Skip to main content
Top
Published in: Drugs 8/2014

01-06-2014 | R&D Insight Report

Luseogliflozin: First Global Approval

Authors: Anthony Markham, Shelley Elkinson

Published in: Drugs | Issue 8/2014

Login to get access

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.
Literature
1.
go back to reference 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.CrossRef 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.CrossRef
2.
go back to reference 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.PubMedCrossRef 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.PubMedCrossRef
6.
go back to reference 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.PubMedCrossRef 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.PubMedCrossRef
7.
go back to reference 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. 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.
8.
go back to reference 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.PubMedCentralPubMedCrossRef 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.PubMedCentralPubMedCrossRef
9.
go back to reference 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.CrossRef 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.CrossRef
10.
go back to reference 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.PubMedCentralPubMedCrossRef 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.PubMedCentralPubMedCrossRef
11.
go back to reference 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. 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.
go back to reference 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. 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.
13.
go back to reference 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. 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.
14.
go back to reference 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. 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.
15.
go back to reference 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. 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.
16.
go back to reference 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. 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.
go back to reference 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. 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.
go back to reference 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. 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.
go back to reference 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. 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.
20.
go back to reference 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. 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.
21.
go back to reference 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. 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.
go back to reference 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. 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.
23.
go back to reference 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. 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.
Metadata
Title
Luseogliflozin: First Global Approval
Authors
Anthony Markham
Shelley Elkinson
Publication date
01-06-2014
Publisher
Springer International Publishing
Published in
Drugs / Issue 8/2014
Print ISSN: 0012-6667
Electronic ISSN: 1179-1950
DOI
https://doi.org/10.1007/s40265-014-0230-8

Other articles of this Issue 8/2014

Drugs 8/2014 Go to the issue