Association between sitagliptin plus vitamin D3 (VIDPP-4i) use and clinical remission in patients with new-onset type 1 diabetes: a retrospective case-control study

ABSTRACT Objective: The occurrence of partial remission (honeymoon phase) in type 1 diabetes (T1D) has been associated with a reduced risk of chronic microvascular complications of diabetes. We have published case reports showing that a combination therapy with the DPP-4 inhibitor sitagliptin plus vitamin D3 (VIDPP-4i) can prolong the honeymoon phase in patients with new-onset T1D. In the present case-control study, we investigated the frequency of occurrence of clinical remission (CR) in patients with new-onset T1D after VIDPP-4i treatment. Subjects and methods: In this case-control study, we collected data spanning 10 years from medical records of 46 patients (23 females) recently diagnosed with T1D. Overall, 27 participants with CR (insulin dose-adjusted glycated hemoglobin [IDAA1c] ≤ 9) at 12 or 24 months composed the case group, and 19 participants without CR served as the control group. Chi-square with Yates correction was used to analyze the association between VIDPP-4i use and CR, and odds ratio (OR) was used to determine the chance of CR due to VIDPP-4i treatment exposure. Results: In all, 37 patients (80.4%) experienced CR at some time over 24 months. The mean CR duration was 13.15 ± 9.91 months. Treatment with VIDPP-4i was significantly associated with CR. At 24 months, the OR of CR after VIDPP-4i exposure was 9.0 (95% confidence interval [CI] 2.21-30.18, p = 0.0036). Additionally, 9 (33.6%) and 4 (14.8%) patients in the VIDPP-4i group experienced insulin-free CR at 12 and 24 months, respectively. Conclusion: Therapy with VIDPP-4i was associated with a higher frequency and duration of the honeymoon phase. Randomized controlled trials are needed to confirm these findings.

Effect of Sitagliptin on Diabetic Profile of Type 2 Diabetes Mellitus Patients

Introduction: Time since death is an important topic that playsmajor role in forensic medicine. The accurate determinationof time since death is found to be helpful in medico legalinvestigation. Advancements in the methods for estimatingtime since death have enabled us to determine post-morteminterval more precisely. Since the 1850s, scientists have beenworking on different methods to determine post-morteminterval. Hence, the aim of the present study was to assess thetime since death using method of rigor mortis in the autopsiesdone at the mortuary of Osmania General Hospital.Materials and Methods: About 500 medico-legal autopsieswere selected where the exact time of death was known andthe body had been kept at prevailing room temperature. Agood quality digital hygrometer was used to note the dailyreadings of temperature and humidity. Presence or absence ofrigor mortis and its extent was noticed in both voluntary andinvoluntary muscles.Results: More unnatural deaths are in suspiciouscircumstances are occurring in males when compared tofemales. The average duration for onset of rigor mortis was 8hours and 39 minutes. The minimum duration in which rigormortis had begun to appear in the body was 1 hour and 35minutes while the longest maximum by which rigor mortishad not completely appeared in the body was 24 hours.Conclusion: Rigor mortis has been used for assessment oftime since death from long time. It is considered to be themost important and interesting method to estimate the timesince death.

Effect of teneligliptin vs metformin on glycemic control in Indian patients with newly-diagnosed, drug-naïve type 2 diabetes mellitus: a 12-week randomized comparative clinical study

