SGLT-2 inhibitors and their potential in the treatment of diabetes

Rebecca F Rosenwasser,1 Senan Sultan,2 David Sutton,2 Rushab Choksi,1 Benjamin J Epstein3 1East Coast Institute for Research, Jacksonville, FL, USA; 2Northeast Florida Endocrine and Diabetes Associates, Jacksonville, FL, USA; 3Department of Pharmacotherapy and Translational Research, University of F...

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Autores principales: Rosenwasser RF, Sultan S, Sutton D, Choksi R, Epstein BJ
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Publicado: Dove Medical Press 2013
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spelling oai:doaj.org-article:d53dfd6d79ef4ad3b1248865a63a3a152021-12-02T06:19:38ZSGLT-2 inhibitors and their potential in the treatment of diabetes1178-7007https://doaj.org/article/d53dfd6d79ef4ad3b1248865a63a3a152013-11-01T00:00:00Zhttp://www.dovepress.com/sglt-2-inhibitors-and-their-potential-in-the-treatment-of-diabetes-a15100https://doaj.org/toc/1178-7007Rebecca F Rosenwasser,1 Senan Sultan,2 David Sutton,2 Rushab Choksi,1 Benjamin J Epstein3 1East Coast Institute for Research, Jacksonville, FL, USA; 2Northeast Florida Endocrine and Diabetes Associates, Jacksonville, FL, USA; 3Department of Pharmacotherapy and Translational Research, University of Florida College of Pharmacy, Gainesville, FL, USA Abstract: Diabetes remains a burgeoning global problem, necessitating ongoing efforts on the part of pharmaceutical and device manufacturers, patients, and society to curb the frightening trends in morbidity and mortality attributable to the malady. Since 1835 when phlorizin was discovered, sodium glucose co-transporter 2 (SGLT-2) inhibitors have rested tantalizingly on the horizon, promising a more physiological approach to glucose control. These agents lower glucose by enhancing its excretion by blocking reabsorption in the renal tubules, thus eliminating glucose from the body along with the molecules' attendant effects on caloric balance, plasma osmolality, and lipids. Consequently, SGLT-2 inhibitors improve glucose control to an extent comparable to other hypoglycemic agents while simultaneously reducing body weight, blood pressure, and cholesterol – an admirable portfolio. One agent, canagliflozin, has recently been approved by the US Food and Drug Administration (FDA) and two other agents have progressed through Phase III trials, including dapagliflozin and empagliflozin. Collectively, when used as monotherapy, these agents have demonstrated reductions in hemoglobin A1c (HbA1c), body weight, and blood pressure of –0.34% to –1.03%, –2.0 to -3.4 kg, and –1.7 to –6.4 mmHg/–0.3 to –2.6 mmHg (systolic blood pressure/diastolic blood pressure), respectively. SGLT-2 inhibitors have been well tolerated, with hypoglycemia (0.9% to 4.3%) occurring infrequently in clinical trials. Safety signals related to breast and bladder cancer have arisen with dapagliflozin, though these are unsubstantiated and likely ascribed to the presence of preexisting cancer. As these agents emerge, clinicians should embrace the addition to the formulary for treating type 2 diabetes, but must also weight the risk–benefit of this new class in deciding which patient types are most likely to benefit from their novel mechanism of action. Keywords: diabetes, sodium–glucose transporter 2, canagliflozin, dapagliflozin, empagliflozinRosenwasser RFSultan SSutton DChoksi REpstein BJDove Medical PressarticleSpecialties of internal medicineRC581-951ENDiabetes, Metabolic Syndrome and Obesity: Targets and Therapy, Vol 2013, Iss default, Pp 453-467 (2013)
institution DOAJ
collection DOAJ
language EN
topic Specialties of internal medicine
RC581-951
spellingShingle Specialties of internal medicine
RC581-951
Rosenwasser RF
Sultan S
Sutton D
Choksi R
Epstein BJ
SGLT-2 inhibitors and their potential in the treatment of diabetes
description Rebecca F Rosenwasser,1 Senan Sultan,2 David Sutton,2 Rushab Choksi,1 Benjamin J Epstein3 1East Coast Institute for Research, Jacksonville, FL, USA; 2Northeast Florida Endocrine and Diabetes Associates, Jacksonville, FL, USA; 3Department of Pharmacotherapy and Translational Research, University of Florida College of Pharmacy, Gainesville, FL, USA Abstract: Diabetes remains a burgeoning global problem, necessitating ongoing efforts on the part of pharmaceutical and device manufacturers, patients, and society to curb the frightening trends in morbidity and mortality attributable to the malady. Since 1835 when phlorizin was discovered, sodium glucose co-transporter 2 (SGLT-2) inhibitors have rested tantalizingly on the horizon, promising a more physiological approach to glucose control. These agents lower glucose by enhancing its excretion by blocking reabsorption in the renal tubules, thus eliminating glucose from the body along with the molecules' attendant effects on caloric balance, plasma osmolality, and lipids. Consequently, SGLT-2 inhibitors improve glucose control to an extent comparable to other hypoglycemic agents while simultaneously reducing body weight, blood pressure, and cholesterol – an admirable portfolio. One agent, canagliflozin, has recently been approved by the US Food and Drug Administration (FDA) and two other agents have progressed through Phase III trials, including dapagliflozin and empagliflozin. Collectively, when used as monotherapy, these agents have demonstrated reductions in hemoglobin A1c (HbA1c), body weight, and blood pressure of –0.34% to –1.03%, –2.0 to -3.4 kg, and –1.7 to –6.4 mmHg/–0.3 to –2.6 mmHg (systolic blood pressure/diastolic blood pressure), respectively. SGLT-2 inhibitors have been well tolerated, with hypoglycemia (0.9% to 4.3%) occurring infrequently in clinical trials. Safety signals related to breast and bladder cancer have arisen with dapagliflozin, though these are unsubstantiated and likely ascribed to the presence of preexisting cancer. As these agents emerge, clinicians should embrace the addition to the formulary for treating type 2 diabetes, but must also weight the risk–benefit of this new class in deciding which patient types are most likely to benefit from their novel mechanism of action. Keywords: diabetes, sodium–glucose transporter 2, canagliflozin, dapagliflozin, empagliflozin
format article
author Rosenwasser RF
Sultan S
Sutton D
Choksi R
Epstein BJ
author_facet Rosenwasser RF
Sultan S
Sutton D
Choksi R
Epstein BJ
author_sort Rosenwasser RF
title SGLT-2 inhibitors and their potential in the treatment of diabetes
title_short SGLT-2 inhibitors and their potential in the treatment of diabetes
title_full SGLT-2 inhibitors and their potential in the treatment of diabetes
title_fullStr SGLT-2 inhibitors and their potential in the treatment of diabetes
title_full_unstemmed SGLT-2 inhibitors and their potential in the treatment of diabetes
title_sort sglt-2 inhibitors and their potential in the treatment of diabetes
publisher Dove Medical Press
publishDate 2013
url https://doaj.org/article/d53dfd6d79ef4ad3b1248865a63a3a15
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