An update of SGLT1 and SGLT2 inhibitors in early phase diabetes-type 2 clinical trials

References

• Diabetes Atlas. 2017. International diabetes Federation. 8th ed.
   Google Scholar
• American Diabetes Association. Classification and diagnosis of diabetes. Diabetes Care. 2015;38(Supplement 1):S8–S16.
   Google Scholar
• Adeghate E, Schattner P, Dunn E. An update on the etiology and epidemiology of diabetes mellitus. Ann NY Acad Sci. 2006;1084:1–29.
   PubMed Web of Science ®Google Scholar
• Ali O. Genetics of type 2 diabetes. World J Diabetes. 2013;4:114–123.
   PubMedGoogle Scholar
• Hediger MA, Turk E, Wright EM. Homology of the human intestinal Na+/glucose and escherichia coli Na+/proline cotransporters. Proc Natl Acad Sci USA. 1989;86:5748–5752.
   PubMed Web of Science ®Google Scholar
• Ghezzi C, Loo DDF, Wright EM. Physiology of renal glucose handling via SGLT1, SGLT2 and GLUT2. Diabetologia. 2018;61:2087–2097.
   PubMed Web of Science ®Google Scholar
• Chasis H, Jolliffe N, Smith HW. The action of phlorizin on the excretion of glucose, xylose, sucrose, creatinine and urea by man. J Clin Invest. 1933;12:1083–1090.
   PubMedGoogle Scholar
• Hopfer U, Nelson K, Perrotto J, et al. Glucose transport in isolated brush border membrane from rat small intestine. J Biol Chem. 1973;248:25–32.
   PubMed Web of Science ®Google Scholar
• Sala-Rabanal M, Hirayama BA, Ghezzi C, et al. Revisiting the physiological roles of SGLTs and GLUTs using positron emission tomography in mice. J Physiol. 2016;594:4425–4438.
   PubMed Web of Science ®Google Scholar
• Hediger MA, Coady MJ, Ikeda TS, et al. Expression cloning and cDNA sequencing of the Na+/glucose co-transporter. Nature. 1987;330:379–381.
   PubMed Web of Science ®Google Scholar
• Lotfy M, Adeghate J, Kalasz H, et al. Chronic complications of diabetes mellitus: a mini review. Curr Diabetes Rev. 2017;13:3–10.
   PubMed Web of Science ®Google Scholar
• De Koninck L. About the phloridzin (phlorrhizin). Ann Pharm. 1835;15:75–77.
   Google Scholar
• Blaschek W. Natural products as lead Compounds for sodium glucose cotransporter (SGLT) inhibitors. Planta Med. 2017;83:985–993.
   PubMed Web of Science ®Google Scholar
• Zemplen G, Bognar R. Synthese des natürlichen Phlorrhizins. Chem Ber. 1942;75:1040.
   Google Scholar
• Von Mering J. Über künstlichen Diabetes. Centralbl Med Wiss. 1886;22:531.
   Google Scholar
• Lee WS, Wells RG, Hediger MA. The high affinity Na/glucose cotransporter: reevaluation and distribution of expression. J Biol Chem. 1994;268:12032–12039.
   Google Scholar
• Link JT, Sorensen BK. A method for preparing C-glycosides related to phlorizin. Tetrahedron Lett. 2000;41:9213–9217.
   Web of Science ®Google Scholar
• Meng W, Ellsworth BA, Nirschl AA, et al. Discovery of dapagliflozin: A potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes. J Med Chem. 2008;51:1145–1149.
   PubMed Web of Science ®Google Scholar
• Jung CH, Jang JE, Park JY. A novel therapeutic agent for type 2 diabetes mellitus: SGLT2 inhibitor. Diabetes Metab J. 2014;38:261–273.
   PubMedGoogle Scholar
• Kurosaki E, Ogasawara H. Ipragliflozin and other sodium-glucose cotransporter-2 (SGLT2) inhibitors in the treatment of type 2 diabetes: preclinical and clinical data. Pharmacol Ther. 2013;139:51–59.
   PubMed Web of Science ®Google Scholar
• Vrhovac I, Balen Eror D, Klessen D, et al. Localizations of Na(+)-D-glucose cotransporters SGLT1 and SGLT2 in human kidney and of SGLT1 in human small intestine, liver, lung, and heart. Pflugers Arch. 2015;467:1881–1898.
   PubMed Web of Science ®Google Scholar
• Abdul-Ghani MA, Norton L, DeFronzo RA. Role of sodium-glucose cotransporter 2 (SGLT 2) inhibitors in the treatment of type 2 diabetes. Endocr Rev. 2011;32:515–531.