Background: This comparative study was done to evaluate the change from baseline in HbA1c levels with teneligliptin vs. metformin treatments at week 12 among recently diagnosed type 2 DM patients attending Medicine OPD of Dr. B. C. Roy Hospital, Haldia, West Bengal (a tertiary care teaching hospital).Methods: In this prospective parallel group clinical study patients were divided into two groups. Group A patients were on metformin monotherapy therapy and Group B patients were on teneligliptin monotherapy. Data of 40 patients (20 patients in each group) were available for analysis in the present study. Secondary endpoints included changes from baseline FPG and 2h-PPG values at 12 weeks were evaluated. Safety and tolerability were assessed by the incidence of adverse events (AEs) throughout the study period.Results: The mean age of patients was 50.05±12.35 years and out of the entire patient population 70% were males and 30% were females. At the end of 12 weeks or 3 months of metformin therapy, mean HbA1c, FBG, and PPG were significantly reduced by 0.52%, 16.2mg/dL, and 36.8mg/dL, respectively, and 37.75% of patients achieved the HbA1c target of <7%. At the end of 12 weeks or 3 months of teneligliptin therapy, mean HbA1c, FBG, and PPG were significantly reduced by 0.60%, 19.4mg/dL, and 49.8mg/dL, respectively (Table 2), and 40% of patients achieved the HbA1c target of <7%.Conclusions: Teneligliptin, a DPP4 inhibitor reduced HbA1C significantly compared with monotherapy of metformin in treatment naive patients at week 12. It also reduced FBG and 2-h PPBG as compared with metformin at week 12.

DPP-4 inhibitory activity and myocardial salvaging effects of Commiphora mukul in experimental diabetes

Background: Commiphora mukul (Burseraceae) is commonly known as Guggul in Ayurveda. Several studies have reported antidiabetic activity of Commiphora mukul but there are no studies to explore the DPP-4 inhibitory activity and myocardial salvaging effects of Commiphora mukul in setting of diabetes mellitus. The present study was designed to evaluate the cardioprotective efficacy as well as safety of the medicinal plant Commiphora mukul (Guggul) in the experimental model of myocardial infarction co-existing with diabetes.Methods: Diabetes was induced with single dose of streptozotocin (STZ): 45mg/kg ip and myocardial infarction was produced by administering isoproterenol (ISP): (85mg/kg, sc) to rats 24 and 48 h prior to scarification (5th week). After the confirmation of diabetes on 7th day (glucose>200mg/dl), vildagliptin (10 mg/kg) and Commiphora mukul (200 mg/kg) were administered orally from 1st to 5th week (4 weeks). At the end of experimental period, normal control, diabetic-isoproterenol control, vildagliptin and Commiphora mukul group rats were sacrificed for further biochemical investigations as well as histopathological evaluation.Results: Commiphora mukul treatment demonstrated significant antidiabetic as well as myocardial salvaging effects as indicated by restoration of blood glucose, HbA1c and CPK-MB serum DPP-4, hs-CRP levels as compared to diabetic ISP control group. In addition, Commiphora mukul showed significant cardioprotection as indicated by positive correlation between cardiac marker CPK-MB and serum DPP-4. The histopathological assessment of heart, pancreas and biochemical indices of injury confirmed the cardioprotective effects of Commiphora mukul. In addition, Commiphora mukul was found to be safe to the liver and kidney.Conclusions: The natural DPP-4 inhibitor Commiphora mukul demonstrated significant cardioprotective effects in experimental model of myocardial infarction co-existing with diabetes.

Signal Detection for Cardiovascular Adverse Events of DPP-4 Inhibitors Using the Korea Adverse Event Reporting System Database, 2008–2016

PURPOSE: Cardiovascular adverse events (AEs) after use of dipeptidyl peptidase-4 (DPP4) inhibitors have been reported and suspected since the launch of DPP-4 inhibitors in 2006. However, few studies have investigated the association between cardiovascular AEs and DPP-4 inhibitors. The objective of this study is to detect the signals of cardiovascular AEs after use of DPP-4 inhibitors by analyzing the Korea Institute of Drug Safety & Risk Management-Korea Adverse Event Reporting System Database (KIDS-KD). MATERIALS AND METHODS: Data on the use of oral antidiabetic drugs from 2008 to 2016 were extracted from KIDS-KD, and analyzed descriptively. Data mining was conducted by calculating three indices, which were proportional reporting ratios, reporting odds ratios, and information components, to detect signals from use of all oral antidiabetic drugs including DPP-4 inhibitors. Then, the suspected adverse drug reactions (ADRs) were confirmed by signal detection, and drug label information between the Korea Ministry of Food and Drug Safety and the U.S. Food and Drug Administration were compared. RESULTS: Cardiovascular AEs after taking DPP-4 inhibitors were detected in only three (1.0%) out of a total of 307 AE reports. Two of the three cardiovascular AEs were reported after using sitagliptin and one using gemiglipitin, but these were not statistically significant. CONCLUSION: Analysis of spontaneous ADR reports data on the use of DPP-4 inhibitors could not showed the association between DPP-4 inhibitors and cardiovascular AEs, due to a small number of cardiovascular AEs reports.

