Investigational Drug Details
| Drug ID: | D101 |
| Drug Name: | Dapagliflozin |
| Synonyms: | (2S,3R,4R,5S,6R)-2-(4-Chloro-3-(4-ethoxybenzyl)phenyl)-6- (hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol; Dapagliflozin |
| Type: | Chemical drug |
| DrugBank ID: | DB06292 |
| DrugBank Description: | Dapagliflozin is a sodium-glucose cotransporter 2 inhibitor indicated for managing diabetes mellitus type 2. When combined with diet and exercise in adults, dapagliflozin helps to improve glycemic control by inhibiting glucose resorption in the proximal tubule of the nephron and causing glycosuria. Dapagliflozin was approved by the FDA on Jan 08, 2014. |
| PubChem ID: | 9887712 |
| CasNo: | 461432-26-8 |
| Repositioning for NAFLD: | Yes |
| SMILES: | O[C@H]1[C@@H](O[C@@H]([C@H]([C@@H]1O)O)CO)c1cc(Cc2ccc(cc2)OCC)c(cc1)Cl |
| Structure: |
|
| InChiKey: | JVHXJTBJCFBINQ-ADAARDCZSA-N |
| Molecular Weight: | 408.878 |
| DrugBank Targets: | Sodium/glucose cotransporter 2 antagonist&inhibitor |
| DrugBank MoA: | Dapagliflozin inhibits the sodium-glucose contransporter 2(SGLT2) which is primarily located in the proximal tubule of the nephron. SGLT2 facilitates 90% of glucose resorption in the kidneys and so its inhibition allows for glucose to be excreted in the urine. This excretion allows for better glycemic control and potentially weight loss in patients with type 2 diabetes mellitus. |
| DrugBank Pharmacology: | Dapagliflozin inhibits the sodium-glucose contransporter 2(SGLT2) which is primarily located in the proximal tubule of the nephron. SGLT2 facilitates 90% of glucose resorption in the kidneys and so its inhibition allows for glucose to be excreted in the urine. This excretion allows for better glycemic control and potentially weight loss in patients with type 2 diabetes mellitus. |
| DrugBank Indication: | Dapagliflozin is indicated to improve glycemic control in adult patients with type 2 diabetes mellitus along with diet and exercise. |
| Targets: | SLC5A2 antagonist; SLC5A2 inhibitor |
| Therapeutic Category: | Antidiabetic drug |
| Clinical Trial Progress: | Phase 2 completed (NCT02426541: In this study, 8 weeks of treatment with dapagliflozin reduced liver PDFF and the volume of visceral adipose tissue in obese patients with type 2 diabetes. Although glycemic control was improved, no effect on tissue-level insulin sensitivity was observed.) |
| Latest Progress: | Under clinical trials |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L0184 | NCT05254626 | Phase 4 | Not yet recruiting | No Results Available | March 2022 | February 24, 2022 | Details |
| L0257 | NCT03723252 | Phase 3 | Recruiting | No Results Available | March 20, 2019 | June 22, 2021 | Details |
| L0366 | NCT02279407 | Phase 2 | Completed | Has Results | January 2015 | March 17, 2017 | Details |
| L0473 | JPRN-jRCT1031180386 | Not applicable | Recruiting | No Results Available | 20/03/2019 | 17 May 2021 | Details |
| L0516 | JPRN-UMIN000030548 | Not applicable | Not Recruiting | No Results Available | 25/12/2017 | 2 April 2019 | Details |
| L0546 | JPRN-UMIN000027304 | Not selected | Not Recruiting | Has Results | 15/05/2017 | 17 May 2021 | Details |
| L0588 | JPRN-UMIN000021291 | Not selected | Not Recruiting | No Results Available | 02/03/2016 | 2 April 2019 | Details |
| L0623 | EUCTR2014-003638-26-SE | Not applicable | Not Recruiting | No Results Available | 03/10/2014 | 11 April 2016 | Details |
| L0803 | JPRN-UMIN000030498 | Not selected | Recruiting | No Results Available | 20/12/2017 | 2 April 2019 | Details |
| L0821 | TCTR20170511001 | Phase 4 | Not Recruiting | Has Results | 11/05/2017 | 7 February 2022 | Details |
| L0884 | JPRN-UMIN000016306 | Not selected | Not Recruiting | No Results Available | 27/01/2015 | 2 April 2019 | Details |
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A00170 | 35202771 | Diabetes Res Clin Pract | Dapagliflozin for nonalcoholic fatty liver disease: A systematic review and meta-analysis. | Details |
