Canagliflozin, a sodium glucose co-transporter 2 inhibitor, improves model-based indices of beta cell function in patients with type 2 diabetes

Diabetologia. 2014 May;57(5):891-901. doi: 10.1007/s00125-014-3196-x. Epub 2014 Mar 1.

Abstract

Aims/hypothesis: In rodent models of diabetes, treatment with sodium glucose co-transporter 2 (SGLT2) inhibitors improves beta cell function. This analysis assessed the effects of the SGLT2 inhibitor, canagliflozin, on model-based measures of beta cell function in patients with type 2 diabetes.

Methods: Data from three Phase 3 studies were analysed, in which: (Study 1) canagliflozin 100 and 300 mg were compared with placebo as monotherapy for 26 weeks; (Study 2) canagliflozin 100 and 300 mg were compared with placebo as add-on to metformin + sulfonylurea for 26 weeks; or (Study 3) canagliflozin 300 mg was compared with sitagliptin 100 mg as add-on to metformin + sulfonylurea for 52 weeks. In each study, a subset of patients was given mixed-meal tolerance tests at baseline and study endpoint, and model-based beta cell function parameters were calculated from plasma glucose and C-peptide.

Results: In Studies 1 and 2, both canagliflozin doses increased beta cell glucose sensitivity compared with placebo. Placebo-subtracted least squares mean (LSM) (SEM) changes were 23 (9) and 18 (9) pmol min(-1) m(-2) (mmol/l)(-1) with canagliflozin 100 and 300 mg, respectively (p < 0.002, Study 1), and 16 (8) and 10 (9) pmol min(-1) m(-2) (mmol/l)(-1) (p < 0.02, Study 2). In Study 3, beta cell glucose sensitivity was minimally affected, but the insulin secretion rate at 9 mmol/l glucose increased to similar degrees from baseline with canagliflozin and sitagliptin [LSM (SEM) changes 38 (8) and 28 (9) pmol min(-1) m(-2), respectively; p < 0.05 for both].

Conclusions/interpretation: Treatment with canagliflozin for 6 to 12 months improved model-based measures of beta cell function in three separate Phase 3 studies.

Trial registration: Clinicaltrials.gov NCT01081834 (Study 1); NCT01106625 (Study 2); NCT01137812 (Study 3).

Publication types

  • Clinical Trial, Phase III
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Blood Glucose / analysis
  • C-Peptide / blood
  • Canagliflozin
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Diabetes Mellitus, Type 2 / physiopathology*
  • Double-Blind Method
  • Female
  • Glucosides / therapeutic use*
  • Humans
  • Insulin-Secreting Cells / drug effects*
  • Least-Squares Analysis
  • Male
  • Metformin / administration & dosage
  • Middle Aged
  • Pyrazines / administration & dosage
  • Sitagliptin Phosphate
  • Sodium-Glucose Transporter 2 / metabolism
  • Sulfonylurea Compounds / administration & dosage
  • Thiophenes / therapeutic use*
  • Time Factors
  • Triazoles / administration & dosage

Substances

  • Blood Glucose
  • C-Peptide
  • Glucosides
  • Pyrazines
  • SLC5A2 protein, human
  • Sodium-Glucose Transporter 2
  • Sulfonylurea Compounds
  • Thiophenes
  • Triazoles
  • Canagliflozin
  • Metformin
  • Sitagliptin Phosphate

Associated data

  • ClinicalTrials.gov/NCT01081834
  • ClinicalTrials.gov/NCT01106625
  • ClinicalTrials.gov/NCT01137812