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Review

Sodium glucose co-transporter 2 (SGLT2) inhibitors as potential antidiabetic agents

Pages 1531-1540 | Published online: 28 Oct 2005

Keep up to date with the latest research on this topic with citation updates for this article.

Read on this site (4)

Tomasz J. Block, Duygu Batu & Mark E. Cooper. (2022) Recent advances in the pharmacotherapeutic management of diabetic kidney disease. Expert Opinion on Pharmacotherapy 23:7, pages 791-803.
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William N Washburn. (2012) Sodium glucose co-transporter 2 (SGLT2) inhibitors: novel antidiabetic agents. Expert Opinion on Therapeutic Patents 22:5, pages 483-494.
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William N Washburn. (2009) Evolution of sodium glucose co-transporter 2 inhibitors as anti-diabetic agents. Expert Opinion on Therapeutic Patents 19:11, pages 1485-1499.
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Su-Yen Goh, Mariusz Jasik & Mark E Cooper. (2008) Agents in development for the treatment of diabetic nephropathy. Expert Opinion on Emerging Drugs 13:3, pages 447-463.
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Articles from other publishers (36)

Tomasz J. Block & Mark E. Cooper. (2023) Clinical trials with reno-vascular end points in patients with diabetes: Changing the scenario over the past 20 years. La Presse Médicale 52:1, pages 104178.
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Ádám Sipos, Eszter Szennyes, Nikolett Éva Hajnal, Sándor Kun, Katalin E. Szabó, Karen Uray, László Somsák, Tibor Docsa & Éva Bokor. (2021) Dual-Target Compounds against Type 2 Diabetes Mellitus: Proof of Concept for Sodium Dependent Glucose Transporter (SGLT) and Glycogen Phosphorylase (GP) Inhibitors. Pharmaceuticals 14:4, pages 364.
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Ping Wu, Zhenyu Liu, Xiaohong Jiang & Hao Fang. (2020) An Overview of Prospective Drugs for Type 1 and Type 2 Diabetes. Current Drug Targets 21:5, pages 445-457.
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Noha SAYED, Osama ABDALLA, Omnia KILANY, Amina DESSOUKI, Toshinori YOSHIDA, Kazuaki SASAKI & Minoru SHIMODA. (2020) Effect of dapagliflozin alone and in combination with insulin in a rat model of type 1 diabetes. Journal of Veterinary Medical Science 82:4, pages 467-474.
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Kashif Haider, Ankita Pathak, Ankit Rohilla, Md Rafi Haider, Kamal Ahmad & M. Shahar Yar. (2019) Synthetic strategy and SAR studies of C-glucoside heteroaryls as SGLT2 inhibitor: A review. European Journal of Medicinal Chemistry 184, pages 111773.
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Ping Chen, Mengyao Zhao, Qiming Chen, Liqiang Fan, Feng Gao & Liming Zhao. (2019) Absorption Characteristics of Chitobiose and Chitopentaose in the Human Intestinal Cell Line Caco-2 and Everted Gut Sacs. Journal of Agricultural and Food Chemistry 67:16, pages 4513-4523.
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Kai Cao, John A. Brailsford, Ming Yao, Janet Caceres-Cortes, Robert Espina & Samuel J. BonacorsiJrJr. (2017) Synthesis of unlabelled and stable-isotope-labelled glucuronide metabolites of dapagliflozin and synthesis of stable-isotope-labelled dapagliflozin. Journal of Labelled Compounds and Radiopharmaceuticals 60:3, pages 150-159.
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Yonghai Liu, Tingming Fu, Zhidong Chen & Chunyan Ou. (2015) A new and improved process for C-aryl glucoside SGLT2 inhibitors. Monatshefte für Chemie - Chemical Monthly 146:10, pages 1715-1721.
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Sumihiro Nomura, Yasuo Yamamoto, Yosuke Matsumura, Kiyomi Ohba, Shigeki Sakamaki, Hirotaka Kimata, Keiko Nakayama, Chiaki Kuriyama, Yasuaki Matsushita, Kiichiro Ueta & Minoru Tsuda-Tsukimoto. (2013) Novel Indole- N -glucoside, TA-1887 As a Sodium Glucose Cotransporter 2 Inhibitor for Treatment of Type 2 Diabetes . ACS Medicinal Chemistry Letters 5:1, pages 51-55.
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Anita Kapur, Robin O’Connor-Semmes, Elizabeth K Hussey, Robert L Dobbins, Wenli Tao, Marcus Hompesch, Glenn A Smith, Joseph W Polli, Charles D James Jr, Imao Mikoshiba & Derek J Nunez. (2013) First human dose-escalation study with remogliflozin etabonate, a selective inhibitor of the sodium-glucose transporter 2 (SGLT2), in healthy subjects and in subjects with type 2 diabetes mellitus. BMC Pharmacology and Toxicology 14:1.
