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Bexagliflozin: First Approval

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Abstract

Bexagliflozin (BRENZAVVY™) is an orally administered potent inhibitor of sodium–glucose transporter 2 (SGLT-2). It is being developed by TheracosBio for the treatment of type 2 diabetes (T2D) and essential hypertension, and in January 2023 it received its first approval in the USA for use as an adjunct to diet and exercise to improve glycaemic control in adults with T2D. Bexagliflozin is contraindicated in patients receiving dialysis and is not recommended in patients with type 1 diabetes or in those with an estimated glomerular filtration rate of < 30 mL/min/1.73 m2. Bexagliflozin is undergoing clinical development for the treatment of essential hypertension in the USA. This article summarizes the milestones in the development of bexagliflozin leading to this first approval for the treatment of T2D.

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References

  1. Diamant M, Morsink LM. SGLT2 inhibitors for diabetes: turning symptoms into therapy. Lancet. 2013;382(9896):917–8.

    Article  PubMed  Google Scholar 

  2. Hsia DS, Grove O, Cefalu WT. An update on sodium-glucose co-transporter-2 inhibitors for the treatment of diabetes mellitus. Curr Opin Endocrinol Diabetes Obes. 2017;24(1):73–9.

    CAS  PubMed  PubMed Central  Google Scholar 

  3. Peng Y, Qin D, Wang Y, et al. The effect of SGLT-2 inhibitors on cardiorespiratory fitness capacity: a systematic review and meta-analysis. Front Physiol. 2022;13:1081920.

    Article  PubMed  Google Scholar 

  4. TheracosBio LLC. BRENZAVVY (bexagliflozin) tablets, for oral use: US prescribing information; 2023. https://www.fda.gov/. Accessed 26 Jan 2023.

  5. TheracosBio. TheracosBio announces FDA approval of Brenzavvy™ (bexagliflozin) for the treatment of adults with type 2 diabetes [media release]. 23 Jan 2023. https://theracosbio.com/.

  6. US National Institutes of Health. ClinicalTrials.gov identifier NCT03514641; 2021. https://clinicaltrials.gov/. Accessed 7 Feb 2023.

  7. Zhang W, Welihinda A, Mechanic J, et al. EGT1442, a potent and selective SGLT2 inhibitor, attenuates blood glucose and HbA(1c) levels in db/db mice and prolongs the survival of stroke-prone rats. Pharmacol Res. 2011;63(4):284–93.

    Article  CAS  PubMed  Google Scholar 

  8. Zhang W, Li X, Ding H, et al. Metabolism and disposition of the SGLT2 inhibitor bexagliflozin in rats, monkeys and humans. Xenobiotica. 2020;50(5):559–69.

    Article  CAS  PubMed  Google Scholar 

  9. Halvorsen YC, Walford GA, Massaro J. A 96-week, multinational, randomized, double-blind, parallel-group, clinical trial evaluating the safety and effectiveness of bexagliflozin as a monotherapy for adults with type 2 diabetes. Diabetes Obes Metab. 2019;21(11):2496–504.

    Article  CAS  PubMed  Google Scholar 

  10. Halvorsen YD, Walford G, Thurber T, et al. A 12-week, randomized, double-blind, placebo-controlled, four-arm dose-finding phase 2 study evaluating bexagliflozin as monotherapy for adults with type 2 diabetes. Diabetes Obes Metab. 2020;22(4):566–73.

    Article  CAS  PubMed  Google Scholar 

  11. Halvorsen YD, Lock JP, Freeman MW. Cardiovascular and glycemic benefits of bexagliflozin as an adjunct to metformin for the treatment of type 2 diabetes in adults: a 24-week, randomized, double-blind, placebo-controlled trial. Diabetes. 2020;69(Suppl 1):1117-P.

    Article  Google Scholar 

  12. Halvorsen YD, Lock JP, Frias JP, et al. A 96-week, double-blind, randomized controlled trial comparing bexagliflozin to glimepiride as an adjunct to metformin for the treatment of type 2 diabetes in adults. Diabetes Obes Metab. 2023;25(1):293–301.

    Article  CAS  PubMed  Google Scholar 

  13. Halvorsen YD, Lock JP, Zhou W. A 24-week, randomized, double-blind, active-controlled clinical trial comparing bexagliflozin with sitagliptin as an adjunct to metformin for the treatment of type 2 diabetes in adults. Diabetes Obes Metab. 2019;21(10):2248–56.

    Article  CAS  PubMed  Google Scholar 

  14. Allegretti AS, Zhang W, Zhou W, et al. Safety and effectiveness of bexagliflozin in patients with type 2 diabetes mellitus and stage 3a/3b CKD. Am J Kidney Dis. 2019;74(3):328–37.

    Article  CAS  PubMed  Google Scholar 

  15. McMurray JJV, Freeman MW, Massaro J, et al. The Bexagliflozin Efficacy and Safety Trial (BEST): a randomized, double-blind, placebo-controlled, phase IIII, clinical trial [abstract]. Diabetes. 2020;69(Suppl 1):32-OR.

    Article  Google Scholar 

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Correspondence to Sheridan M. Hoy.

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The preparation of this review was not supported by any external funding.

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During the peer review process the manufacturer of the agent under review was offered an opportunity to comment on the article. Changes resulting from any comments received were made by the authors on the basis of scientific completeness and accuracy. Sheridan M. Hoy is a salaried employee of Adis International Ltd/Springer Nature, and declares no relevant conflicts of interest. All authors contributed to the review and are responsible for the article content.

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This profile has been extracted and modified from the AdisInsight database. AdisInsight tracks drug development worldwide through the entire development process, from discovery, through pre-clinical and clinical studies to market launch and beyond.

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Hoy, S.M. Bexagliflozin: First Approval. Drugs 83, 447–453 (2023). https://doi.org/10.1007/s40265-023-01848-x

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