Using RCT Data to Evaluate the Association of DPP-4 Inhibitors on Pancreatitis and/or Pancreatic Cancer Risk in T2DM: A Systematic Review and Meta-analysis / 中国药学杂志

OBJECTIVE: To review systematically the association of dipeptidyl peptidase-4 inhibitors on pancreatitis and/or pancreatic cancer risk in type-2 diabetes mellitus. METHODS: Databases including The Cochrane Library, PubMed, Embase, Clinical Trials. gov, CNKI, WanFang Data and CBM, were searched electronically for randomized controlled trials (RCTs) of DPP-4 inhibitors in pancreatitis and pancreatic cancer risk in T2DM patients up to June 2017. Two reviewers independently screened literatures according to the inclusion and exclusion criteria, extracted data, and assessed the methodological quality of the included studies. Then Metaanalysis was performed using Rev Man 5.3 software. RESULTS: A total of 39 RCTs involving 65 189 patients were included. The results of Meta-analysis showed that there were no significant differences between the DPP-4 inhibitors group and the control group in the pancreatitis and/or pancreatic cancer adverse events (RR = 0.92, 95%CI 0.69 to 1.23, P = 0.59), pancreatitis (RR = 1.05, 95% CI 0.76 to 1.4, P = 0.79) and pancreatic cancer (RR = 0.62, 95%CI (0.35, 1.08), P = 0.09). Subgroup analyses showed there were no significant differences of acute pancreatitis events between DPP-4 inhibitors group and the control group (RR = 1.42, 95%CI 0.82 to 2.47, P = 0.21). CONCLUSION: The present Meta-analysis of RCTs data does not suggest that DPP-4 inhibitors are associated with pancreatitis and/or pancreatic cancer. Long-term clinical studies are required to further prove this conclusion.

Omarigliptin: A new kind of long acting DPP-4 inhibitor / 药物评价研究

Diabetes is a kind of metabolic disease characterized by hyperglycemia The oral hypoglycemic agents used currently are required to take every day,which brings inconvenience to patients.Omarigliptin is a small molecule DPP-4 (depeptidyl peptidase-4) inhibitor.The drug is developed by the Merck Co,mainly for the treatment of type two diabetes.The drug only need to be taken once a week,so as to improve the patient's compliance and adherence,thereby improving the therapeutic effect.This article introduces the information of omarigliptin from the aspects of synthesis,pharmacology,pharmacokinetics,and clinical research,which provides valuable information for pharmaceutical workers.

Effects of Dipeptidyl Peptidase-4 inhibitor on albuminuria in patients with type 2 diabetes mellitus / 中国糖尿病杂志

Dipeptidyl Peptidase-4 inhibitor (DPP-4 inhibitor),a new kind of oral anti-diabetic medicine,has been widely used for the treatment of type 2 diabetes (T2DM) during the last decades.Recent evidence showed that DPP-4 inhibitor may have renal protective effects beyond glycemic control.Some clinical studies revealed that the reduction of HbA1c by DPP-4 inhibitor was paralleled by an improvement of albuminuria and renal function.Experimental studies indicated that the renal protection mechanism of DPP-4 inhibitor may be involved in its multiple effects including anti-inflammatory,anti-oxidation and improvement of endothelial function.However,the evidence of decreasing albuminuria for DPP-4 inhibitor mainly comes from animal models and some clinical trials with small sample size.More large randomized controlled trials (RCT) will be needed to certify the renal protection effect of DPP-4 inhibitor.In this review,the role of DPP-4 inhibitor on albuminuria will be considered and discussed from both experimental and clinical perspectives.

