Remogliflozin etabonate
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Routes of administration | By mouth |
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Metabolism | Remoglifozin 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] |
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Remogliflozin etabonate (
Clinical trials
Remogliflozin etabonate was shown to enhance urinary glucose excretion in rodents and humans. Early studies in diabetics improved plasma glucose levels.[5][6] Remogliflozin etabonate has been studied at doses up to 1000 mg.[7] 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.[8] In a meta-analysis published by Dutta et al. involving data from 3 randomized controlled trials (535 patients), remogliflozin was noted to have similar glycaemic efficacy (reduction in HbA1c and fasting glucose) as compared to dapagliflozin and pioglitazone. [9] A study concluded that concomitant administration of remogliflozin etabonate, either 500 mg or 750 mg BID (twice a day), with metformin 2000 mg BID was safe and effective in patients with type 2 diabetes mellitus during the observation period.[10]
Method of action
Remogliflozin etabonate is a pro-drug of remogliflozin. Remogliflozin inhibits the
See also
References
- ^ Markham, A.J.D., Remogliflozin etabonate: first global approval. 2019. 79(10): p. 1157-1161.
- ^ Statement on a nonproprietory name adopted by the USAN council
- ^ "Avolynt Announces Completion of Phase 2b BRID Study of SGLT2 Inhibitor Remogliflozin-Etabonate" (Press release). Avolynt, Inc. Retrieved July 24, 2018.
- ^ Mohan, V., et al., Remogliflozin etabonate in the treatment of type 2 diabetes: design, development, and place in therapy. 2020: p. 2487-2501.
- PMID 23011728.
- S2CID 23372554.
- S2CID 6436562.
- S2CID 25280330.
- S2CID 239491862.
- ^ Dobbins, R., et al., Assessment of safety and tolerability of remogliflozin etabonate (GSK189075) when administered with total daily dose of 2000 mg of metformin. 2021. 22: p. 1-11.
- ^ "Molecule of the Month: Dapagliflozin". Prous Science. November 2007. Archived from the original on January 6, 2008.