   PubMed Web of Science ®Google Scholar
• Cariou B, Charbonnel B. Sotagliflozin as a potential treatment for type 2 diabetes mellitus. Expert Opin Investig Drugs. 2015;24:1647–1656.
   PubMed Web of Science ®Google Scholar
• He YL, Haynes W, Meyers CD, et al. The effects of licogliflozin, a dual SGLT1/2 inhibitor, on body weight in obese patients with or without diabetes. Diabetes Obes Metab. 2019;21:1311–1321.
   PubMed Web of Science ®Google Scholar
• Cefalo CMA, Cinti F, Moffa S, et al. Sotagliflozin, the first dual SGLT inhibitor: current outlook and perspectives. Cardiovasc Diabetol. 2019;18:20.
   PubMed Web of Science ®Google Scholar
• Garg SK, Henry RR, Banks P, et al. Effects of sotagliflozin added to insulin in patients with type 1 diabetes. N Engl J Med. 2017;377:2337–2348.
   PubMed Web of Science ®Google Scholar
• Johnsson K, Johnsson E, Mansfield TA, et al. Osmotic diuresis with SGLT2 inhibition: analysis of events related to volume reduction in dapagliflozin clinical trials. Postgrad Med. 2016;128:346–355.
   PubMed Web of Science ®Google Scholar
• Kmietowicz Z. SGLT2 inhibitors for diabetes are linked to increased risk of lower limb amputation. BMJ. 2018;363:k4828.
   PubMedGoogle Scholar
• Dicembrini I, Tomberli B, Nreu B, et al. Peripheral artery disease and amputations with sodium-glucose co-transporter-2 (SGLT-2) inhibitors: a meta-analysis of randomized controlled trials. Diabetes Res Clin Pract. 2019;153:138–144.
   PubMed Web of Science ®Google Scholar
• Beitelshees AL, Leslie BR, Taylor SI. Sodium-glucose cotransporter 2 inhibitors: a case study in translational research. Diabetes. 2019;68:1109–1120.
   PubMed Web of Science ®Google Scholar
• Bersoff-Matcha SJ, Chamberlain C, Cao C, et al. Fournier gangrene associated with sodium-glucose cotransporter-2 inhibitors: a review of spontaneous post-marketing cases. Ann Intern Med. 2019 May 7. [Epub ahead of print]. DOI:10.7326/M19-0085.
   PubMed Web of Science ®Google Scholar
• Kasichayanula S, Liu X, Lacreta F, et al. Clinical pharmacokinetics and pharmacodynamics of dapagliflozin, a selective inhibitor of sodium-glucose co-transporter type 2. Clin Pharmacokinet. 2014;53:17–27.
   PubMed Web of Science ®Google Scholar
• Wiviott SD, Raz I, Bonaca MP, et al. Dapagliflozin and cardiovascular outcomes in type 2 diabetes. N Engl J Med. 2019;380:347–357.
   PubMed Web of Science ®Google Scholar
• Mosenzon O, Wiviott SD, Cahn A, et al. Effects of dapagliflozin on development and progression of kidney disease in patients with type 2 diabetes: an analysis from the DECLARE-TIMI 58 randomised trial. Lancet Diabetes Endocrinol. 2019;pii: S2213-8587(19):30180–30189.
   Google Scholar
• Neal B, Perkovic V, Mahaffey KW, et al. Canagliflozin and cardiovascular and renal events in type 2 diabetes. N Engl J Med. 2017;377:644–657.
   PubMed Web of Science ®Google Scholar
• Mahaffey KW, Neal B, Perkovic V, et al. Canagliflozin for primary and secondary prevention of cardiovascular events: results from the CANVAS program (canagliflozin cardiovascular assessment study). Circulation. 2018;137:323–334.
   PubMed Web of Science ®Google Scholar
• Mahaffey KW, Jardine MJ, Bompoint S, et al. Canagliflozin and cardiovascular and renal outcomes in type 2 diabetes and chronic kidney disease in primary and secondary cardiovascular prevention groups: results from the randomized CREDENCE trial. Circulation. 2019 Jul 11. [Epub ahead of print]. DOI:10.1161/CIRCULATIONAHA.119.042007.
   Web of Science ®Google Scholar
• Perkovic V, Jardine MJ, Neal B, et al. Canagliflozin and renal outcomes in type 2 diabetes and nephropathy. N Engl J Med. 2019;380(24):2295–2306.
