Multiple-dose pharmacokinetics and pharmacodynamics of evogliptin (DA-1229), a novel dipeptidyl peptidase IV inhibitor, in healthy volunteers

Drug Design, Development and Therapy

Volumn 8, Issue , 2014, Pages 1709-1721

  Gu, Namyi ^a,c   Park, Min Kyu ^a,d   Kim, Tae Eun ^a,e   Bahng, Mi Young ^b   Lim, Kyoung Soo ^a   Cho, Sang Heon ^a   Yoon, Seo Hyun ^a   Cho, Joo Youn ^a   Jang, In Jin ^a   Yu, Kyung Sang ^a  

^a Seoul National University College of Medicine   (South Korea)

^b Dong A ST Co Ltd   (South Korea)

^c Dongguk University College of Medicine   (South Korea)

^d Dong A University College of Medicine   (South Korea)

^e Konkuk University Hospital   (South Korea)

Author keywords

DPP IV; GLP 1; Glucagon like peptide 1; Glucose; Insulin

Indexed keywords

DIPEPTIDYL PEPTIDASE IV; EVOGLIPTIN; GLUCAGON LIKE PEPTIDE 1; GLUCOSE; INSULIN; PLACEBO; 4-(3-AMINO-4-(2,4,5-TRIFLUOROPHENYL)BUTANOYL)-3-(TERT-BUTOXYMETHYL)PIPERAZIN-2-ONE; DIPEPTIDYL PEPTIDASE IV INHIBITOR; PIPERAZINE DERIVATIVE;

ADULT; AREA UNDER THE CURVE; ARTICLE; CLINICAL EVALUATION; CONTROLLED STUDY; DOSE RESPONSE; DOUBLE BLIND PROCEDURE; DRUG ACCUMULATION; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DOSE ESCALATION; DRUG EFFICACY; DRUG ELIMINATION; DRUG EXPOSURE; DRUG HALF LIFE; DRUG SAFETY; DRUG STRUCTURE; DRUG TOLERABILITY; DRUG URINE LEVEL; ENZYME INHIBITION; EPIGASTRIC DISCOMFORT; FATIGUE; GLUCOSE BLOOD LEVEL; HEADACHE; HUMAN; HUMAN EXPERIMENT; INSOMNIA; INSULIN BLOOD LEVEL; MALE; MULTIPLE DRUG DOSE; NORMAL HUMAN; ORAL MUCOSA EROSION; ORAL MUCOSAL DISEASE; POLYURIA; POSTPRANDIAL STATE; RANDOMIZED CONTROLLED TRIAL; TIME TO MAXIMUM PLASMA CONCENTRATION; BLOOD; CHEMISTRY; METABOLISM; ORAL DRUG ADMINISTRATION; YOUNG ADULT;

ADMINISTRATION, ORAL; ADULT; DIPEPTIDYL PEPTIDASE 4; DIPEPTIDYL-PEPTIDASE IV INHIBITORS; DOSE-RESPONSE RELATIONSHIP, DRUG; DOUBLE-BLIND METHOD; HEALTHY VOLUNTEERS; HUMANS; MALE; PIPERAZINES; YOUNG ADULT;

EID: 84908077770     PISSN: 11778881     EISSN: 11778881     Source Type: Journal    
DOI: 10.2147/DDDT.S65678     Document Type: Article

References (29)

