renal glucose reabsorption. However, SGLT2 inhibitors in clinical development inhibit only 30-50% of the filtered glucose load. Why are they unable to inhibit 90% of glucose reabsorption in humans? We will try to provide an explanation to this puzzle in this perspective analysis of the unique pharmacokinetic and pharmacodynamic profiles of SGLT2 inhibitors in clinical trials and examine possible mechanisms and molecular properties that may be responsible.

Original languageEnglish (US)
Pages (from-to)2199-2204
Number of pages6
JournalDiabetes
Volume61
Issue number9
DOIs
StatePublished - Sep 1 2012

ASJC Scopus subject areas

  • Internal Medicine
  • Endocrinology, Diabetes and Metabolism

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