DPP-4 inhibitor Sig Leo Dean on the newly diagnosed type 2 diabetes mellitus and its effect on blood pressure and body weigh / 重庆医学

Objective To investigate the clinical efficacy of DPP-4 inhibitors in the treatment of newly diagnosed type 2 diabetes mellitus and its effect on blood pressure and body weight.Methods A total of 100 newly diagnosed elderly patients with type 2 diabetes mellitus were enrolled in this study from July 2013 to June 2015 in this hospital.They were divided into observation group and control group(n=50).The control group was treated with placebo on the basis of diet control and exercise.The observation group was treated with sitagliptin on the basis of diet control and exercise.Fasting plasma glucose(FPG),2 h postprandial blood glucose(2 h PG) and glycated albumin (GA) were measured before and after treatment,and the incidence rate of hypoglycemia,blood pressure,body weight and other adverse reactions were monitored.Results After treatment,two groups of patients,condition were significantly improved,FPG,2 h PG,GA changes in observation group were significantly better than that of control group,the difference were statistically significant(P＜0.05).There was no significant difference in blood pressure,body weight and body mass index before and after treatment,and also between the two groups(P＞0.05).The incidence of adverse reactions in the observation group and the control group were 10.0％ and 8.0％,The incidence of adverse reactions in the two groups was not statistically significant(P＞0.05).Conclusion The clinical efficacy of DPP-4 inhibitor siglitazide in the treatment of newly diagnosed elderly patients with type 2 diabetes mellitus is good,and it is very useful in the treatment of these patients.

Effect of DPP-4 inhibitor on glucose fluctuation in patients with type 2 diabetes mellitus treated by insulin / 重庆医学

Objective To probe into the effect of sitagliptin on blood glucose fluctuation of the patients with type 2 diabetes mellitus(T2DM) and poor control by insulin aspart 30.Methods Ninety cases of T2DM and poor control by insulin aspart 30 in affiliated Zhongshan hospital from January 1,2014 to December 31,2014 were selected and randomly divided into three groups:simply continuous subcutaneous insulin injection(CSII),acarbose combined CSII group(CSII + Aca) and sitagliptincombined CSII group (CSII + Sig),30 cases in each group.Three groups received the intensive treatment for 2 weeks,and72-h continuous glucose monitoring was performed on last 3 d.The 24 h mean blood glucose(24 hMBG),largest amplitude of glycemic fluctuation(LAGE),mean amplitude of glycemic excursion(MAGE) within 1 d,postprandial blood glucose spike(PGS),postprandial glucose peak time(△t),postprandial glucose excursion(PPGE) and total T were observed within 24 h.The difference of insulin dose(△ insulin),hypoglycemia incidence,glucose-target rate,blood glucose profiles were compared at the end of treatment.Results After two-week treatment,intraday blood glucose variation indicators(24 hMBG,LAGE and MAGE) and postprandial blood glucose variation indicators (PGS,△t,PPGE and total T) in the CSII+Sig and CSII+-Aca groups were significantly lower than those in the CSII group(P＜ 0.05),while the differences in blood glucose variation indicators between the CSII+Sig group and CSII+-Aca group were not statistical significant(P＞ 0.05).In the comparison after treatment,△ insulin,hypoglycemia incidence and glucose-target rate in the CSI + Sig group were lower(P＜0.05).Conclusion The combined application of short-term CSII and sitagliptin will achieve a better effect than the combination with acarbose,can smoothly and steadily reduces the blood glucose level,relieves the whole day glucose fluctuations,effectively reduces △ insulin,and has lower hypoglycemia occurrence rate.

