Remogliflozin etabonate

Remogliflozin etabonate (INN/USAN)[1] is a drug of the gliflozin class for the treatment of non-alcoholic steatohepatitis ("NASH") and type 2 diabetes. Remogliflozin was discovered by the Japanese company Kissei Pharmaceutical and is currently being developed by BHV Pharma, a wholly owned subsidiary of North Carolina USA-based Avolynt, and Glenmark Pharmaceuticals through a collaboration with BHV.[2] Remogliflozin was commercially launched first in India by Glenmark in May 2019.

Remogliflozin etabonate
Clinical data
Routes of
administration
By mouth
ATC code
  • none
Legal status
Legal status
  • Investigational
Identifiers
CAS Number
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC26H38N2O9
Molar mass522.586 g/mol g·mol−1
3D model (JSmol)
 NY (what is this?)  (verify)

Clinical trials

Remogliflozin etabonate was shown to enhance urinary glucose excretion in rodents and humans. Early studies in diabetics improved plasma glucose levels.[3][4] Remogliflozin etabonate has been studied at doses up to 1000 mg.[5] 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.[6]

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.[7] Remogliflozin is selective for SGLT2.

See also

References

  1. Statement on a nonproprietory name adopted by the USAN council
  2. "Avolynt Announces Completion of Phase 2b BRID Study of SGLT2 Inhibitor Remogliflozin-Etabonate" (Press release). Avolynt, Inc. Retrieved July 24, 2018.
  3. Mudaliar, S; Armstrong, DA; Mavian, AA; O'Connor-Semmes, R; Mydlow, PK; Ye, J; Hussey, EK; Nunez, DJ; Henry, RR; Dobbins, RL (Nov 2012). "Remogliflozin etabonate, a selective inhibitor of the sodium-glucose transporter 2, improves serum glucose profiles in type 1 diabetes". Diabetes Care. 35 (11): 2198–200. doi:10.2337/dc12-0508. PMC 3476920. PMID 23011728.
  4. Dobbins, RL; O'Connor-Semmes, R; Kapur, A; Kapitza, C; Golor, G; Mikoshiba, I; Tao, W; Hussey, EK (Jan 2012). "Remogliflozin etabonate, a selective inhibitor of the sodium-dependent transporter 2 reduces serum glucose in type 2 diabetes mellitus patients". Diabetes Obes Metab. 14 (1): 15–22. doi:10.1111/j.1463-1326.2011.01462.x. PMID 21733056.
  5. Sykes, AP; O'Connor-Semmes, R; Dobbins, R; Dorey, DJ; Lorimer, JD; Walker, S; Wilkison, WO; Kler, L (Jan 2015). "Randomized trial showing efficacy and safety of twice-daily remogliflozin etabonate for the treatment of type 2 diabetes". Diabetes Obes. Metab. 17 (1): 94–7. doi:10.1111/dom.12391. PMID 25223369.
  6. Sykes, AP; Kemp, GL; Dobbins, R; O'Connor-Semmes, R; Almond, SR; Wilkison, WO; Walker, S; Kler, L (Jan 2015). "Randomized efficacy and safety trial of once-daily remogliflozin etabonate for the treatment of type 2 diabetes". Diabetes Obes Metab. 17 (1): 98–101. doi:10.1111/dom.12393. PMID 25238025.
  7. Prous Science: Molecule of the Month November 2007 Archived January 6, 2008, at the Wayback Machine
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