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Luseogliflozin: First Global Approval

Drugs volume 74, pages 945–950 (2014)Cite this article

Abstract

Luseogliflozin [Lusefi® (Japan)] is an orally active second-generation sodium-glucose co-transporter 2 (SGLT2) inhibitor developed by Taisho Pharmaceutical for the treatment of patients with type 2 diabetes mellitus (T2DM). The drug has received its first global approval for this indication in Japan, either as monotherapy or in combination with other antihyperglycaemic agents. This article summarises the milestones in the development of luseogliflozin leading to this first approval for the treatment of T2DM.

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References

  1. Abdul-Ghani MA, Norton L, DeFronzo RA. Efficacy and safety of SGLT2 inhibitors in the treatment of type 2 diabetes mellitus. Curr Diabetes Rep. 2012;12(3):230–8.

    CAS  Article  Google Scholar 

  2. Vasilakou D, Karagiannis T, Athanasiadou E, et al. Sodium-glucose cotransporter 2 inhibitors for type 2 diabetes: A systematic review and meta-analysis. Ann Intern Med. 2013;159(4):262–74.

    PubMed  Article  Google Scholar 

  3. Taisho P. Acquisition of Manufacturing and Marketing Approval in Japan for SGLT2 Inhibitor Lusefi(Rm) Tablets 2.5 mg and Lusefi(Rm) Tablets 5 mg [media release. http://www.taisho-holdings.co.jp]. 24 Mar 2014.

  4. Novartis. Lusefi (luseogliflozin): Japanese prescribing information [In Japanese]. 2014. http://medical.taishotoyama.co.jp/cgi-bin/index2_n.cgi?mode=sel&rows=86&caut=tenp&page=/data/tenp/pdf/tenp_lsf.pdf. Accessed 11 May 2014.

  5. Taisho Pharmaceutical Holdings Co L. Signing of Domestic Sales Rights Licensing Agreement Regarding SGLT2 Inhibitor TS-071 [media release]. http://www.taisho-holdings.co.jp. 30 Nov 2012.

  6. Kakinuma H, Oi T, Hashimoto-Tsuchiya Y, et al. (1S)-1,5-anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-D-glucitol (TS-071) is a potent, selective sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for type 2 diabetes treatment. J Med Chem. 2010;53(8):3247–61.

    CAS  PubMed  Article  Google Scholar 

  7. Teisuke T, Kozakai A, Kojima N, et al. Long-term treatment of TS-071, a novel, potent and selective SGLT2 inhibitor, improves hyperglycaemia and prevents the loss of beta cell in diabetic mice. Diabetologia. 2011;54:S345.

    Google Scholar 

  8. Yamamoto K, Uchida S, Kitano K, et al. TS-071 is a novel, potent and selective renal sodium-glucose cotransporter 2 (SGLT2) inhibitor with anti-hyperglycaemic activity. Br J Pharmacol. 2011;164(1):181–91.

    CAS  PubMed Central  PubMed  Article  Google Scholar 

  9. Uchida S, Takahashi T, Tomoike H, et al. TS-071, a novel, potent and selective SGLT2 inhibitor, induces weight loss and a reduction in adipocyte size in diet-induced obese rats. Diabetes. 2011;60:A274.

    Article  Google Scholar 

  10. Sasaki T, Seino Y, Fukatsu A, et al. Safety, pharmacokinetics, and pharmacodynamics of single and multiple luseogliflozin dosing in healthy Japanese males: a randomized, single-blind, placebo-controlled trial. Adv Ther. 2014;31(3):345–61.

    CAS  PubMed Central  PubMed  Article  Google Scholar 

  11. Sasaki T, Seino Y, Fukatsu A, et al. TS-071, a novel potent and highly selective renal sodium-glucose co- transporter 2 (SGLT2) inhibitor, increases urinary glucose excretion and reduces plasma glucose levels in Japanese patients with type 2 diabetes mellitus. 47th Annual Meeting of the European Association for the Study of Diabetes. 2011:abstr. 846.

  12. Morrow LA, Guttierrez MJ, Tanaka Y, et al. Luseogliflozin (TS-071), a novel, potent, and selective inhibitor of SGLT2 is safe and well-tolerated in type 2 diabetes mellitus and showed dosedependent PK/PD in both US/Japanese ethnicities. Diabetologia. 2012;55:S304.

    Google Scholar 

  13. Haneda M, Seino Y, Sasaki T, et al. The effect of luseogliflozin (TS-071), a selective SGLT2 inhibitor, on pharmacodynamics and pharmacokinetics in Japanese type 2 diabetic subjects with renal impairment. Diabetes. 2012;61:A273.

