Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2020 Jun 24:14:2487-2501.
doi: 10.2147/DDDT.S221093. eCollection 2020.

Remogliflozin Etabonate in the Treatment of Type 2 Diabetes: Design, Development, and Place in Therapy

Viswanathan Mohan  1 , Ambrish Mithal  2 , Shashank R Joshi  3 , S R Aravind  4 , Subhankar Chowdhury  5
Affiliations
Review

Remogliflozin Etabonate in the Treatment of Type 2 Diabetes: Design, Development, and Place in Therapy

Viswanathan Mohan et al. Drug Des Devel Ther. .

Abstract

Type 2 diabetes mellitus (T2DM) is an emerging epidemic in Asian countries, especially in India. With the advent of the SGLT2 inhibitor class of drugs demonstrating benefits beyond glycemic control, viz. weight loss, blood pressure reduction, and cardiovascular and renal protection, the management of T2DM has taken a quantum leap. Remogliflozin etabonate (RE) is the latest addition to the SGLT2 inhibitor class of drugs that have been recently approved in India for the management of T2DM. RE is a potent and selective inhibitor of SGLT2 with the unique distinction of being administered as a prodrug, existence of active metabolites, and short half-life necessitating twice-daily dosing. The Phase III study of RE demonstrated it to be an efficacious and safe agent and non-inferior to the currently available SGLT2 inhibitors. This paper reviews not only the pharmacokinetics, pharmacodynamics, clinical efficacy, and safety profile of RE but also its molecular and clinical development program. This review has taken into consideration all available published as well as unpublished literature on RE and discusses the individual studies performed during its development for characterization of pharmacological profile.

Keywords: SGLT2 inhibitor; T2DM; design; development; etabonate; place in therapy; remogliflozin.

PubMed Disclaimer

Conflict of interest statement

Dr. Viswanathan Mohan and all other authors of this manuscript report personal fees as an Advisory Board Member of Glenmark Pharmaceuticals which markets Remogliflozin in India, outside the submitted work. The authors report no other conflicts of interest in this work.

Figures

Figure 1
Figure 1
Diagrammatic representation of methods. Overall process of followed for selection of evidence considered for review.
Figure 2
Figure 2
Chemical structure of remogliflozin etabonate and remogliflozin. (A) Chemical structure of remogliflozin etabonate. (B) Chemical structure of remogliflozin. (C) Portions of structure of remogliflozin showing glycone, aglycone portions and O-glycosidic bond. The O-glycosidic bond makes the drug susceptible to beta-glucosidase enzyme. (D) Remogliflozin is esterified with etabonic acid to overcome metabolism by beta-glucosidase enzyme.
Figure 3
Figure 3
Clinical studies in development program of remogliflozin etabonate. Abbreviations: PK, pharmacokinetics; PD, pharmacodynamics; GI, gastrointestinal; OC, oral contraceptive pills; DM, diabetes mellitus; Pbo, placebo; Pio, pioglitazone; QD, once daily; IR, immediate release; BID, twice daily; Dapa, dapagliflozin.
Figure 4
Figure 4
Mean change in HbA1c %, Fasting plasma glucose and post-prandial plasma glucose from baseline to week 24. (A) HbA1c at week 24. (B) Fasting blood glucose at week 24. (C) Post-prandial plasma glucose at week 24. Abbreviations: Dapa, dapagliflozin; RE, remogliflozin etabonate.
See this image and copyright information in PMC

References

    1. Zheng Y, Ley SH, Hu FB. Global aetiology and epidemiology of type 2 diabetes mellitus and its complications. Nat Rev Endocrinol. 2017;14(2):88. doi:10.1038/nrendo.2017.151 - DOI - PubMed
    1. International Diabetes Federation. IDF diabetes atlas 9th edition; 2019. Available from: https://www.diabetesatlas.org/en/resources/.Accessed December20, 2019.
    1. Choi CI. Sodium-glucose cotransporter 2 (SGLT2) inhibitors from natural products: discovery of next-generation antihyperglycemic agents. Molecules. 2016;21(9):1136. doi:10.3390/molecules21091136 - DOI - PMC - PubMed
    1. Dey L, Attele AS, Yuan CS. Alternative therapies for type 2 diabetes. Altern Med Rev. 2002;7(1):45–58. - PubMed
    1. Tamez-Perez HE, Gonzalez-Guajardo EE, Tamez-Pena AL. Consensus statement by The American Association of Clinical Endocrinologists and American College of Endocrinology on the comprehensive type 2 diabetes management algorithm - 2019 executive summary. Endocr Pract. 2019;25(6):622. - PubMed

MeSH terms