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Elizabeth K Hussey, Anita Kapur, Robin O’Connor-Semmes, Wenli Tao, Bryan Rafferty, Joseph W Polli, Charles D JamesJrJr & Robert L Dobbins. (2013) Safety, pharmacokinetics and pharmacodynamics of remogliflozin etabonate, a novel SGLT2 inhibitor, and metformin when co-administered in subjects with type 2 diabetes mellitus. BMC Pharmacology and Toxicology 14:1.
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Nobuhiko Fushimi, Hideki Fujikura, Hiroaki Shiohara, Hirotaka Teranishi, Kazuo Shimizu, Shigeru Yonekubo, Kohsuke Ohno, Takashi Miyagi, Fumiaki Itoh, Toshihide Shibazaki, Masaki Tomae, Yukiko Ishikawa-Takemura, Takeshi Nakabayashi, Noboru Kamada, Tomonaga Ozawa, Susumu Kobayashi & Masayuki Isaji. (2012) Structure–activity relationship studies of 4-benzyl-1H-pyrazol-3-yl β-d-glucopyranoside derivatives as potent and selective sodium glucose co-transporter 1 (SGLT1) inhibitors with therapeutic activity on postprandial hyperglycemia. Bioorganic & Medicinal Chemistry 20:22, pages 6598-6612.
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G. Luippold, T. Klein, M. Mark & R. Grempler. (2012) Empagliflozin, a novel potent and selective SGLT‐2 inhibitor, improves glycaemic control alone and in combination with insulin in streptozotocin‐induced diabetic rats, a model of type 1 diabetes mellitus. Diabetes, Obesity and Metabolism 14:7, pages 601-607.
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Ivan SabolićIvana VrhovacDaniela Balen ErorMaria Gerasimova, Michael Rose, Davorka BreljakMarija LjubojevićHrvoje BrzicaAnne Sebastiani, Serge C. Thal, Christoph Sauvant, Helmut Kipp, Volker Vallon & Hermann Koepsell. (2012) Expression of Na + - d -glucose cotransporter SGLT2 in rodents is kidney-specific and exhibits sex and species differences . American Journal of Physiology-Cell Physiology 302:8, pages C1174-C1188.
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E. J. Verspohl. (2012) Novel Pharmacological Approaches to the Treatment of Type 2 Diabetes. Pharmacological Reviews 64:2, pages 188-237.
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Horacio Osorio, Israel Coronel, Abraham Arellano, Ursino Pacheco, Rocío Bautista, Martha Franco & Bruno Escalante. (2012) Sodium-Glucose Cotransporter Inhibition Prevents Oxidative Stress in the Kidney of Diabetic Rats. Oxidative Medicine and Cellular Longevity 2012, pages 1-7.
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Xiaohui Du, Mike Lizarzaburu, Simon Turcotte, Taeweon Lee, Joanne Greenberg, Bei Shan, Peter Fan, Yun Ling, Julio C. Medina & Jonathan Houze. (2011) Optimization of triazoles as novel and potent nonphlorizin SGLT2 inhibitors. Bioorganic & Medicinal Chemistry Letters 21:12, pages 3774-3779.
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Masayuki Isaji. (2011) SGLT2 inhibitors: molecular design and potential differences in effect. Kidney International 79, pages S14-S19.
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Margaret Ryan & Serge A. Jabbour. 2011. Metabolic Syndrome. Metabolic Syndrome 359 375 .
Sumihiro Nomura, Shigeki Sakamaki, Mitsuya Hongu, Eiji Kawanishi, Yuichi Koga, Toshiaki Sakamoto, Yasuo Yamamoto, Kiichiro Ueta, Hirotaka Kimata, Keiko Nakayama & Minoru Tsuda-Tsukimoto. (2010) Discovery of Canagliflozin, a Novel C -Glucoside with Thiophene Ring, as Sodium-Dependent Glucose Cotransporter 2 Inhibitor for the Treatment of Type 2 Diabetes Mellitus . Journal of Medicinal Chemistry 53:17, pages 6355-6360.
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Yong-Hai Liu, Da-Li Li, Qin-Hua Li, Jun-Fang Yang & Lu-De Lu. (2010) Convenient synthesis of [3R-(3α,4β,5α,6β)]-2-[7-chloro-1-(4-ethylbenzyl)-5-methyl-1H-indol-3-yl]-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol. Monatshefte für Chemie - Chemical Monthly 141:8, pages 913-916.
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Elizabeth K. Hussey, Robert L. Dobbins, Randall R. Stoltz, Nancy L. Stockman, Robin L. O'Connor‐Semmes, Anita Kapur, Sharon C. Murray, Debbi Layko & Derek J. R. Nunez. (2013) Multiple‐Dose Pharmacokinetics and Pharmacodynamics of Sergliflozin Etabonate, a Novel Inhibitor of Glucose Reabsorption, in Healthy Overweight and Obese Subjects: A Randomized Double‐Blind Study. The Journal of Clinical Pharmacology 50:6, pages 636-646.