   PubMed Web of Science ®Google Scholar
• Zinman B, Wanner C, Lachin JM, et al. Empagliflozin, cardiovascular outcomes, and mortality in type 2 diabetes. N Engl J Med. 2015;373:2117–2128.
   PubMed Web of Science ®Google Scholar
• Sizar O, Talati R. Empagliflozin. Sourcestatpearls [internet]. Treasure Island (FL): StatPearls Publishing; 2019 Jan 16.
   Google Scholar
• Abdul-Ghani M, Del Prato S, Chilton R, et al. SGLT2 inhibitors and cardiovascular risk: lessons learned from the EMPA-REG OUTCOME study. Diabetes Care. 2016;39:717–725.
   PubMed Web of Science ®Google Scholar
• Fitchett D, Inzucchi SE, Lachin JM, et al. Cardiovascular mortality reduction with empagliflozin in patients with type 2 diabetes and cardiovascular disease. J Am Coll Cardiol. 2018;71:364–367.
   PubMed Web of Science ®Google Scholar
• Butler J, Zannad F, Fitchett D, et al. Empagliflozin improves kidney outcomes in patients with or without heart failure. Circ Heart Fail. 2019;12:e005875.
   PubMed Web of Science ®Google Scholar
• Grunberger G, Camp S, Johnson J, et al. Ertugliflozin in patients with stage 3 chronic kidney disease and type 2 diabetes mellitus: the VERTIS RENAL randomized study. Diabetes Ther. 2018;9:49–66.
   PubMed Web of Science ®Google Scholar
• Aronson R, Frias J, Goldman A, et al. Long-term efficacy and safety of ertugliflozin monotherapy in patients with inadequately controlled T2DM despite diet and exercise: VERTIS MONO extension study. Diabetes Obes Metab. 2018;20:1453–1460.
   PubMed Web of Science ®Google Scholar
• [cited 2019 Jul 18]. Available from: https://clinicaltrials.gov/ct2/show/NCT01986881?term=Ertugliflozin&rank=7
   Google Scholar
• Cannon CP, McGuire DK, Pratley R, et al. Design and baseline characteristics of the eValuation of ERTugliflozin effIcacy and safety cardioVascular outcomes trial (VERTIS-CV). Am Heart J. 2018;206:11–23.
   PubMed Web of Science ®Google Scholar
• Nakamura I, Maegawa H, Tobe K, et al. Safety and efficacy of ipragliflozin in Japanese patients with type 2 diabetes in real-world clinical practice: interim results of the STELLA-LONG TERM post-marketing surveillance study. Expert Opin Pharmacother. 2018;19:189–201.
   PubMed Web of Science ®Google Scholar
• Veltkamp SA, Kadokura T, Krauwinkel WJ, 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;31:839–851.
   PubMed Web of Science ®Google Scholar
• Ohkura T. Ipragliflozin: A novel sodium-glucose co-transporter 2 inhibitor developed in Japan. World J Diabetes. 2015;6:136–144.
   PubMed Web of Science ®Google Scholar
• Utsunomiya K, Senda M, Kakiuchi S, et al. Safety and efficacy of tofogliflozin in Japanese patients with type 2 diabetes mellitus in real-world clinical practice: Results of 3-month interim analysis of a long-term post-marketing surveillance study (J-STEP/LT). J Diabetes Investig. 2019 Jan 31. [Epub ahead of print]. DOI:10.1111/jdi.13017.
   Web of Science ®Google Scholar
• Danni T, Cariou B, Buse JB, et al. Improved time in range and glycemic variability with sotagliflozin in combination with insulin in adults with type 1 diabetes: a pooled analysis of 24-week continuous glucose monitoring data from the in tandem program. Diabetes Care. 2019 Mar 4;pii: dc182149. [Epub ahead of print]. DOI: 10.2337/dc18-2149.
   Google Scholar
• [cited 2019 Mar 15]. Available from: https://www.diabetes.co.uk/news/2018/mar/sotagliflozin-accepted-by-ema-for-review-in-treating-people-with-type-1-diabetes-97785339.html
   Google Scholar
• Busch RS, Kane MP. Combination SGLT2 inhibitor and GLP-1 receptor agonist therapy: a complementary approach to the treatment of type 2 diabetes. Postgrad Med. 2017;129:686–697.
   Google Scholar
• Musso G, Gambino R professor, Cassader M, et al. Efficacy and safety of dual SGLT 1/2 inhibitor sotagliflozin in type 1 diabetes: meta-analysis of randomised controlled trials. BMJ. 2019;365:l1328.
