Pharmacokinetics and pharmacodynamics of canagliflozin, a sodium glucose co-transporter 2 inhibitor, in subjects with type 2 diabetes mellitus

Journal of Clinical Pharmacology

Volumn 53, Issue 6, 2013, Pages 601-610

  Devineni, Damayanthi ^a   Curtin, Christopher R ^a   Polidori, David ^b   Gutierrez, Maria J ^c   Murphy, Joseph ^a   Rusch, Sarah ^b   Rothenberg, Paul L ^a  

^a JANSSEN RESEARCH AND DEVELOPMENT   (United States)

^b JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

^c Janssen Research and Development ^*  (United States)

Author keywords

Canagliflozin; Pharmacodynamics; Pharmacokinetics; Sodium glucose co transporter 2 inhibitor; Type 2 diabetes mellitus

Indexed keywords

CANAGLIFLOZIN; DRUG METABOLITE; GLUCOSE; GLUCURONIDE; O GLUCURONIDE; PLACEBO; UNCLASSIFIED DRUG;

ADULT; AGED; AREA UNDER THE CURVE; ARTICLE; CLINICAL ARTICLE; CONSTIPATION; CONTROLLED STUDY; DOSE RESPONSE; DOUBLE BLIND PROCEDURE; DRUG BLOOD LEVEL; DRUG HALF LIFE; DRUG INDUCED HEADACHE; DRUG METABOLISM; DRUG SAFETY; FEMALE; GLUCOSE URINE LEVEL; HALF LIFE TIME; HUMAN; HYPOGLYCEMIA; MALE; MAXIMUM PLASMA CONCENTRATION; MULTICENTER STUDY; NON INSULIN DEPENDENT DIABETES MELLITUS; PHASE 1 CLINICAL TRIAL; POLLAKISURIA; RANDOMIZED CONTROLLED TRIAL; STEADY STATE;

ADULT; AREA UNDER CURVE; BLOOD GLUCOSE; DIABETES MELLITUS, TYPE 2; DOSE-RESPONSE RELATIONSHIP, DRUG; DOUBLE-BLIND METHOD; FEMALE; GLUCOSE; GLUCOSIDES; GLUCURONIDES; HALF-LIFE; HUMANS; HYPOGLYCEMIC AGENTS; MALE; MIDDLE AGED; SODIUM-GLUCOSE TRANSPORTER 2; THIOPHENES;

EID: 84880320337     PISSN: 00912700     EISSN: 15524604     Source Type: Journal    
DOI: 10.1002/jcph.88     Document Type: Article

References (28)