Screening and identification of DPP-4 inhibitors from Xiaokean formula by a fluorescent probe / 中国中药杂志

Fluorescent bio-probes have attracted increasing attentions in studies for screening bioactive compounds from traditional Chinese medicines. In this study, a new-type fluorescent probe with the function of aggregation-induced emission (AIE) was used to screen dipeptidyl peptidase-4 (DPP-4) inhibitor from Xiaokean formula, which has been clinically used for the treatment of type 2 diabetes mellitus. Potential DPP-4 inhibitors were screened by the fluorescent probe, with diprotin A as the positive control; totally 43 components were isolated from Xiaokean formula by systematic separation. The results showed that 13 components can exert inhibitory effects on DPP-4 activity; 16 compounds were further identified by liquid chromatography-mass spectrometry (LC-MS) from those active components. The inhibitory effects of 14 compounds were further verified, while five of them showed significant inhibition against DPP-4. Salvianolicacid C, ginsenoside Rg₅ and timosaponin AI inhibited DPP-4 activity at the concentration of 5-50 μmol•L⁻¹ in a dose-dependent manner. Thus, our study provided a successful example for screening bioactive compounds from traditional Chinese medicines by using a novelfluorescent probe.

Renoprotective Effect of Gemigliptin, a Dipeptidyl Peptidase-4 Inhibitor, in Streptozotocin-Induced Type 1 Diabetic Mice

BACKGROUND: Dipeptidyl peptidase-4 (DPP-4) inhibitors are widely used in the treatment of patients with type 2 diabetes and have proven protective effects on diabetic kidney disease (DKD). Whether DPP-4 inhibitors have renoprotective effects on insulin-deficient type 1 diabetes has not been comprehensively examined. The aim of this study was to determine whether gemigliptin, a new DPP-4 inhibitor, has renoprotective effects in streptozotocin (STZ)-induced type 1 diabetic mice. METHODS: Diabetes was induced by intraperitoneal administration of a single dose of STZ. Mice with diabetes were treated without or with gemigliptin (300 mg/kg) for 8 weeks. Morphological changes of the glomerular basement membrane (GBM) were observed by electron microscopy and periodic-acid Schiff staining. In addition, we measured blood glucose and urinary albumin excretion and evaluated fibrotic markers using immunohistochemical staining, quantitative reverse transcription polymerase chain reaction analysis, and Western blot analysis. RESULTS: Gemigliptin did not reduce the blood glucose levels of STZ-treated mice. In gemigliptin-treated mice with STZ, a significant reduction in urinary albumin excretion and GBM thickness was observed. Immunohistological examination revealed that gemigliptin attenuated renal fibrosis induced by STZ and decreased extracellular matrix protein levels, including those of type I collagen and fibronectin, and Smad3 phosphorylation. In cultured rat renal cells, gemigliptin inhibited transforming growth factor β-stimulated type I collagen and fibronectin mRNA and protein levels via down-regulation of Smad3 phosphorylation. CONCLUSION: Our data demonstrate that gemigliptin has renoprotective effects on DKD, regardless of its glucose-lowering effect, suggesting that it could be used to prevent DKD, including in patients with type 1 diabetes.

Comparison of the efficacy and safety between DPP-4 Inhibitors and GLP-1 analogues for treatment of type 2 diabetes mellitus: A meta-analysis / 中国药学杂志

OBJECTIVE: To systematically review the efficacy and safety of dipeptidyl peptidase-4 (DPP-4) inhibitors versus glucagon like peptide-1 (GLP-1) receptor agonists for type 2 diabetes mellitus (T2DM). METHODS: Databases including EMbase, PubMed, The Cochrane Library, Clinical Trial, CBM, CNKI and WanFang Data, were searched electronically for randomized controlled trials (RCTs) of DPP-4 inhibitors versus GLP-1 receptor agonists for T2DM up to December 2015. Two reviewers independently screened literatures according to the inclusion and exclusion criteria, extracted data, and assessed the methodological quality of the included studies. Then Meta-analysis was performed using RevMan 5.3 soft ware. RESULTS: A total of 13 RCTs were included. The results of Meta-analysis showed that compared with DPP-4- inhibitors, GLP-1 receptor agonists were more effective in reducing the levels of fasting plasma glucose [MD = 0.93, 95% CI (0.48, 1.38), P < 0.0001] and glycated hemoglobin [ MD = 0.53, 95% CI (0.34, 0.73), P<0.00001] andBMI [MD = 1.53, 95% CI(0.83, 2.22), P <0.001]. However, DPP-4 inhibitors were more effective than GLP-1 receptor agonists in the reducing the 2-hour postprandial blood glucose level. And GLP-1 receptor agonists were more prone to cause gastrointestinal adverse reactions than DPP-4 inhibitors [RR =0.44,95% CI (0.33, 0.59), P <0.0001]. CONCLUSION GLP-1 receptor agonists are superior to DPP-4 inhibitors in controlling the fasting plasma glucose and glycated hemoglobin levels and reducing the body weight of T2DM patients, while DPP-4 inhibitors have better efficacy in reducing 2-hour postprandial blood glucose level, with better tolerability.

