Skip to main content
SpringerLink
Log in

Ipragliflozin: First Global Approval

  • R&D Insight Report
  • Published:
Drugs Aims and scope Submit manuscript

Abstract

Ipragliflozin (Suglat® [Japan]), an orally active, next-generation sodium-glucose transporter 2 (SGLT2) inhibitor, has been developed by Astellas Pharma and Kotobuki Pharmaceutical for the treatment of type 2 diabetes mellitus. Ipragliflozin has received its first global approval in this indication in Japan, for use as monotherapy or in combination with another antihyperglycaemic agent (metformin, pioglitazone, a sulfonylurea, an α-glucosidase inhibitor, a dipeptidylpeptidase-4 inhibitor or nateglinide). Ipragliflozin is the first SGLT2 inhibitor to be approved in Japan. This article summarizes the milestones in the development of ipragliflozin leading to this first approval for the treatment of type 2 diabetes mellitus.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Similar content being viewed by others

References

  1. Imamura M, Nakanishi K, Suzuki T, et al. Discovery of ipragliflozin (ASP1941): a novel C-glucoside with benzothiophene structure as a potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes mellitus. Bioorg Med Chem. 2012;20(10):3263–79.

    Article  CAS  PubMed  Google Scholar 

  2. Veltkamp SA, Kadokura T, Krauwinkel WJJ, et al. Effect of ipragliflozin (ASP1941), a novel selective sodium-dependent glucose co-transporter 2 inhibitor, on urinary glucose excretion in healthy subjects. Clin Drug Investig. 2011;31(12):839–51.

    Article  CAS  PubMed  Google Scholar 

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

    Article  CAS  PubMed  Google Scholar 

  4. Misra M. SGLT2 inhibitors: a promising new therapeutic option for treatment of type 2 diabetes mellitus. J Pharm Pharmacol. 2013;65(3):317–27.

    Article  CAS  PubMed  Google Scholar 

  5. Cangoz S, Chang YY, Chempakaseril SJ, et al. The kidney as a new target for antidiabetic drugs: SGLT2 inhibitors. J Clin Pharm Ther. 2013;38(5):350–9.

    Article  CAS  PubMed  Google Scholar 

  6. Kadokura T, Saito M, Utsuno A, et al. Ipragliflozin (ASP1941), a selective sodium-dependent glucose cotransporter 2 inhibitor, safely stimulates urinary glucose excretion without inducing hypoglycemia in healthy Japanese subjects. Diabetol Int. 2011;2(4):172–82.

    Article  Google Scholar 

  7. Tahara A, Kurosaki E, Yokono M, et al. Effects of SGLT2 selective inhibitor ipragliflozin on hyperglycemia, hyperlipidemia, hepatic steatosis, oxidative stress, inflammation, and obesity in type 2 diabetic mice. Eur J Pharmacol. 2013;715(1–3):246–55.

    Article  CAS  PubMed  Google Scholar 

  8. Astellas Pharma Inc. Approval of Suglat(Rm) tablets, a selective SGLT2 inhibitor for treatment of type 2 diabetes, in Japan. Media Release. 2014.

  9. Astellas Pharma Inc. R&D Pipeline (November 2012). 2012. http://www.astellas.com/en/ir/library/pdf/2q2013_rd_en.pdf. Accessed.

  10. Astellas Pharma Inc. Financial Results for 2Q/FY2012 Ending March 31, 2013. 2012. http://www.astellas.com/en/ir/library/pdf/2q2013pre_en.pdf. Accessed.

  11. Astellas Pharma Inc., Msd K.K. Astellas and MSD enter co-promotion agreement in Japan for ipragliflozin, SGLT2 inhibitor for treatment of type 2 diabetes. Media Release. 2013.

  12. Tahara A, Kurosaki E, Yokono M, et al. Pharmacological profile of ipragliflozin (ASP1941), a novel selective SGLT2 inhibitor, in vitro and in vivo. Naunyn-Schmiedebergs Arch Pharmacol. 2012;385(4):423–36.

    Article  CAS  PubMed  Google Scholar 

  13. Tahara A, Kurosaki E, Yokono M, et al. Antidiabetic effects of SGLT2-selective inhibitor ipragliflozin in streptozotocin-nicotinamide-induced mildly diabetic mice. J Pharmacol Sci. 2012;120(1):36–44.

    Article  CAS  PubMed  Google Scholar 

  14. Smulders RA, Leeflang S, Schliess F, et al. The effect of ipragliflozin on the total glucose turnover after OGTT in healthy subjects and patients with type 2 diabetes mellitus. Diabetologia. 2013;56(Suppl):S399–400.

    Google Scholar 

  15. Akiyama N, Kashiwagi A, Kadokura T, et al. ASP1941, a novel, selective SGLT2 inhibitor improved both fasting and postprandial glucose levels in Japanese type 2 diabetic patients. Diabetes. 2011;60(Suppl 1):A280–1.

    Google Scholar 

  16. Zhang W, Smulders R, Abeyratne A, et al. Ipragliflozin does not prolong QTc interval in healthy male and female subjects: a phase I study. Clin Ther. 2013;35(8):1150–61.e3.

