Dapagliflozin: A review on efficacy, clinical effectiveness and safety

Expert Opinion on Investigational Drugs

Volumn 22, Issue 1, 2013, Pages 131-140

  Paisley, Angela J ^a   Yadav, Rahul ^b   Younis, Naveed ^c   Rao Balakrishna, Prasanna ^c   Soran, Handrean ^d  

^a SALFORD ROYAL NHS FOUNDATION TRUST   (United Kingdom)

^b UNIVERSITY OF MANCHESTER   (United Kingdom)

^c MANCHESTER UNIVERSITY NHS FOUNDATION TRUST   (United Kingdom)

^d MANCHESTER ROYAL INFIRMARY   (United Kingdom)

Author keywords

Dapagliflozin; Glucose; Renal; SGLT2; Type 2 diabetes

Indexed keywords

ANTIDIABETIC AGENT; CANAGLIFLOZIN; DAPAGLIFLOZIN; EGT 0001442; EMPAGLIFLOZIN; ERTUGLIFLOZIN; GLIMEPIRIDE; GLIPIZIDE; GLUCOSE; INSULIN; IPRAGLIFLOZIN; ISIS 388626; KGT 1681; LUSEOGLIFLOZIN; LX 4211; METFORMIN; PIOGLITAZONE; PLACEBO; REMOGLIFLOZIN; SERGLIFLOZIN ETABONATE; SITAGLIPTIN; SODIUM GLUCOSE COTRANSPORTER 2; SULFONYLUREA; TOFOGLIFLOZIN; TS 071; UNCLASSIFIED DRUG;

BLADDER CANCER; BLOOD PRESSURE; BREAST CANCER; CARDIOVASCULAR RISK; CLINICAL EFFECTIVENESS; DRUG DOSE COMPARISON; DRUG DOSE TITRATION; DRUG EFFICACY; DRUG HALF LIFE; DRUG SAFETY; DRUG STRUCTURE; DRUG WITHDRAWAL; EVENING DOSAGE; GENITAL TRACT INFECTION; GLUCOSE HOMEOSTASIS; GLYCEMIC CONTROL; HEMATURIA; HUMAN; HYPOGLYCEMIA; MEDLINE; MONOTHERAPY; MORNING DOSAGE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; PHASE 1 CLINICAL TRIAL (TOPIC); PHASE 2 CLINICAL TRIAL (TOPIC); PHASE 3 CLINICAL TRIAL (TOPIC); REVIEW; RISK; SIDE EFFECT; URINARY TRACT INFECTION; WEIGHT REDUCTION;

ANIMALS; DIABETES MELLITUS, TYPE 2; GLUCOSE; GLUCOSIDES; HUMANS; HYPOGLYCEMIC AGENTS; SODIUM-GLUCOSE TRANSPORTER 2; TREATMENT OUTCOME;

EID: 84871015248     PISSN: 13543784     EISSN: 17447658     Source Type: Journal    
DOI: 10.1517/13543784.2013.740009     Document Type: Review

References (36)