   PubMedGoogle Scholar
• Sasaki T, Sugawara M, Fukuda M. Sodium-glucose cotransporter 2 inhibitor-induced changes in body composition and simultaneous changes in metabolic profile: 52-week prospective LIGHT (luseogliflozin: the components of weight loss in Japanese patients with type 2 diabetes mellitus) study. J Diabetes Investig. 2019;10:108–117.
   PubMed Web of Science ®Google Scholar
• Sumida Y, Murotani K, Saito M, et al. Effect of luseogliflozin on hepatic fat content in type 2 diabetes patients with non-alcoholic fatty liver disease: A prospective, single-arm trial (LEAD trial). Hepatol Res. 2019;49:64–71.
   PubMed Web of Science ®Google Scholar
• Markham A, Elkinson S. Luseogliflozin: first global approval. Drugs. 2014;74:945–950.
   PubMed Web of Science ®Google Scholar
• Samukawa Y, Haneda M, Seino Y, et al. Pharmacokinetics and Pharmacodynamics of luseogliflozin, a selective SGLT2 inhibitor, in Japanese patients with type 2 diabetes with mild to severe renal impairment. Clin Pharmacol Drug Dev. 2018;7:820–828.
   PubMed Web of Science ®Google Scholar
• Dash RP, Babu RJ, Srinivas NR. Comparative pharmacokinetics of three SGLT-2 inhibitors sergliflozin, remogliflozin and ertugliflozin: an overview. Xenobiotica. 2017;47:1015–1026.
   PubMed Web of Science ®Google Scholar
• [cited 2019 Mar 16]. Available from: https://finance.yahoo.com/news/avolynt-announces-completion-phase-2b-143600142.html
   Google Scholar
• Markham A. Remogliflozin etabonate: first global approval. Drugs. 2019;79:1157–1161.
   PubMed Web of Science ®Google Scholar
• [cited 2019 Jul 18]. Available from: https://www.prnewswire.com/in/news-releases/glenmark-launches-novel-globally-researched-anti-diabetes-drug-remogliflozin-in-india-806614073.html
   Google Scholar
• Mikhail N. Remogliflozin etabonate: a novel SGLT2 inhibitor for treatment of diabetes mellitus. Expert Opin Investig Drugs. 2015;24:1381–1387.
   PubMed Web of Science ®Google Scholar
• Meier A, de Laat M, Reiche D, et al. The efficacy and safety of velagliflozin over 16 weeks as a treatment for insulin dysregulation in ponies. BMC Vet Res. 2019;15:65.
   PubMed Web of Science ®Google Scholar
• Yong X, Wen A, Liu X, et al. Pharmacokinetics and pharmacodynamics of henagliflozin, a sodium glucose co-transporter 2 inhibitor, in Chinese patients with type 2 diabetes mellitus. Clin Drug Investig. 2016;36:195–202.
   PubMed Web of Science ®Google Scholar
• [Cited 2019 April 20]. Available from: http://www.hrs.com.cn/hren/products_pipeline_metabolics.html
   Google Scholar
• Halvorsen YD, Walford GA, Massaro J, et al. 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 Jul 12. [Epub ahead of print]. DOI:10.1111/dom.13833.
   Web of Science ®Google Scholar
• Scheen AJ. An update on the safety of SGLT2 inhibitors. Expert Opin Drug Saf. 2019;18:295–311.
   PubMed Web of Science ®Google Scholar
• Zelniker TA, Wiviott SD, Raz I, et al. Comparison of the effects of glucagon-like peptide receptor agonists and sodium-glucose cotransporter 2 inhibitors for prevention of major adverse cardiovascular and renal outcomes in type 2 diabetes mellitus. Circulation. 2019;139:2022–2031.
   PubMed Web of Science ®Google Scholar
• Lotfy M, Singh J, Kalász H, et al. Medicinal chemistry and applications of incretins and dpp-4 inhibitors in the treatment of type 2 diabetes mellitus. Open Med Chem J. 2011;5(Suppl 2):82–92.
   PubMedGoogle Scholar
• Li J, Gong Y, Li C, et al. Long-term efficacy and safety of sodium-glucose cotransporter-2 inhibitors as add-on to metformin treatment in the management of type 2 diabetes mellitus: A meta-analysis. Medicine (Baltimore). 2017;96:e7201.
   PubMed Web of Science ®Google Scholar
• Busch RS, Kane MP. Combination SGLT2 inhibitor and GLP-1 receptor agonist therapy: a complementary approach to the treatment of type 2 diabetes. Postgrad Med. 2017;129:686–697.
   PubMed Web of Science ®Google Scholar