A novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor, teneligliptin, improves postprandial hyperglycemia and dyslipidemia after single and repeated administrations

Fukuda-Tsuru, Sayaka; Anabuki, Jun; Abe, Yuji; Yoshida, Kumiko; Ishii, Shin‐ichi

doi:10.1016/j.ejphar.2012.09.024

Cited by 44 publications

(25 citation statements)

References 51 publications

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“…Inhibitory activities of test compounds against rat DPP4 were measured using serum collected from 7-weekold male Sprague-Dawley (SD) rats (Charles River Japan, Yokohama, Japan). Rat serum and Gly-Pro 4-methylcoumaryl-7-amide were mixed with the assay buffer (phosphate-buffered saline containing 0.003% Brij-35 solution) to initiate the enzyme reaction, as described previously (Fukuda-Tsuru et al, 2012). The fluorescence intensity of Gly-Pro 4-methylcoumaryl-7-amide was measured using a microplate reader (Molecular Devices, Sunnyvale, CA) after 1-hour incubation at 37°C.…”

Section: Cell-based Assaysmentioning

confidence: 99%

“…GLP-1 is secreted from enteroendocrine L cells in the distal part of the small intestine in response to dietary stimulation (Orskov et al, 1993) and exerts antidiabetic effects, such as enhancing glucose-dependent insulin secretion and inhibiting gastric emptying, food intake, and glucagon secretion (Drucker, 2003). Dipeptidyl peptidase-4 (DPP4) inhibitors, a novel class of OADs, delay enzymatic degradation and inactivation of GLP-1, thereby increasing insulin release and decreasing glucagon secretion in a glucose-dependent manner (Drucker, 2003;Fukuda-Tsuru et al, 2012).…”

Section: Introductionmentioning

confidence: 99%

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Intestinal Sodium Glucose Cotransporter 1 Inhibition Enhances Glucagon-Like Peptide-1 Secretion in Normal and Diabetic Rodents

Oguma¹,

Nakayama²,

Kuriyama³

et al. 2015

J Pharmacol Exp Ther

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The sodium glucose cotransporter (SGLT) 1 plays a major role in glucose absorption and incretin hormone release in the gastrointestinal tract; however, the impact of SGLT1 inhibition on plasma glucagon-like peptide-1 (GLP-1) levels in vivo is controversial. We analyzed the effects of SGLT1 inhibitors on GLP-1 secretion in normoglycemic and hyperglycemic rodents using phloridzin, CGMI [3-(4-cyclopropylphenylmethyl)-1-(b-Dglucopyranosyl)-4-methylindole], and canagliflozin. These compounds are SGLT2 inhibitors with moderate SGLT1 inhibitory activity, and their IC 50 values against rat SGLT1 and mouse SGLT1 were 609 and 760 nM for phloridzin, 39.4 and 41.5 nM for CGMI, and 555 and 613 nM for canagliflozin, respectively. Oral administration of these inhibitors markedly enhanced and prolonged the glucose-induced plasma active GLP-1 (aGLP-1) increase in combination treatment with sitagliptin, a dipeptidyl peptidase-4 (DPP4) inhibitor, in normoglycemic mice and rats. CGMI, the most potent SGLT1 inhibitor among them, enhanced glucose-induced, but not fat-induced, plasma aGLP-1 increase at a lower dose compared with canagliflozin. Both CGMI and canagliflozin delayed intestinal glucose absorption after oral administration in normoglycemic rats. The combined treatment of canagliflozin and a DPP4 inhibitor increased plasma aGLP-1 levels and improved glucose tolerance compared with single treatment in both 8-and 13-week-old Zucker diabetic fatty rats. These results suggest that transient inhibition of intestinal SGLT1 promotes GLP-1 secretion by delaying glucose absorption and that concomitant inhibition of intestinal SGLT1 and DPP4 is a novel therapeutic option for glycemic control in type 2 diabetes mellitus.