1. World Health Organization diabetes fact sheet. 2011.Available from: http://www.who. int/mediacentre/factsheets/fs312/en/[Cited August 2011]
2. Prentki M, Nolan CJ. Islet beta cell failure in type 2 diabetes. J Clin Invest 2006;116:1802-12
3. Ray KK, Seshasai SR, Wijesuriya S, et al. Effect of intensive control of glucose on cardiovascular outcomes and death in patients with diabetes mellitus: a meta-analysis of randomised controlled trials. Lancet 2009;373:1765-72
4. Del Prato S. Megatrials in type 2 diabetes. From excitement to frustration Diabetologia 2009;52:1219-26
5. Katsiki N, Papanas N, Mikhailidis DP. Dapagliflozin: more than just another oral glucose-lowering agent Expert Opin Investig Drugs 2010;19:1581-9
6. Abdul-Ghani MA, DeFronzo RA. Inhibition of renal glucose reabsorption: a novel strategy for achieving glucose control in type 2 diabetes mellitus. Endocr Pract 2008;14:782-90
7. Wright EM. Renal Na(+)-glucose cotransporters. Am J Physiol Renal Physiol 2001;280:F10-18
8. Rossetti L, Smith D, Shulman GI, et al. Correction of hyperglycemia with phlorizin normalizes tissue sensitivity to insulin in diabetic rats. J Clin Invest 1987;79:1510-15
9. Chao EC A paradigm shift in diabetes therapy-dapagliflozin and other SGLT2 inhibitors. Discov Med 2011;11:255-63
10. Rosenstock J, Aggarwal N, Polidori D, et al. Dose-ranging effects of canagliflozin, a sodium-glucose cotransporter 2 inhibitor, as add-on to metformin in subjects with type 2 diabetes. Diabetes Care 2012;35:1232-8
11. FDA. FDA Briefing Document-NDA 202293. Advisory Committee Meeting (July 19, 2011). Dapagliflozin Tablets, 5 and 10 mg. Sponsor: Bristol-Myers Squibb. [Briefing Document]. 2011.Available from: http://www.fda.gov/downloads/ AdvisoryCommittees/CommitteesMeetingMaterials/drugs/ EndocrinologicandMetabolicDrugs AdvisoryCommittee/ucm262994.pdf
12. European Medicines Agency recommends authorisation of novel treatment for type 2 diabetes-Press release. 2012.Available from: http://www.ema. europa.eu/ema/index.jspcurl=pages/news-and-events/news/2012/04/ news-detail-001499.jsp&mid=WC0b01ac058004d5c1
13. 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;51:1145-9
14. Komoroski B, Vachharajani N, Boulton D, et al. Dapagliflozin, a novel SGLT2 inhibitor, induces dose-dependent glucosuria in healthy subjects. Clin Pharmacol Ther 2009;85:520-6
15. Han S, Hagan DL, Taylor JR, et al. Dapagliflozin, a selective SGLT2 inhibitor, improves glucose homeostasis in normal and diabetic rats. Diabetes 2008;57:1723-9
16. Komoroski B, Vachharajani N, Feng Y, et al. Dapagliflozin, a novel, selective SGLT2 inhibitor, improved glycemic control over 2 weeks in patients with type 2 diabetes mellitus. Clin Pharmacol Ther 2009;85:513-19
17. List JF, Woo V, Morales E, et al. Sodium-glucose cotransport inhibition with dapagliflozin in type 2 diabetes. Diabetes Care 2009;32:650-7
18. Wilding JP, Norwood P, T'Joen C, et al. A study of dapagliflozin in patients with type 2 diabetes receiving high doses of insulin plus insulin sensitizers: applicability of a novel insulin-independent treatment. Diabetes Care 2009;32:1656-62
19. Zhang L, Feng Y, List J, et al. Dapagliflozin treatment in patients with different stages of type 2 diabetes mellitus: effects on glycaemic control and body weight. Diabetes Obes Metab 2010;12:510-16
20. Bailey CJ, Gross JL, Pieters A, et al. Effect of dapagliflozin in patients with type 2 diabetes who have inadequate glycaemic control with metformin: a randomised, double-blind, placebo-controlled trial. Lancet 2010;375:2223-33