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Elizabeth K. Hussey, Richard V. Clark, Dipti M. Amin, Mark S. Kipnes, Robin L. O'Connor‐Semmes, Eilis C. O'Driscoll, Jenny Leong, Sharon C. Murray, Robert L. Dobbins, Debbi Layko & Derek J. R. Nunez. (2013) Single‐Dose Pharmacokinetics and Pharmacodynamics of Sergliflozin Etabonate, a Novel Inhibitor of Glucose Reabsorption, in Healthy Volunteers and Patients With Type 2 Diabetes Mellitus. The Journal of Clinical Pharmacology 50:6, pages 623-635.
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Hiroyuki Kakinuma, Takahiro Oi, Yuko Hashimoto-Tsuchiya, Masayuki Arai, Yasunori Kawakita, Yoshiki Fukasawa, Izumi Iida, Naoko Hagima, Hiroyuki Takeuchi, Yukihiro Chino, Jun Asami, Lisa Okumura-Kitajima, Fusayo Io, Daisuke Yamamoto, Noriyuki Miyata, Teisuke Takahashi, Saeko Uchida & Koji Yamamoto. (2010) (1 S )-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 . Journal of Medicinal Chemistry 53:8, pages 3247-3261.
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Volker Derdau, Thorsten Fey & Jens Atzrodt. (2010) Synthesis of isotopically labelled SGLT inhibitors and their metabolites. Tetrahedron 66:7, pages 1472-1482.
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Praveen M. Bahadduri, James E. Polli, Peter W. Swaan & Sean Ekins. 2010. Membrane Transporters in Drug Discovery and Development. Membrane Transporters in Drug Discovery and Development 65 103 .
Aleksandra Bołdys & Bogusław Okopień. (2009) Inhibitors of type 2 sodium glucose co-transporters – a new strategy for diabetes treatment. Pharmacological Reports 61:5, pages 778-784.
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Sean R. Werner & John A. Morgan. (2009) Expression of a Dianthus flavonoid glucosyltransferase in Saccharomyces cerevisiae for whole-cell biocatalysis. Journal of Biotechnology 142:3-4, pages 233-241.
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Stefan Balaz. (2009) Modeling Kinetics of Subcellular Disposition of Chemicals. Chemical Reviews 109:5, pages 1793-1899.
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B Komoroski, N Vachharajani, D Boulton, D Kornhauser, M Geraldes, L Li & M Pfister. (2009) Dapagliflozin, a Novel SGLT2 Inhibitor, Induces Dose-Dependent Glucosuria in Healthy Subjects. Clinical Pharmacology & Therapeutics 85:5, pages 520-526.
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B Komoroski, N Vachharajani, Y Feng, L Li, D Kornhauser & M Pfister. (2009) Dapagliflozin, a Novel, Selective SGLT2 Inhibitor, Improved Glycemic Control Over 2 Weeks in Patients With Type 2 Diabetes Mellitus. Clinical Pharmacology & Therapeutics 85:5, pages 513-519.
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William N. Washburn. (2009) Development of the Renal Glucose Reabsorption Inhibitors: A New Mechanism for the Pharmacotherapy of Diabetes Mellitus Type 2. Journal of Medicinal Chemistry 52:7, pages 1785-1794.
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Iskandar Idris & Richard Donnelly. (2009) Sodium-glucose co-transporter-2 inhibitors: an emerging new class of oral antidiabetic drug. Diabetes, Obesity and Metabolism 11:2, pages 79-88.
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Mark I. Lansdell, Denise J. Burring, David Hepworth, Matthew Strawbridge, Emily Graham, Thierry Guyot, Mark S. Betson & James D. Hart. (2008) Design and synthesis of fluorescent SGLT2 inhibitors. Bioorganic & Medicinal Chemistry Letters 18:18, pages 4944-4947.
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S. A. Jabbour & B. J. Goldstein. (2008) Sodium glucose co-transporter 2 inhibitors: blocking renal tubular reabsorption of glucose to improve glycaemic control in patients with diabetes. International Journal of Clinical Practice 62:8, pages 1279-1284.
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Yong Hai Liu, Da Li Li, Lu De Lu & Zhen Yuan Miao. (2008) Convenient synthesis of (2S,3R,4R,5S,6R)-2-(3-(4-ethylbenzyl)-4-chlorophenyl)-6-(hydroxymethyl)-tetrahydro-2H-pyran-3,4,5-triol. Chinese Chemical Letters 19:7, pages 814-816.
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