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Sodium-Glucose Cotransporter Inhibitors as Antidiabetic Drugs: Current Development and Future Perspectives
Rosanna Maccari1, Rosaria Ottanà1
1Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale F. Stagno D'Alcontres, 31, 98166 Messina, Italy.
Journal of Medicinal Chemistry
|August 4, 2022
Summary
Sodium-glucose cotransporter 2 (SGLT-2) inhibitors offer a new way to manage hyperglycemia and protect the heart and kidneys. Research now explores dual SGLT-1/SGLT-2 inhibitors for improved antidiabetic drug development.
Area of Science:
- Pharmacology
- Endocrinology
- Drug Discovery
Background:
- Sodium-glucose cotransporter 2 (SGLT-2) inhibitors are a recent class of oral antidiabetic drugs.
- SGLT-2 overexpression in diabetes exacerbates hyperglycemia and complications.
- SGLT-2 is a key therapeutic target for managing diabetes.
Purpose of the Study:
- To review the mechanism of action and therapeutic applications of SGLT-2 inhibitors.
- To explore the potential of targeting intestinal SGLT-1 for glycemic control.
- To highlight the development of dual SGLT-1/SGLT-2 inhibitors as novel antidiabetic drug candidates.
Main Methods:
- Review of existing literature on SGLT-2 inhibitors and their structure-activity relationships.
- Analysis of the role of intestinal SGLT-1 in glucose homeostasis.
- Discussion of design strategies for selective SGLT-1 and dual SGLT-1/SGLT-2 inhibitors.
Main Results:
- SGLT-2 inhibitors improve glycemic control via an insulin-independent mechanism.
- These drugs demonstrate significant cardiorenal protective effects in various populations.
- Intestinal SGLT-1 inhibition presents a novel multifactorial approach to hyperglycemia management.
Conclusions:
- SGLT-2 inhibitors are effective oral antidiabetic agents with cardiorenal benefits.
- Targeting intestinal SGLT-1, alone or in combination with SGLT-2, offers promising therapeutic strategies.
- Development of dual SGLT-1/SGLT-2 inhibitors represents a compelling avenue for new antidiabetic drug discovery.
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