Dapagliflozin, a Novel SGLT2 Inhibitor, Induces Dose-Dependent Glucosuria in Healthy Subjects
Open accessAbstract
Dapagliflozin selectively inhibits renal glucose reabsorption by inhibiting sodium-glucose cotransporter-2 (SGLT2). It was developed as an insulin-independent treatment approach for type 2 diabetes mellitus (T2DM). The safety, tolerability, pharmacokinetics, and pharmacodynamics of the drug were evaluated in single-ascending-dose (SAD; 2.5-500 mg) and multiple-ascending-dose (MAD; 2.5-100 mg daily for 14 days) studies in healthy subjects. Dapagliflozin exhibited dose-proportional plasma concentrations with a half-life of approximately 17 h. The amount of glucosuria was also dose-dependent. Cumulative amounts of glucose excreted on day 1, relating to doses from 2.5-100 mg (MAD), ranged from 18 to 62 g; day 14 values were comparable to day 1 values, with no apparent changes in glycemic parameters. Doses of approximately 20-50 mg provided close-to-maximal SGLT2 inhibition for at least 24 h. Dapagliflozin demonstrates pharmacokinetic (PK) characteristics and dose-dependent glucosuria that are sustained over 24 h, which indicates that it is suitable for administration in once-daily doses and suggests that further investigation of its efficacy in T2DM patients is warranted.
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Similar results were reported by some studies that the blood glucose concentration of the dapagliflozin-treated group peaked in 2 hours.
“Similar results were reported by some studies that the blood glucose concentration of the dapagliflozin treated group peaked in 2 hours,23,24”
From <p>Dapagliflozin Activates Neurons in the Central Nervous System and Regulates Cardiovascular Activity by Inhibiting SGLT-2 in Mice</p> (2020) · cites this paper as [23]
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References 26 · Cited by 350
- Authors
- Komoroski, B., Vachharajani, N., Boulton, D., Kornhauser, D., Geraldes, M., Li, L., & Pfister, M.
- Affiliations
- Bristol-Myers Squibb (United States) (US)
- ORCID
- Venue
- Clinical Pharmacology & Therapeutics
- Publisher
- Wiley
- Published
- 2009-01-07
- Volume
- 85
- Issue
- 5
- Pages
- 520-526
- ISSN
- 0009-9236 (ISSN-L)
- 1532-6535
- OpenAlex
- W2149973065
- Cited by
- 350
- References
- 26
- Citations by year
- 2026: 11 · 2025: 10 · 2024: 12 · 2023: 14 · 2022: 19 · 2021: 18 · 2020: 16 · 2019: 16 · 2018: 15 · 2017: 16 · 2016: 26 · 2015: 17 · 2014: 36 · 2013: 35 · 2012: 24
- FWCI
- 21.81
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Clinical Pharmacology & Therapeutics (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Bristol-Myers Squibb
- Topics
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Treatment and Management
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Management and Research
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Keywords
- dapagliflozin, SGLT2 inhibitors, glycosuria, renal glucose reabsorption, type 2 diabetes, pharmacokinetics, pharmacodynamics, dose proportionality, single ascending dose, multiple ascending dose, healthy volunteers, once-daily dosing
- MeSH terms
- Sodium-Glucose Transporter 2 Inhibitors, Adult, Benzhydryl Compounds, Blood Glucose, Diabetes Mellitus, Type 2, Dose-Response Relationship, Drug, Double-Blind Method, Glucosides, Glycosuria, Half-Life, Humans, Hypoglycemic Agents, Male, Time Factors, Sodium-Glucose Transporter 2
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