Remogliflozin etabonate

Remogliflozin etabonate
Systematic (IUPAC) name
5-methyl-4-[4-(1-methylethoxy)benzyl]-1-(1-methylethyl)-1H-pyrazol-3-yl 6-O-(ethoxycarbonyl)-β-D-glucopyranoside
Clinical data
Routes of
administration		 Oral
Identifiers
CAS Number 442201-24-3 YesY
ATC code None
ChemSpider 8047110
UNII TR0QT6QSUL N
KEGG D10055 N
ChEMBL CHEMBL494323 N
Chemical data
Formula C26H38N2O9
Molar mass 522.586 g/mol
 NYesY (what is this?)  (verify)

Remogliflozin etabonate (INN/USAN)[1] is a proposed drug of the gliflozin class for the treatment of type 2 diabetes, investigated by GlaxoSmithKline.[2] Remogliflozin is now being developed by BHV Pharma with Islet Sciences.[3]

Clinical trials

Remogliflozin etabonate (RE) was shown to enhance urinary glucose excretion in rodents and humans. Early studies in diabetics improved plasma glucose levels.[4][5] Remogliflozin etabonate has been studied at doses up to 1000 mg.[6] A pair of 12-week phase 2b randomized clinical trials of diabetics published in 2015, found reductions in glycated hemoglobin and that it was generally well tolerated.[7]

Method of action

Remogliflozin etabonate is a pro-drug of remogliflozin. Remogliflozin inhibits the sodium-glucose transport proteins (SGLT), which are responsible for glucose reabsorption in the kidney. Blocking this transporter causes blood glucose to be eliminated through the urine.[8] Remogliflozin is selective for SGLT2.

See also

References

  1. ↑ Statement on a nonproprietory name adopted by the USAN council
  2. ↑ Fujimori Y, Katsuno K, Nakashima I, Ishikawa-Takemura Y, Fujikura H, Isaji M (June 2008). "Remogliflozin etabonate, in a Novel Category of Selective Low-Affinity / High-Capacity Sodium Glucose Cotransporter (SGLT2) Inhibitors, Exhibits Antidiabetic Efficacy in Rodent Models". J. Pharmacol. Exp. Ther. 327 (1): 268–276. doi:10.1124/jpet.108.140210. PMID 18583547.
  3. ↑ "Islet Sciences to Acquire BHV Pharma and Phase 2 SGLT2 Inhibitor Remogliflozin Etabonate Indicated for Type 2 Diabetes and NASH". Yahoo Finance. March 13, 2014.
  4. ↑ "Remogliflozin etabonate, a selective inhibitor of the sodium-glucose transporter 2, improves serum glucose profiles in type 1 diabetes." 35. Nov 2012: 2198–200. doi:10.2337/dc12-0508. PMID 23011728.
  5. ↑ "Remogliflozin etabonate, a selective inhibitor of the sodium-dependent transporter 2 reduces serum glucose in type 2 diabetes mellitus patients." 14. Jan 2012: 15–22. doi:10.1111/j.1463-1326.2011.01462.x. PMID 21733056.
  6. ↑ "Randomized trial showing efficacy and safety of twice-daily remogliflozin etabonate for the treatment of type 2 diabetes.". Diabetes Obes Metab. 17: 94–7. Jan 2015. doi:10.1111/dom.12391. PMID 25223369.
  7. ↑ "Randomized efficacy and safety trial of once-daily remogliflozin etabonate for the treatment of type 2 diabetes." 17. Jan 2015: 98–101. doi:10.1111/dom.12393. PMID 25238025.
  8. ↑ Prous Science: Molecule of the Month November 2007 Archived January 6, 2008 at the Wayback Machine


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