1. Bakris GL, Fonseca VA, Sharma K, Wright EM. Renal sodiumglucose transport: role in diabetes mellitus and potential clinical implications. Kidney Int. 2009;75(12):1272-1277.
2. Vaidya HB, Goyal RK. Exploring newer target sodium glucose transporter 2 for the treatment of diabetes mellitus. Mini Rev Med Chem. 2010;10(10):905-913.
3. Mogensen CE. Maximum tubular reabsorption capacity for glucose and renal hemodynamics during rapid hypertonic glucose infusion in normal and diabetic subjects. Scand J Clin Lab Invest. 1971;28 (1):101-109.
4. Farber SJ, Berger EY, Earle DP. Effect of diabetes and insulin of the maximum capacity of the renal tubules to reabsorb glucose. J Clin Invest. 1951;30(2):125-129.
5. Nomura S, Sakamaki S, Hongu M, et al. 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. J Med Chem. 2010;53(17):6355-6360.
6. Sha S, Devineni D, Ghosh A, et al. Canagliflozin, a novel inhibitor of sodium glucose co transporter 2, dose dependently reduces calculated renal threshold for glucose excretion and increases urinary glucose excretion in healthy subjects. Diabetes Obes Metab. 2011;13(7):669-672.
7. Lee YJ, Lee YJ, Han HJ. Regulatory mechanisms of Na(+)/glucose cotransporters in renal proximal tubule cells. Kidney Int Suppl. 2007;106:S27-S35.
8. Nair S, Wilding JP. Sodium glucose cotransporter 2 inhibitors as a new treatment for diabetes mellitus. J Clin Endocrinol Metab. 2010;95(1):34-42.
9. Liang Y, Arakawa K, Ueta K, et al. Effect of canagliflozin on renal threshold for glucose, glycemia, body weight in normal, diabetic animal models. PLoS ONE. 2012;7(2):e30555.
10. Levey AS, Bosch JP, Lewis JB, Greene T, Rogers N, Roth D.Amore accurate method to estimate glomerular filtration rate from serum creatinine: a new prediction equation. Modification of Diet in Renal Disease Study Group. Ann Intern Med. 1999;130(6):461-470.
11. U.S. Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research. Guidance for Industry, Bioanalytical Method Validation, May 2001. Available at: http://www.fda.gov/ downloads/Drugs/./Guidances/ucm070107. pdf (Accessed January 28, 2013).
12. Shah VP, Midha KK, Findlay JW, et al. Bioanalytical method validation - a revisit with a decade of progress. Pharm Res. 2000;17 (12):1551-1557.
13. Viswanathan CT, Bansai S, Booth B, et al. Workshop/Conference Report - quantitative bioanalytical methods validation, implementation: best practices for chromatographic, ligand binding assays. AAPS J. 2007;9(1):E30.
14. Schwartz S, Morrow L, Hompesch M, et al. Canagliflozin improves glycemic control in subjects with type 2 diabetes (T2D) not optimally controlled on stable doses of insulin. Presented at: The 70th Scientific Sessions of the American Diabetes Association (ADA); June 25-29, 2010; Orlando, FL. Abstract 564 P.
15. Sha S, Devineni D, Ghosh A, et al. Canagliflozin, a novel inhibitor of sodium glucose co transporter 2, improved glucose control in subjects with type 2 diabetes and was well tolerated. Presented at: the 70th Scientific Sessions of the American Diabetes Association (ADA); June 25-29, 2010; Orlando, FL. Abstract 568 P.
16. Devineni D, Morrow L, Hompesch M, et al. Canagliflozin improves glycemic control over 28 days in subjects with type 2 diabetes not optimally controlled on insulin. Diabetes Obes Metab. 2012;14 (6):539-545.
17. Polidori D, Sha S, Ghosh A, Plum Mörschel L, Heise T, Rothenberg P. Validation of a novel method for determining the renal threshold for glucose excretion in untreated and canagliflozin treated subjects with type 2 diabetes mellitus. J Clin Endocrinol. 2013; Apr 12. doi: 10.1210/jc.2012 4205.
18. 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(6):1232-1238.
19. Ganong WF. Formation and excretion of urine. Renal function and micturition. In: Foltin J, Lebowitz H, Brown RY, eds. Review of Medical Physiology, 22nd edition. New York, NY: Lange Medical Books/McGraw Hill; 2005; pp. 699-728.
20. Rave K, Nosek L, Posner J, Heise T, Roggen K, van Hoogdalem EJ. Renal glucose excretion as a function of blood glucose concentration in subjects with type 2 diabetes - results of a hyperglycaemic glucose clamp study. Nephrol Dial Transplant. 2006;21(8):2166- 2171.
21. Freitas HS, Anhe GF, Melo KF, et al. Na(+) glucose transporter 2 messenger ribonucleic acid expression in kidney of diabetic rats correlates with glycemic levels: involvement of hepatocyte nuclear factor 1alpha expression and activity. Endocrinology. 2008;149 (2):717-724.
22. Rahmoune H, Thompson PW, Ward JM, Smith CD, Hong G, Brown J. Glucose transporters in human renal proximal tubular cells isolated from the urine of patients with non insulin dependent diabetes. Diabetes. 2005;54(12):3427-3434.
23. Vestri S, Okamoto MM, de Freitas HS, et al. Changes in sodium or glucose filtration rate modulate expression of glucose transporters in renal proximal tubular cells of rat. J Membr Biol. 2001;182(2):105- 112.
24. Defronzo RA. Banting lecture. From the triumvirate to the ominous octet: a new paradigm for the treatment of type 2 diabetes mellitus. Diabetes. 2009;58(4):773-795.
25. Stenlof K, Cefalu WT, Kim K A, et al. Efficacy and safety of canagliflozin monotherapy in subjects with type 2 diabetes mellitus inadequately controlled with diet and exercise. Diabetes Obes Metab. 2013;15(4):372-382.
26. 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 (6):405-415.
27. Wright EM, Loo DD, Hirayama BA. Biology of human sodium glucose transporters. Physiol Rev. 2011;91(2):733-794.
28. Grempler R, Thomas L, Eckhardt M, et al. Empagliflozin, a novel selective sodium glucose cotransporter 2 (SGLT 2) inhibitor: characterisation and comparison with other SGLT 2 inhibitors. Diabetes Obes Metab. 2012;14(1):83-90.