    Google Scholar 

  17. Zhang W, Krauwinkel WJJ, Keirns J, et al. The effect of moderate hepatic impairment on the pharmacokinetics of ipragliflozin, a novel sodium glucose co-transporter 2 (SGLT2) inhibitor. Clin Drug Investig. 2013;33(7):489–96.

    Article  CAS  PubMed  Google Scholar 

  18. Schwartz SL, Akinlade B, Klasen S, et al. Safety, pharmacokinetic, and pharmacodynamic profiles of ipragliflozin (ASP1941), a novel and selective inhibitor of sodium-dependent glucose co-transporter 2, in patients with type 2 diabetes mellitus. Diabetes Technol Ther. 2011;13(12):1219–27.

    Article  CAS  PubMed  Google Scholar 

  19. Kadokura T, Ishikawa H, Nakajo I, et al. The effect of renal impairment on the pharmacokinetics and urinary glucose excretion of the SGLT2 inhibitor ipragliflozin (ASP1941) in Japanese type 2 diabetes mellitus patients. Diabetologia. 2011;54:S346.

    Google Scholar 

  20. Nakajo I, Taniuchi Y, Yoshida S, et al. Drug interaction study of ipragliflozin and migitol in healthy Japanese subjects. Clin Pharmacol Ther. 2012;91:S11.

    Google Scholar 

  21. Zhang W, et al. Lack of pharmacokinetic interactions between Asp1941, a selective sodium glucose co-transporter 2 (Sglt2) inhibitor, and pioglitazone in healthy subjects. Clin Pharmacol Ther. 2011;89(Suppl 1):S82.

    Google Scholar 

  22. Smulders RA, Zhang W, Veltkamp SA, et al. No pharmacokinetic interaction between ipragliflozin and sitagliptin, pioglitazone, or glimepiride in healthy subjects. Diabetes Obes Metab. 2012;14(10):937–43.

    Article  CAS  PubMed  Google Scholar 

  23. Zhang W, et al. Lack of pharmacokinetic interactions between Asp 1941, a selective sodium glucose co-transporter 2 (Sglt2) inhibitor, and sitagliptin in healthy subjects. Clin Pharmacol Ther. 2011;89(Suppl 1):S81–2.

    Google Scholar 

  24. Veltkamp SA, Van Dijk J, Krauwinkel WJ, et al. Lack of pharmacokinetic and pharmacodynamic interaction between ipragliflozin, a selective sodium glucose co-transporter 2 (SGLT2) inhibitor, and glimepiride in healthy subjects. Clin Pharmacol Ther. 2012;91:S11–2.

    Google Scholar 

  25. Veltkamp SA, van Dijk J, Collins C, et al. Combination treatment with ipragliflozin and metformin: a randomized, double-blind, placebo-controlled study in patients with type 2 diabetes mellitus. Clin Ther. 2012;34(8):1761–71.

    Article  CAS  PubMed  Google Scholar 

  26. Goto K, Kashiwagi A, Kazuta K, et al. Ipragliflozin reduces A1C and body weight in type 2 diabetes patients who have inadequate glycemic control on metformin alone: Illuminate study. Diabetes. 2012;61:A269.

    Google Scholar 

  27. Kashiwagi A, Shiga T, Akiyama N, et al. Ipragliflozin reduced HbA1c and body weight in Japanese type 2 diabetes patients who have inadequate glycaemic control on sulfonylurea or pioglitazone alone. Diabetologia. 2012;55:S302–3.

    Google Scholar 

  28. Wilding JPH, Ferrannini E, Fonseca VA, et al. Efficacy and safety of ipragliflozin in patients with type 2 diabetes inadequately controlled on metformin: a dose-finding study. Diabetes Obes Metab. 2013;15(5):403–9.

    Article  CAS  PubMed  Google Scholar 

  29. Kashiwagi A, Takinami Y, Kazuta K, et al. Ipragliflozin improved glycaemic control with additional benefits of reductions of body weight and blood pressure in Japanese patients with type 2 diabetes mellitus: BRIGHTEN Study. Diabetologia. 2011;54:S68–9.

    Google Scholar 

  30. Kawano H, Kashiwagi A, Kazuta K, et al. Long-term safety, tolerability and efficacy of ipragliflozin in Japanese patients with type 2 diabetes mellitus: Ignite. Diabetes. 2012;61:A610.

    Article  Google Scholar 

  31. Fonseca VA, Ferrannini E, Wilding JP, et al. Active- and placebo-controlled dose-finding study to assess the efficacy, safety, and tolerability of multiple doses of ipragliflozin in patients with type 2 diabetes mellitus. J Diabetes Complicat. 2013;27(3):268–73.

    Article  PubMed  Google Scholar 

Download references

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. R. Poole is a contracted employee of Adis, Springer SBM. R. Dungo is a salaried employee of Adis, Springer SBM.

Author information

Authors and Affiliations

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

    Rosselle T. Dungo

  2. Adis, Auckland, New Zealand

    Raewyn M. Poole

Authors
  1. Raewyn M. Poole
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Rosselle T. Dungo
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Rosselle T. Dungo.

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.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Poole, R.M., Dungo, R.T. Ipragliflozin: First Global Approval. Drugs 74, 611–617 (2014). https://doi.org/10.1007/s40265-014-0204-x

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s40265-014-0204-x

Keywords

Search

Navigation