| A00217 | 35181350 | Diabetes Res Clin Pract | Metabolic Changes Induced by Dapagliflozin, an SGLT2 Inhibitor, in Japanese Patients with Type 2 Diabetes Treated by Oral Anti-diabetic Agents: A Randomized, Clinical Trial. | Details |
| A00609 | 35030323 | Lancet Gastroenterol Hepatol | Efficacy of peroxisome proliferator-activated receptor agonists, glucagon-like peptide-1 receptor agonists, or sodium-glucose cotransporter-2 inhibitors for treatment of non-alcoholic fatty liver disease: a systematic review. | Details |
| A00701 | 34998036 | Int Immunopharmacol | Dapagliflozin improves steatohepatitis in diabetic rats via inhibition of oxidative stress and inflammation. | Details |
| A01853 | 34588764 | Drug Des Devel Ther | Non-Alcoholic Steatohepatitis (NASH) - A Review of a Crowded Clinical Landscape, Driven by a Complex Disease. | Details |
| A01964 | 34550043 | Adipocyte | Sodium glucose cotransporter 2 inhibitor dapagliflozin depressed adiposity and ameliorated hepatic steatosis in high-fat diet induced obese mice. | Details |
| A02788 | 34239714 | Oman Med J | Effect of SGLT-2 Inhibitors on Non-alcoholic Fatty Liver Disease among Patients with Type 2 Diabetes Mellitus: Systematic Review with Meta-analysis and Trial Sequential Analysis of Randomized Clinical Trials. | Details |
| A02838 | 34224699 | Eur J Pharmacol | Dapagliflozin attenuates steatosis in livers of high-fat diet-induced mice and oleic acid-treated L02 cells via regulating AMPK/mTOR pathway. | Details |
| A03106 | 34129252 | J Gastroenterol Hepatol | The effects of dapagliflozin on hepatic and visceral fat in type 2 diabetes patients with non-alcoholic fatty liver disease. | Details |
| A03117 | 34123670 | Cureus | Effect of Dapagliflozin on Type 2 Diabetes Mellitus With Nonalcoholic Fatty Liver Disease: A Single-Center Survey. | Details |
| A03197 | 34093169 | Front Pharmacol | Dapagliflozin Alleviates Hepatic Steatosis by Restoring Autophagy via the AMPK-mTOR Pathway. | Details |
| A03398 | 34016738 | J Investig Med | Serum high-molecular-weight adiponectin and response to dapagliflozin in patients with type 2 diabetes and non-alcoholic fatty liver disease. | Details |
| A03745 | 33879970 | J Clin Biochem Nutr | Comparison of dapagliflozin and teneligliptin in nonalcoholic fatty liver disease patients without type 2 diabetes mellitus: a prospective randomized study. | Details |
| A04769 | 33511282 | Clin Exp Hepatol | SGLT2 inhibitors for improving hepatic fibrosis and steatosis in non-alcoholic fatty liver disease complicated with type 2 diabetes mellitus: a systematic review. | Details |
| A04892 | 33464703 | Diabetes Obes Metab | Combined exenatide and dapagliflozin has no additive effects on reduction of hepatocellular lipids despite better glycaemic control in patients with type 2 diabetes mellitus treated with metformin: EXENDA, a 24-week, prospective, randomized, placebo-controlled pilot trial. | Details |
| A04904 | 33457424 | J Diabetes Res | Effects of Sodium-Glucose Cotransporter 2 Inhibition on Glucose Metabolism, Liver Function, Ascites, and Hemodynamics in a Mouse Model of Nonalcoholic Steatohepatitis and Type 2 Diabetes. | Details |
| A05042 | 33396949 | Metabolites | Sodium-Glucose Cotransporter-2 Inhibitors for Treatment of Nonalcoholic Fatty Liver Disease: A Meta-Analysis of Randomized Controlled Trials. | Details |
| A05758 | 33131199 | J Diabetes Investig | Favorable effect of sodium-glucose cotransporter 2 inhibitor, dapagliflozin, on non-alcoholic fatty liver disease compared with pioglitazone. | Details |
| A06861 | 32719069 | J Pharmacol Exp Ther | The GPR40 Full Agonist SCO-267 Improves Liver Parameters in a Mouse Model of Nonalcoholic Fatty Liver Disease without Affecting Glucose or Body Weight. | Details |
| A07150 | 32599319 | Int Immunopharmacol | Potential anti-inflammatory effect of dapagliflozin in HCHF diet- induced fatty liver degeneration through inhibition of TNF-α, IL-1β, and IL-18 in rat liver. | Details |