Remogliflozin etabonate

Remogliflozin etabonate
Clinical data
Routes of
administration		By mouth
ATC code
  • none
Legal status
Legal status
  • Investigational
Pharmacokinetic data
MetabolismRemoglifozin is metabolized primarily by cytochrome P450 (CYP) 3A4 and to a lesser extent by CYP2C19 to GSK 279782 (the active metabolite) and GSK 333081 before being glucuronidated to generate inactive glucuronide conjugates.[1]
Identifiers
  • 5-Methyl-4-[4-(1-methylethoxy)benzyl]-1-(1-methylethyl)-1H-pyrazol-3-yl 6-O-(ethoxycarbonyl)-β-D-glucopyranoside
CAS Number
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC26H38N2O9
Molar mass522.595 g·mol−1
3D model (JSmol)
  • OC1C(COC(=O)OCC)OC(C(O)C1O)Oc(nn(C(C)C)c2C)c2Cc3ccc(cc3)OC(C)C
  • InChI=1S/C26H38N2O9/c1-7-33-26(32)34-13-20-21(29)22(30)23(31)25(36-20)37-24-19(16(6)28(27-24)14(2)3)12-17-8-10-18(11-9-17)35-15(4)5/h8-11,14-15,20-23,25,29-31H,7,12-13H2,1-6H3/t20-,21-,22+,23-,25+/m1/s1 ☒N
  • Key:UAOCLDQAQNNEAX-ABMICEGHSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Remogliflozin etabonate (INN/USAN)[2] 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, US-based Avolynt, and Glenmark Pharmaceuticals through a collaboration with BHV.[3] In 2002, GlaxoSmithKline (GSK) received a license to use it. From 2002 to 2009, GSK carried out a significant clinical development program for the treatment of type-2 diabetes mellitus in various nations across the world and obesity in the UK. Remogliflozin etabonate's pharmacokinetics, pharmacodynamics, and clinical dose regimens were characterized in 18 Phase I and 2 Phase II investigations. Due to financial concerns, GSK stopped working on remogliflozin and sergliflozin, two further SGLT2 inhibitors that were licensed to the company, in 2009.[4] Remogliflozin was commercially launched first in India by Glenmark in May 2019.

  1. ^ Markham, A.J.D., Remogliflozin etabonate: first global approval. 2019. 79(10): p. 1157-1161.
  2. ^ Statement on a nonproprietory name adopted by the USAN council
  3. ^ "Avolynt Announces Completion of Phase 2b BRID Study of SGLT2 Inhibitor Remogliflozin-Etabonate" (Press release). Avolynt, Inc. Retrieved July 24, 2018.
  4. ^ Mohan, V., et al., Remogliflozin etabonate in the treatment of type 2 diabetes: design, development, and place in therapy. 2020: p. 2487-2501.