Remogliflozin etabonate, a selective inhibitor of the sodium‐dependent transporter 2 reduces serum glucose in type 2 diabetes mellitus patients

Dobbins, Robert L.; O’Connor-Semmes, Robin L.; Kapur, Anita; Kapitza, Christoph; Golor, Georg; Mikoshiba, Imao; Wan, Tao; Hussey, Elizabeth K.

doi:10.1111/j.1463-1326.2011.01462.x

Cited by 67 publications

(57 citation statements)

References 30 publications

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“…The modest changes in remogliflozin exposure are not clinically significant, because remogliflozin etabonate has a large therapeutic window, as demonstrated in clinical studies up to 1000 mg b.i.d. Dobbins et al, 2012). Therefore, these data suggest that remogliflozin etabonate can be administered with P450 inhibitors without dose adjustments.…”

Section: Discussionmentioning

confidence: 99%

“…1) (Fujimori et al, 2008). Remogliflozin etabonate causes a concentration-dependent increase in urinary glucose excretion in humans and nonclinical species Dobbins et al, 2012). Oral administration of remogliflozin etabonate reduces postprandial glucose excursions without inducing hypoglycemia, improves plasma glucose concentrations in subjects with diabetes, and reduces glycosylated hemoglobin (HbA1c) levels.…”

Section: Abbreviationsmentioning

confidence: 99%

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Assessment of the Drug Interaction Risk for Remogliflozin Etabonate, a Sodium-Dependent Glucose Cotransporter-2 Inhibitor: Evidence from In Vitro, Human Mass Balance, and Ketoconazole Interaction Studies

et al. 2012

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ABSTRACT:Remogliflozin etabonate is the ester prodrug of remogliflozin, a selective sodium-dependent glucose cotransporter-2 inhibitor. This work investigated the absorption, metabolism, and excretion of [ A ketoconazole clinical drug interaction study, along with the human mass balance findings, confirmed that CYP3A4 contributes less than 50% to remogliflozin metabolism, demonstrating that other enzyme pathways (e.g., P450s, UDP-glucuronosyltransferases, and glucosidases) make significant contributions to the drug's clearance. Overall, these studies support a low clinical drug interaction risk for remogliflozin etabonate due to the availability of multiple biotransformation pathways.

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Section: Discussionmentioning

confidence: 99%

Section: Abbreviationsmentioning

confidence: 99%

Assessment of the Drug Interaction Risk for Remogliflozin Etabonate, a Sodium-Dependent Glucose Cotransporter-2 Inhibitor: Evidence from In Vitro, Human Mass Balance, and Ketoconazole Interaction Studies

et al. 2012

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“…(296-and 395-fold, respectively) but remained susceptible to glucosidase cleavage in the gut 27 and had relatively short half-lives 28 . The discovery of Carylglucoside SGLT2 inhibitors, which are resistant to gastrointestinal tract bglucosidases, followed.…”

Section: Therapeutic Implications Of Sglts Inhibitionmentioning

confidence: 99%

Glucuretics: A New Class of Drug for the Treatment of Type 2 Diabetes

Hoque¹,

Rahman²,

Islam³

et al. 2017

KYAMC j.

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Type 2 diabetes is a common, chronic disease with a prevalence that is increasing at epidemic proportions. Management involves advice on lifestyle changes, oral anti-hyperglycaemic agents and/or insulin. The kidney plays an important role in glucose homeostasis via its production, utilization, and, most importantly, reabsorption of glucose from glomerular filtrate which is largely mediated via the sodium glucose cotransporter 2 (SGLT2). Competitive inhibition of SGLT2 induces glucosuria in a dose dependent manner and appears to have beneficial effects on glucose regulation in individuals with type 2 diabetes. Agents that inhibit SGLT2 represent a novel class of drugs, which has recently become available for treatment of type 2 diabetes. This article summarizes the rationale for use of these agents and reviews available clinical data on their efficacy, safety, and risks/benefits.KYAMC Journal Vol. 6, No.-1, Jul 2015, Page 592-597

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“…Remigliflozin is an O-glycoside which is susceptible to β-glucosidase [39]. Moreover, it causes reduction of blood glucose and body weight as well as the blood pressure in type2 diabetes mellitus patients [21].…”

Section: Remigliflozinmentioning

confidence: 99%

“…Sergliflozin was discontinued for various unfavorable effects such as non-desired pharmaceutical properties, non-selectivity and development of new SGLT2 inhibitors [21][22][23].…”

Section: Sergiflozin Etabonatementioning

confidence: 99%

An Emerging Protagonist: Sodium Glucose Co-transporters (SGLTs) as a Burgeoning Target for the Treatment of Diabetes Mellitus

et al. 2014

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Remogliflozin etabonate, a selective inhibitor of the sodium‐dependent transporter 2 reduces serum glucose in type 2 diabetes mellitus patients

Abstract: Administration of RE for 12 days is well-tolerated and results in clinically meaningful improvements in plasma glucose, accompanied by changes in body weight and blood pressure in subjects with T2DM.

Cited by 67 publications

References 30 publications

Assessment of the Drug Interaction Risk for Remogliflozin Etabonate, a Sodium-Dependent Glucose Cotransporter-2 Inhibitor: Evidence from In Vitro, Human Mass Balance, and Ketoconazole Interaction Studies

Assessment of the Drug Interaction Risk for Remogliflozin Etabonate, a Sodium-Dependent Glucose Cotransporter-2 Inhibitor: Evidence from In Vitro, Human Mass Balance, and Ketoconazole Interaction Studies

Glucuretics: A New Class of Drug for the Treatment of Type 2 Diabetes

An Emerging Protagonist: Sodium Glucose Co-transporters (SGLTs) as a Burgeoning Target for the Treatment of Diabetes Mellitus

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