Effect of canagliflozin, a sodium glucose co-transporter 2 inhibitor, on C-peptide kinetics

Clinical Pharmacology in Drug Development

Volumn 4, Issue 1, 2015, Pages 12-17

  Polidori, David ^a   Sha, Sue ^b   Heise, Tim ^c   Natarajan, Jaya ^b   Artis, Eunice ^b   Wang, Shean Sheng ^b   Vaccaro, Nicole ^b   Rothenberg, Paul ^b   Stirban, Alin ^c  

^a JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

^b JANSSEN RESEARCH AND DEVELOPMENT   (United States)

^c Profil   (Germany)

Author keywords

C peptide; Canagliflozin; Kinetics; Sodium glucose co transporter 2 (SGLT2) inhibitor; cell function

Indexed keywords

C PEPTIDE; CANAGLIFLOZIN; GLUCOSE; INSULIN; PLACEBO; SODIUM GLUCOSE COTRANSPORTER 2 INHIBITOR; SOMATOSTATIN; ANTIDIABETIC AGENT; BIOLOGICAL MARKER; SLC5A2 PROTEIN, HUMAN; SODIUM GLUCOSE COTRANSPORTER 2;

ADULT; ARTICLE; BOLUS INJECTION; C PEPTIDE BLOOD LEVEL; CELL FUNCTION; CHEMICAL PARAMETERS; CONTROLLED STUDY; CROSSOVER PROCEDURE; DOUBLE BLIND PROCEDURE; DRUG EFFECT; ELECTROCARDIOGRAPHY; FEMALE; GLUCOSE URINE LEVEL; HUMAN; HUMAN EXPERIMENT; INSULIN RELEASE; KIDNEY CLEARANCE; KINETICS; LABORATORY TEST; MALE; MEASUREMENT; MORNING DOSAGE; NAUSEA; NORMAL HUMAN; PANCREAS ISLET BETA CELL; PROTEIN BLOOD LEVEL; PROTEIN DETERMINATION; PROTEIN SECRETION; RANDOMIZED CONTROLLED TRIAL; SINGLE DRUG DOSE; VITAL SIGN; ADOLESCENT; ANTAGONISTS AND INHIBITORS; BIOLOGICAL MODEL; BLOOD; DRUG EFFECTS; GERMANY; KIDNEY TUBULE; METABOLISM; MIDDLE AGED; SECRETION (PROCESS); URINE; YOUNG ADULT;

ADOLESCENT; ADULT; BIOMARKERS; C-PEPTIDE; CANAGLIFLOZIN; CROSS-OVER STUDIES; DOUBLE-BLIND METHOD; FEMALE; GERMANY; HEALTHY VOLUNTEERS; HUMANS; HYPOGLYCEMIC AGENTS; INSULIN-SECRETING CELLS; KIDNEY TUBULES; KINETICS; MALE; MIDDLE AGED; MODELS, BIOLOGICAL; SODIUM-GLUCOSE TRANSPORTER 2; YOUNG ADULT;

EID: 84921029942     PISSN: 2160763X     EISSN: 21607648     Source Type: Journal    
DOI: 10.1002/cpdd.115     Document Type: Article

References (34)