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Section: Cell-based Assaysmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Intestinal Sodium Glucose Cotransporter 1 Inhibition Enhances Glucagon-Like Peptide-1 Secretion in Normal and Diabetic Rodents

Oguma¹,

Nakayama²,

Kuriyama³

et al. 2015

J Pharmacol Exp Ther

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“…The absence of accumulation has also been shown in simulation experiments, although these studies were based on single-dose administration (15,29). Moreover, in addition to its hypoglycemic effects, the multifaceted extrapancreatic actions, including the improvement of lipid profiles or hypotensive actions mediated by the inhibition of reabsorption of sodium in the kidneys, of alogliptin have been reported, although in a small number of patients (24,30,31). While it is unknown if these actions result in renal protection, no significant changes were observed in the lipid profiles or blood pressure, and neither blood pressure nor the lipid levels were correlated with the rate of change in eGFR in this study.…”

Section: Discussionmentioning

confidence: 99%

Effects of Alogliptin in Chronic Kidney Disease Patients with Type 2 Diabetes

et al. 2014

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Objective Diabetes is a major risk factor for chronic kidney disease (CKD). In this study, we examined the effects of alogliptin on blood glucose control and the renal function in type 2 diabetes CKD patients. Methods We recruited 36 CKD patients with type 2 diabetes. The patients were followed up for six months after adding alogliptin. Blood biochemical, urine test and office BP values were obtained six months before and after the start of treatment. Results The mean HbA1c value was not decreased; however, the 1,5-AG values tended to improve (p= 0.1023). The mean eGFR was unchanged. There were no significant changes in the patients with an eGFR of 60 mL/min/1.73 m 2 or more (25 patients) or in the patients with an eGFR less than 60 mL/min/1.73 m 2 (11 patients). A total of 15 patients were identified to have rapidly declining diabetic nephropathy, with an annual reduction in eGFR of 5 mL/min/1.73 m 2 or more. The slope of the regression line for eGFR (-1.296 before starting treatment with alogliptin) was positive, increasing up to 0.08786. The eGFR values appeared to stop decreasing and positively reversed. The urinary albumin-to-creatinine ratio exhibited a downward trend. The effect on the renal function was independent of the levels of blood sugar, blood pressure and lipids. Conclusion We examined the ability of alogliptin to maintain the renal function in patients with CKD complicated by type 2 diabetes. Our study suggests that alogliptin can be safely administered in patients with CKD. However, although we expected alogliptin to demonstrate renal protective effects, were unable to detect statistically significant differences. One reason for this finding is that there are few registered cases.

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“…Therefore, incretin-related agents such as DPP- Teneligliptin which inhibits the enzyme DPP-4 and degrades incretin, a hormone which adjusts blood glucose level and improves blood glucose control as stated above. A survey of chemical literature has shown that the drug Teneligliptin is effectively used to treat Type 2 diabetes mellitus [1][2][3][4][5][6][7][8] (T2DM). Further it is noticed that only a very few methods on the development and validation for the estimation of Teneligliptin are reported which include UV spectrophotometric methods [9][10] and High Performance Thin Layer Chromatographic (HPTLC) method [11] and High Performance Liquid Chromatography (HPLC) methods.…”

Section: World Journal Of Pharmacy and Pharmaceutical Sciencesmentioning

confidence: 99%

Spectrophotometric Assay of Teneligliptin in Pharmaceutical Tablet Dosage Form by Ion-Pair Complex Method Using Bromo Phenol Blue (Bpb)

Prasanna¹

2017

WJPPS

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A novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor, teneligliptin, improves postprandial hyperglycemia and dyslipidemia after single and repeated administrations

Cited by 44 publications

References 51 publications

Intestinal Sodium Glucose Cotransporter 1 Inhibition Enhances Glucagon-Like Peptide-1 Secretion in Normal and Diabetic Rodents

Intestinal Sodium Glucose Cotransporter 1 Inhibition Enhances Glucagon-Like Peptide-1 Secretion in Normal and Diabetic Rodents

Effects of Alogliptin in Chronic Kidney Disease Patients with Type 2 Diabetes

Spectrophotometric Assay of Teneligliptin in Pharmaceutical Tablet Dosage Form by Ion-Pair Complex Method Using Bromo Phenol Blue (Bpb)

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