Cargando…

SGLT2-inhibitors; more than just glycosuria and diuresis

Heart failure (HF) continues to be a serious public health challenge despite significant advancements in therapeutics and is often complicated by multiple other comorbidities. Of particular concern is type 2 diabetes mellitus (T2DM) which not only amplifies the risk, but also limits the treatment op...

Descripción completa

Detalles Bibliográficos
Autores principales: Fathi, Amir, Vickneson, Keeran, Singh, Jagdeep S.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Springer US 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8024235/
https://www.ncbi.nlm.nih.gov/pubmed/33274396
http://dx.doi.org/10.1007/s10741-020-10038-w
_version_ 1783675270977290240
author Fathi, Amir
Vickneson, Keeran
Singh, Jagdeep S.
author_facet Fathi, Amir
Vickneson, Keeran
Singh, Jagdeep S.
author_sort Fathi, Amir
collection PubMed
description Heart failure (HF) continues to be a serious public health challenge despite significant advancements in therapeutics and is often complicated by multiple other comorbidities. Of particular concern is type 2 diabetes mellitus (T2DM) which not only amplifies the risk, but also limits the treatment options available to patients. The sodium-glucose linked cotransporter subtype 2 (SGLT2)-inhibitor class, which was initially developed as a treatment for T2DM, has shown great promise in reducing cardiovascular risk, particularly around HF outcomes – regardless of diabetes status. There are ongoing efforts to elucidate the true mechanism of action of this novel drug class. Its primary mechanism of inducing glycosuria and diuresis from receptor blockade in the renal nephron seems unlikely to be responsible for the rapid and striking benefits seen in clinical trials. Early mechanistic work around conventional therapeutic targets seem to be inconclusive. There are some emerging theories around its effect on myocardial energetics and calcium balance as well as on renal physiology. In this review, we discuss some of the cutting-edge hypotheses and concepts currently being explored around this drug class in an attempt better understand the molecular mechanics of this novel agent.
format Online
Article
Text
id pubmed-8024235
institution National Center for Biotechnology Information
language English
publishDate 2020
publisher Springer US
record_format MEDLINE/PubMed
spelling pubmed-80242352021-04-21 SGLT2-inhibitors; more than just glycosuria and diuresis Fathi, Amir Vickneson, Keeran Singh, Jagdeep S. Heart Fail Rev Article Heart failure (HF) continues to be a serious public health challenge despite significant advancements in therapeutics and is often complicated by multiple other comorbidities. Of particular concern is type 2 diabetes mellitus (T2DM) which not only amplifies the risk, but also limits the treatment options available to patients. The sodium-glucose linked cotransporter subtype 2 (SGLT2)-inhibitor class, which was initially developed as a treatment for T2DM, has shown great promise in reducing cardiovascular risk, particularly around HF outcomes – regardless of diabetes status. There are ongoing efforts to elucidate the true mechanism of action of this novel drug class. Its primary mechanism of inducing glycosuria and diuresis from receptor blockade in the renal nephron seems unlikely to be responsible for the rapid and striking benefits seen in clinical trials. Early mechanistic work around conventional therapeutic targets seem to be inconclusive. There are some emerging theories around its effect on myocardial energetics and calcium balance as well as on renal physiology. In this review, we discuss some of the cutting-edge hypotheses and concepts currently being explored around this drug class in an attempt better understand the molecular mechanics of this novel agent. Springer US 2020-12-04 2021 /pmc/articles/PMC8024235/ /pubmed/33274396 http://dx.doi.org/10.1007/s10741-020-10038-w Text en © The Author(s) 2020 Open AccessThis article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/.
spellingShingle Article
Fathi, Amir
Vickneson, Keeran
Singh, Jagdeep S.
SGLT2-inhibitors; more than just glycosuria and diuresis
title SGLT2-inhibitors; more than just glycosuria and diuresis
title_full SGLT2-inhibitors; more than just glycosuria and diuresis
title_fullStr SGLT2-inhibitors; more than just glycosuria and diuresis
title_full_unstemmed SGLT2-inhibitors; more than just glycosuria and diuresis
title_short SGLT2-inhibitors; more than just glycosuria and diuresis
title_sort sglt2-inhibitors; more than just glycosuria and diuresis
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8024235/
https://www.ncbi.nlm.nih.gov/pubmed/33274396
http://dx.doi.org/10.1007/s10741-020-10038-w
work_keys_str_mv AT fathiamir sglt2inhibitorsmorethanjustglycosuriaanddiuresis
AT vicknesonkeeran sglt2inhibitorsmorethanjustglycosuriaanddiuresis
AT singhjagdeeps sglt2inhibitorsmorethanjustglycosuriaanddiuresis