1. International Diabetes Federation. IDF Diabetes Atlas. 6th ed. Brussels: International Diabetes Federation; 2013.
2. American Diabetes Association. Standards of medical care in diabetes - 2013. Diabetes Care. 2013;36 Suppl 1:S11-S66.
3. Saaddine JB, Engelgau MM, Beckles GL, Gregg EW, Thompson TJ, Narayan KM. A diabetes report card for the United States: quality of care in the 1990s. Ann Intern Med. 2002;136(8):565-574.
4. Drucker DJ. Therapeutic potential of dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes. Expert Opin Investig Drugs. 2003;12(1):87-100.
5. Holst JJ, Vilsbøll T, Deacon CF. The incretin system and its role in type 2 diabetes mellitus. Mol Cell Endocrinol. 2009;297(1-2):127-136.
6. Pontikis C, Yavropoulou MP, Toulis KA, et al. The incretin effect and secretion in obese and lean women with polycystic ovary syndrome: a pilot study. J Womens Health (Larchmt). 2011;20(6):971-976.
7. Pospisilik JA, Martin J, Doty T, et al. Dipeptidyl peptidase IV inhibitor treatment stimulates beta-cell survival and islet neogenesis in streptozotocin-induced diabetic rats. Diabetes. 2003;52(3):741-750.
8. Kim HJ, Kwak WY, Min JP, et al. Discovery of DA-1229: a potent, long acting dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes. Bioorg Med Chem Lett. 2011;21(12):3809-3812.
9. Cho JM, Jang HW, Cheon H, et al. A novel dipeptidyl peptidase IV inhibitor DA-1229 ameliorates streptozotocin-induced diabetes by increasing β-cell replication and neogenesis. Diabetes Res Clin Pract. 2011;91(1):72-79.
10. Kim MK, Chae YN, Kim HD, et al. DA-1229, a novel and potent DPP4 inhibitor, improves insulin resistance and delays the onset of diabetes. Life Sci. 2012;90(1-2):21-29.
11. Kim TE, Lim KS, Park MK, et al. Evaluation of the pharmacokinetics, food effect, pharmacodynamics, and tolerability of DA-1229, a dipeptidyl peptidase IV inhibitor, in healthy volunteers: first-in-human study. Clin Ther. 2012;34(9):1986-1998.
12. Drucker DJ, Sherman SI, Gorelick FS, Bergenstal RM, Sherwin RS, Buse JB. Incretin-based therapies for the treatment of type 2 diabetes: evaluation of the risks and benefits. Diabetes Care. 2010;33(2): 428-433.
13. Kazafeos K. Incretin effect: GLP-1, GIP, DPP4. Diabetes Res Clin Pract. 2011;93 Suppl 1:S32-S36.
14. Scheen AJ. Dipeptidyl peptidase-4 (DPP-4) inhibitors are favourable to glucagon-like peptide-1 (GLP-1) receptor agonists: yes. Eur J Intern Med. 2012;23(2):126-131.
15. Davidson JA. Incorporating incretin-based therapies into clinical practice: differences between glucagon-like peptide 1 receptor agonists and dipeptidyl peptidase 4 inhibitors. Mayo Clin Proc. 2010;85(Suppl 12):S27-S37.
16. Gerich J. DPP-4 inhibitors: what may be the clinical differentiators? Diabetes Res Clin Pract. 2010;90(2):131-140.
17. Scheen AJ. Pharmacokinetics of dipeptidyl peptidase-4 inhibitors. Diabetes Obes Metab. 2010;12(8):648-658.
18. Scheen AJ. A review of gliptins in 2011. Expert Opin Pharmacother. 2012;13(1):81-99.
19. Baetta R, Corsini A. Pharmacology of dipeptidyl peptidase-4 inhibitors: similarities and differences. Drugs. 2011;71(11):1441-1467.
20. He YL. Clinical pharmacokinetics and pharmacodynamics of vildagliptin. Clin Pharmacokinet. 2012;51(3):147-162.
21. Li H, Yang L, Tou CK, Patel CG, Zhao J. Pharmacokinetic study of saxagliptin in healthy Chinese subjects. Clin Drug Investig. 2012;32(7):465-473.
22. Gutniak M. [GLP-1 (7-36) amide [GLIP-glucagon like insulinotropic peptide] as a potential treatment for NIDDM]. Journ Annu Diabetol Hotel Dieu. 1998:157-171. French.
23. Flint A, Raben A, Ersbøll AK, Holst JJ, Astrup A. The effect of physiological levels of glucagon-like peptide-1 on appetite, gastric emptying, energy and substrate metabolism in obesity. Int J Obes Relat Metab Disord. 2001;25(6):781-792.
24. Knauf C, Cani PD, Perrin C, et al. Brain glucagon-like peptide-1 increases insulin secretion and muscle insulin resistance to favor hepatic glycogen storage. J Clin Invest. 2005;115(12):3554-3563.
25. Lindgren O, Mari A, Deacon CF, et al. Differential islet and incretin hormone responses in morning versus afternoon after standardized meal in healthy men. J Clin Endocrinol Metab. 2009;94(8):2887-2892.
26. Melani F, Verrillo A, Marasco M, Rivellese A, Osorio J, Bertolini MG. Diurnal variation in blood sugar and serum insulin in response to glucose and/or glucagon in healthy subjects. Horm Metab Res. 1976;8(2):85-88.
27. Lee A, Ader M, Bray GA, Bergman RN. Diurnal variation in glucose tolerance. Cyclic suppression of insulin action and insulin secretion in normal-weight, but not obese, subjects. Diabetes. 1992;41(6): 750-759.
28. Van Cauter E, Shapiro ET, Tillil H, Polonsky KS. Circadian modulation of glucose and insulin responses to meals: relationship to cortisol rhythm. Am J Physiol. 1992;262(4 Pt 1):E467-E475.
29. Saad A, Dalla Man C, Nandy DK, et al. Diurnal pattern to insulin secretion and insulin action in healthy individuals. Diabetes. 2012;61(11):2691-2700.