    Google Scholar 

  14. Sasaki T, Seino Y, Samukawa Y, et al. Effects of gender and age on the pharmacokinetics and pharmacodynamics of luseogliflozin (TS-071), a selective SGLT2 inhibitor. Diabetes. 2012;61:A275.

    Google Scholar 

  15. Nakai Y, Mutoh M. Luseogliflozin (TS-071) a novel, potent and selective sglt2 inhibitor, did not affect the PK of several oral diabetic agents in clinical. Diabetes. 2012;61:A607.

    Google Scholar 

  16. Inagaki N, Seino Y, Sasaki T, et al. Luseogliflozin, a selective SGLT2 inhibitor, added on to glimepiride for 52 weeks improves glycaemic control with no major hypoglycaemia in Japanese type 2 diabetes patients. 49th Annual Meeting of the European Association for the Study of Diabetes. 2013:abstr. 184.

  17. Haneda M, Seino Y, Sasaki T, et al. Luseogliflozin, a SGLT2 inhibitor, as add-on therapy to 5 types of oral antidiabetic drugs improves glycaemic control and reduces body weight in Japanese patients with type 2 diabetes mellitus. 49th Annual Meeting of the European Association for the Study of Diabetes. 2013:abstr. 957.

  18. Seino Y, Sasaki T, Fukatsu A, et al. Luseogliflozin, a selective SGLT2 inhibitor, improves glycemic control as monotherapy in Japanese patients with T2DM. World Diabetes Congress 2013. 2013:abstr. P-1472.

  19. Seino Y, Sasaki T, Fukatsu A, et al. Efficacy and safety of luseogliflozin as monotherapy in Japanese patients with type 2 diabetes mellitus: a randomized, double-blind, placebo-controlled, phase 3 study. Curr Med Res Opin. 2014. doi:10.1185/03007995.2014.912983.

    Google Scholar 

  20. Seino Y, Sasaki T, Fukatsu A, et al. Dose-finding study of luseogliflozin in Japanese patients with type 2 diabetes mellitus: a 12-week, randomized, double-blind, placebo-controlled, phase II study. Curr Med Res Opin. 2014. doi:10.1185/03007995.2014.909390:1-14.

    Google Scholar 

  21. Seino Y, Sasaki T, Fukatsu A, et al. TS-071, a Novel and Selective SGLT2 Inhibitor, Improved Glycemic Control and Decreased Body Weight in 12-Week Study of Japanese Patients with Type 2 Diabetes Mellitus. 71st Annual Scientific Sessions of the American Diabetes Association. 2011:abstr. 0998-P.

  22. Seino Y, Sasaki T, Fukatsu A, et al. TS-071, a novel and selective SGLT2 inhibitor, improved glycemic control and decreased body weight in 12-week study of Japanese patients with type 2 diabetes mellitus. Diabetes. 2011;60:A274.

    Google Scholar 

  23. Seino Y, Sasaki T, Fukatsu A, et al. Luseogliflozin (TS-071), a selective SGLT2 inhibitor, improves glycaemic control and lowers body weight in a 12-week study in Japanese patients with type 2 diabetes mellitus. 48th Annual Meeting of the European Association for the Study of Diabetes. 2012:abstr. 740.

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Disclosure

The preparation of this report was not supported by any external funding. 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. A. Markham is a contracted employee of Adis, Springer SBM. S. Elkinson is a salaried employee of Adis, Springer SBM.

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Affiliations

  1. Adis R&D Insight, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, North Shore, 0754, Auckland, New Zealand

    Shelley Elkinson

  2. Adis, Auckland, New Zealand

    Anthony Markham

Authors
  1. Anthony Markham
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  2. Shelley Elkinson
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Corresponding author

Correspondence to Shelley Elkinson.

Additional information

This profile has been extracted and modified from the Adis R&D Insight drug pipeline database. Adis R&D Insight tracks drug development worldwide through the entire development process, from discovery, through pre-clinical and clinical studies to market launch.

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Markham, A., Elkinson, S. Luseogliflozin: First Global Approval. Drugs 74, 945–950 (2014). https://doi.org/10.1007/s40265-014-0230-8

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  • DOI: https://doi.org/10.1007/s40265-014-0230-8

Keywords

  • Sitagliptin
  • Glimepiride
  • Fast Plasma Glucose Level
  • Antihyperglycaemic Agent
  • Urinary Glucose Excretion