21. Squibb B-M. A study ofBMS-512148 (Dapagliflozin) in patients with type 2 diabetes with inadequately controlled hypertension on an ACEI or ARB and an additional antihypertensive medication. 2010. Available from: http://clinicaltrials.gov/ct2/show/NCT01195662 term=dapagliflozin+AND+blood +pressure&rank=1
22. Squibb B-M. A study of BMS-512148 (Dapagliflozin) in patients with type 2 diabetes with inadequately controlled hypertension on an angiotensin-converting enzyme inhibitor (ACEI) or angiotensin receptor blocker (ARB). 2010.Available from: http://clinicaltrials. gov/ct2/show/NCT01137474 term= dapagliflozin+AND+blood +pressure&rank=2
23. Ferrannini E, Ramos SJ, Salsali A, et al. Dapagliflozin monotherapy in type 2 diabetic patients with inadequate glycemic control by diet and exercise: a randomized, double-blind, placebo-controlled, phase 3 trial. Diabetes Care 2010;33:2217-24
24. Wilding JP, Woo V, Soler NG, et al. Long-term efficacy of dapagliflozin in patients with type 2 diabetes mellitus receiving high doses of insulin: a randomized trial. Ann Intern Med 2012;156:405-15
25. Strojek K, Yoon KH, Hruba V, et al. Effect of dapagliflozin in patients with type 2 diabetes who have inadequate glycaemic control with glimepiride: a randomized, 24-week, double-blind, placebo-controlled trial. Diabetes Obes Metab 2011;13:928-38
26. Nauck MA, Del Prato S, Meier JJ, et al. Dapagliflozin versus glipizide as add-on therapy in patients with type 2 diabetes who have inadequate glycemic control with metformin: a randomized, 52-week, double-blind, active-controlled noninferiority trial. Diabetes Care 2011;34:2015-22
27. Rosenstock J, Vico M, Wei L, et al. Effects of dapagliflozin, a sodium-glucose cotransporter-2 inhibitor, on hemoglobin A1c, body weight, and hypoglycemia risk in patients with type 2 diabetes inadequately controlled on pioglitazone monotherapy. Diabetes Care 2012;35:1473-8
28. Bolinder J, Ljunggren O, Kullberg J. Effects of dapagliflozin on body weight, total fat mass, and regional adipose tissue distribution in patients with type 2 diabetes mellitus with inadequate glycemic control on metformin. J Clin Endocrinol Metab 2012;97:1020-31
29. Henry RR, Murray AV, Marmolejo MH. Dapagliflozin, metformin XR, or both: initial pharmacotherapy for type 2 diabetes, a randomised controlled trial. Int J Clin Pract 2012;66:446-56
30. de Leon EM, Jacober SJ, Sobel JD, et al. Prevalence and risk factors for vaginal Candida colonization in women with type 1 and type 2 diabetes. BMC Infect Dis 2002;2:1
31. Kasichayanula S, Liu X, Zhang W, et al. Influence of hepatic impairment on the pharmacokinetics and safety profile of dapagliflozin: an open-label, parallel-group, single-dose study. Clin Ther 2011;33:1798-808
32. Ljunggren O, Bolinder J, Johansson L, et al. Dapagliflozin has no effect on markers of bone formation and resorption or bone mineral density in patients with inadequately controlled type 2 diabetes mellitus on metformin. Diabetes Obes Metab 2012;14(11):990-9
33. FDA briefing document: dapagliflozin tablets 5 and 10 mg. 2011.Available from: http://www.fda.gov/downloads/AdvisoryCommittees/ CommitteesMeetingMaterials/Drugs/EndocrinologicandMetabolicDrugs AdvisoryCommittee/UCM262994.pdf
34. Macdonald FR, Peel JE, Jones HB, et al. The novel sodium glucose transporter 2 inhibitor dapagliflozin sustains pancreatic function and preserves islet morphology in obese, diabetic rats. Diabetes Obes Metab 2010;12:1004-12
35. Kasichayanula S, Liu X, Shyu W C, et al. Lack of pharmacokinetic interaction between dapagliflozin, a novel sodium-glucose transporter 2 inhibitor, and metformin, pioglitazone, glimepiride or sitagliptin in healthy subjects. Diabetes Obes Metab 2011;13:47-54
36. Kannel WB, McGee DL. Diabetes and cardiovascular disease. The Framingham study. JAMA 1979;241:2035-8