Dapagliflozin, an SGLT2 inhibitor for the treatment of type 2
diabetes

Demaris, K M; White, John R.

doi:10.1358/dot.2013.49.5.1964714

Cited by 7 publications

(3 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The mode of inhibition of DWP16001 was not different from the other SGLT2 inhibitors. They all showed reversible and competitive inhibition ( Figure 10), which is consistent with other SGLT2 inhibitors [23,24]. However, the affinity to SGLT2 inhibition seemed to be different among the three SGLT2 inhibitors ( Table 3).…”

Section: Discussionsupporting

confidence: 81%

Comparative Pharmacokinetics and Pharmacodynamics of a Novel Sodium-Glucose Cotransporter 2 Inhibitor, DWP16001, with Dapagliflozin and Ipragliflozin

Choi

Nam

et al. 2020

Pharmaceutics

View full text Add to dashboard Cite

Since sodium-glucose cotransporter 2 (SGLT2) inhibitors reduced blood glucose level by inhibiting renal tubular glucose reabsorption mediated by SGLT2, we aimed to investigate the pharmacokinetics and kidney distribution of DWP16001, a novel SGLT2 inhibitor, and to compare these properties with those of dapagliflozin and ipragliflozin, representative SGLT2 inhibitors. The plasma exposure of DWP16001 was comparable with that of ipragliflozin but higher than that of dapagliflozin. DWP16001 showed the highest kidney distribution among three SGLT2 inhibitors when expressed as an area under curve (AUC) ratio of kidney to plasma (85.0 ± 16.1 for DWP16001, 64.6 ± 31.8 for dapagliflozin and 38.4 ± 5.3 for ipragliflozin). The organic anion transporter-mediated kidney uptake of DWP16001 could be partly attributed to the highest kidney uptake. Additionally, DWP16001 had the lowest half-maximal inhibitory concentration (IC 50 ) to SGLT2, a target transporter (0.8 ± 0.3 nM for DWP16001, 1.6 ± 0.3 nM for dapagliflozin, and 8.9 ± 1.7 nM for ipragliflozin). The inhibition mode of DWP16001 on SGLT2 was reversible and competitive, but the recovery of the SGLT2 inhibition after the removal of SGLT2 inhibitors in CHO cells overexpressing SGLT2 was retained with DWP16001, which is not the case with dapagliflozin and ipragliflozin. In conclusion, selective and competitive SGLT2 inhibition of DWP16001 could potentiate the efficacy of DWP16001 in coordination with the higher kidney distribution and retained SGLT2 inhibition of DWP16001 relative to dapagliflozin and ipragliflozin.

show abstract

Section: Discussionsupporting

confidence: 81%

Comparative Pharmacokinetics and Pharmacodynamics of a Novel Sodium-Glucose Cotransporter 2 Inhibitor, DWP16001, with Dapagliflozin and Ipragliflozin

Choi

Nam

et al. 2020

Pharmaceutics

View full text Add to dashboard Cite

show abstract

“…In T2DM, when a patient’s plasma glucose levels exceed natural threshold levels (160–180 mg/dL), SGLT2 receptor saturation results, and this triggers the renal elimination of glucose . Similarly, the action of SGLT2 inhibitors prevents reabsorption of filtered glucose by the kidneys, and this results in a glucose-lowering effect …”

Section: Oral Hypoglycemic Agentsmentioning

confidence: 99%

Type 2 Diabetes Mellitus: Limitations of Conventional Therapies and Intervention with Nucleic Acid-Based Therapeutics

et al. 2015

View full text Add to dashboard Cite

“…SGLT2 inhibitors comprise an emerging, novel class of antihyperglycemic drugs that inhibit glucose reabsorption in the kidney and increase excretion of glucose in the urine [64, 65]. This new, orally administered treatment strategy directly lowers plasma glucose concentration in an insulin-independent manner with a low risk of hypoglycemia.…”

Section: Current and Emerging Treatment Options For Elderly Patients mentioning

confidence: 99%

Management of Type 2 Diabetes Mellitus in Older Patients: Current and Emerging Treatment Options

Moghissi

2013

Diabetes Ther

View full text Add to dashboard Cite

Elderly patients with type 2 diabetes mellitus (T2DM) are a rapidly emerging population that presents unique clinical challenges. This diverse patient group can differ widely in terms of physical and mental status, which can increase their risk of complications including hypoglycemia, falls, and depression. These factors can negatively impact their glycemic control, safety, and quality of life. The risk of hypoglycemic events is elevated among elderly patients with diabetes. In many cases, these events are related to antidiabetic therapy and the pursuit of strict glycemic control. Fear of a hypoglycemic episode, on the part of the patient and/or healthcare provider, is another major barrier to achieving glycemic control. Hypoglycemic events, even in the absence of awareness of the event (asymptomatic), can have negative consequences. To help manage these risks, several national and international organizations have proposed guidelines to address individualized treatment goals for older adults with diabetes. This article reviews current treatment guidelines for setting glycemic targets in elderly patients with T2DM, and discusses the role of emerging treatment options in this patient population.

show abstract

Dapagliflozin, an SGLT2 inhibitor for the treatment of type 2 diabetes

Cited by 7 publications

References 0 publications

Comparative Pharmacokinetics and Pharmacodynamics of a Novel Sodium-Glucose Cotransporter 2 Inhibitor, DWP16001, with Dapagliflozin and Ipragliflozin

Comparative Pharmacokinetics and Pharmacodynamics of a Novel Sodium-Glucose Cotransporter 2 Inhibitor, DWP16001, with Dapagliflozin and Ipragliflozin

Type 2 Diabetes Mellitus: Limitations of Conventional Therapies and Intervention with Nucleic Acid-Based Therapeutics

Management of Type 2 Diabetes Mellitus in Older Patients: Current and Emerging Treatment Options

Contact Info

Product

Resources

About