1. Kahn SE. Clinical review 135: the importance of beta-cell failure in the development and progression of type 2 diabetes. J Clin Endocrinol Metab. 2001; 86:4047-4058.
2. Matthews DR, Hosker JP, Rudenski AS, Naylor BA, Treacher DF, Turner RC. Homeostasis model assessment: insulin resistance and beta-cell function from fasting plasma glucose and insulin concentrations in man. Diabetologia. 1985; 28:412-419.
3. Roder ME, Porte D Jr., Schwartz RS, Kahn SE. Disproportionately elevated proinsulin levels reflect the degree of impaired B cell secretory capacity in patients with noninsulin-dependent diabetes mellitus. J Clin Endocrinol Metab. 1998; 83:604-608.
4. Loopstra-Masters RC, Haffner SM, Lorenzo C, Wagenknecht LE, Hanley AJ. Proinsulin-to-C-peptide ratio versus proinsulin-to-insulin ratio in the prediction of incident diabetes: the Insulin Resistance Atherosclerosis Study (IRAS). Diabetologia. 2011; 54:3047-3054.
5. Defronzo RA, Tobin JD, Andres R. Glucose clamp technique: a method for quantifying insulin secretion and resistance. Am J Physiol. 1979; 237:E214-E223.
6. Kahn SE, Prigeon RL, McCulloch DK, et al. Quantification of the relationship between insulin sensitivity and beta-cell function in human subjects. Evidence for a hyperbolic function. Diabetes. 1993; 42:1663-1672.
7. Robertson RP, Sutherland DE, Kendall DM, Teuscher AU, Gruessner RW, Gruessner A. Metabolic characterization of long-term successful pancreas transplants in type I diabetes. J Investig Med. 1996; 44:549-555.
8. Byrne MM, Sturis J, Polonsky KS. Insulin secretion and clearance during low-dose graded glucose infusion. Am J Physiol. 1995; 268:E21-E27.
9. Mari A, Tura A, Gastaldelli A, Ferrannini E. Assessing insulin secretion by modeling in multiple-meal tests: role of potentiation. Diabetes. 2002; 51:S221-S226.
10. Cobelli C, Toffolo GM, Dalla MC, et al. Assessment of beta-cell function in humans, simultaneously with insulin sensitivity and hepatic extraction, from intravenous and oral glucose tests. Am J Physiol Endocrinol Metab. 2007; 293:E1-E15.
11. Kjems LL, Holst JJ, Volund A, Madsbad S. The influence of GLP-1 on glucose-stimulated insulin secretion: effects on beta-cell sensitivity in type 2 and nondiabetic subjects. Diabetes. 2003; 52:380-386.
12. Mari A, Degn K, Brock B, Rungby J, Ferrannini E, Schmitz O. Effects of the long-acting human glucagon-like peptide-1 analog liraglutide on beta-cell function in normal living conditions. Diabetes Care. 2007; 30:2032-2033.
13. Xu L, Man CD, Charbonnel B, et al. Effect of sitagliptin, a dipeptidyl peptidase-4 inhibitor, on beta-cell function in patients with type 2 diabetes: a model-based approach. Diabetes Obes Metab. 2008; 10:1212-1220.
14. 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; 35:1232-1238.
15. Radziuk J, Morishima T. New methods for the analysis of insulin kinetics in vivo: insulin secretion, degradation, systemic dynamics and hepatic extraction. Adv Exp Med Biol. 1985; 189:247-276.
16. Viljanen AP, Iozzo P, Borra R, et al. Effect of weight loss on liver free fatty acid uptake and hepatic insulin resistance. J Clin Endocrinol Metab. 2009; 94:50-55.
17. Henry RR, Brechtel G, Griver K. Secretion and hepatic extraction of insulin after weight loss in obese noninsulin-dependent diabetes mellitus. J Clin Endocrinol Metab. 1988; 66:979-986.
18. Osei K, Gaillard T, Schuster D. Thiazolidinediones increase hepatic insulin extraction in African Americans with impaired glucose tolerance and type 2 diabetes mellitus. A pilot study of rosiglitazone. Metabolism. 2007; 56:24-29.
19. Van Cauter E, Mestrez F, Sturis J, Polonsky KS. Estimation of insulin secretion rates from C-peptide levels. Comparison of individual and standard kinetic parameters for C-peptide clearance. Diabetes. 1992; 41:368-377.
20. Bode B, Stenlof K, Sullivan D, Fung A, Usiskin K. Efficacy and safety of canagliflozin in older subjects with type 2 diabetes: a randomized trial. Hosp Pract. 2013; 41:72-84.
21. Cefalu WT, Leiter LA, Yoon K-H, et al. Canagliflozin promotes body weight loss compared with glimepiride while providing glycaemic efficacy in subjects with type 2 diabetes on background metformin: 52-week findings from a randomised, double-blind trial. Lancet. 2013; 382:941-950.
22. Schernthaner G, Gross JL, Rosenstock J, et al. Canagliflozin compared with sitagliptin for patients with type 2 diabetes who do not have adequate glycemic control with metformin plus sulfonylurea: a 52-week, randomized trial. Diabetes Care. 2013; 36:2508-2515.
23. Stenlöf 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; 15:372-382.
24. Yale JF, Bakris G, Cariou B, et al. Efficacy and safety of canagliflozin in subjects with type 2 diabetes and chronic kidney disease. Diabetes Obes Metab. 2013; 15:463-473.
25. Faber OK, Kehlet H, Madsbad S, Binder C. Kinetics of human C-peptide in man. Diabetes. 1978; 27:207-209.
26. Somatostatin [Package Insert]. Oberhaching, Germany: Lyomark Pharma GmbH; 2009.
27. Devineni D, Curtin CR, Polidori D, et al. Pharmacokinetics and pharmacodynamics of canagliflozin, a sodium glucose co-transporter 2 inhibitor, in subjects with type 2 diabetes mellitus. J Clin Pharmacol. 2013; 53:601-610.
28. Levey AS, Coresh J, Greene T, et al. Using standardized serum creatinine values in the modification of diet in renal disease study equation for estimating glomerular filtration rate. Ann Intern Med. 2006; 145:247-254.
29. 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; 12:1004-1012.
30. Rossetti L, Shulman GI, Zawalich W, Defronzo RA. Effect of chronic hyperglycemia on in vivo insulin secretion in partially pancreatectomized rats. J Clin Invest. 1987; 80:1037-1044.
31. 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; 13:669-672.
32. Nawano M, Oku A, Ueta K, et al. Hyperglycemia contributes insulin resistance in hepatic and adipose tissue but not skeletal muscle of ZDF rats. Am J Physiol Endocrinol Metab. 2000; 278:E535-E543.
33. Tahara A, Kurosaki E, Yokono M, et al. Effects of SGLT2 selective inhibitor ipragliflozin on hyperglycemia, hyperlipidemia, hepatic steatosis, oxidative stress, inflammation, and obesity in type 2 diabetic mice. Eur J Pharmacol. 2013; 715:246-255.
34. Lorenzo C, Hanley AJ, Wagenknecht LE, et al. Relationship of insulin sensitivity, insulin secretion, and adiposity with insulin clearance in a multiethnic population: the insulin Resistance Atherosclerosis study. Diabetes Care. 2013; 36:101-103.