The Validity of the Assessment Criteria and Data Extraction in Meta-Analysis Articles / 医薬品情報学

<b>Objective: </b>Clinical articles are important for individualization of drug therapy.  Especially, meta-analysis is positioned at the highest evidence level.  Therefore, we assessed the Quality Score of Meta-Analysis (QSMA) which provides simple assessments of both the quality and the format of meta-analyses, by applying them to incretin-related drugs as a model.  Furthermore, we attempted to extract clinical data from the literature employing a certain minimum standard.<br><b>Method: </b>We searched for meta-analyses of incretin-related drugs for diabetes in PubMed and the Cochrane Library, scoring the extracted articles for format using PRISMA statements, and for quality using QSMA.  Additionally, we classified these articles into two groups with a QSMA score of 70% as the basis, and verified the analysis sets (ITT, FAS, PP or APT) and sensitivity analysis.  Furthermore, we looked into those articles that scored 70% or higher to extract data that were deemed to have significant statistical differences.<br><b>Results: </b>Scoring of the 66 articles studied yielded 69.9±19.4% (mean ± SD) for format and 62.1±17.8% for quality.  These two variables produced a regression line of <i>y</i>=0.777<i>x</i>+7.834.  Comparison of the two groups classified on the basis of a 70% score on QSMA yielded a significant difference in sensitivity analysis only (<i>p</i><0.05).  Seven effects and five side effects were extracted from articles with a QSMA score of 70% or higher.<br><b>Conclusion: </b>Although QSMA can provide simple assessment of quality and structure using eight items, analysis sets needs to be verified individually.  As the articles assessed provided statistically endorsed data, the clinical application of QSMA will be an issue in the future.

DPP4 inhibitor saxagliptin impact the body weight of patients with type 2 diabetes clinical observation / 局解手术学杂志

Objective To observe the impact of DPP4 inhibitor Saxagliptin on body weight of type 2 diabetes patients. Methods In this randomized and parallel study,50 patients were given either Saxagliptin(n=25)or Glimepiride(n=24). The changes of body weight, HbA1c and hypoglycemic events were observated in 12 weeks. Results There were no significant difference in gender,age and body weight between 2 groups(P>0. 05). After 12 weeks treatment,body weight has significant changed in both group,and the weight changes were sig-nificant differet in two groups:an average of 0. 4 kg weight was increased in Glimepiride group and 0. 4 kg weight was decreased in Saxagliptin group (P0. 05). Hypoglycemia event was happened four times in Glimepiride group,while no hypoglycemia event was happened in Saxagliptin group. Conclusion Compared with Glimepiride,Saxa-gliptin provides similar hypoglycemic action with less hypoglycemia,at the same time,Saxagliptin yields better results in lowering weight.

The Effect of DPP-4 Inhibitors on Metabolic Parameters in Patients with Type 2 Diabetes

BACKGROUND: We evaluated the effects of two dipeptidyl peptidase-4 (DPP-4) inhibitors, sitagliptin and vildagliptin, on metabolic parameters in patients with type 2 diabetes mellitus. METHODS: A total of 170 type 2 diabetes patients treated with sitagliptin or vildagliptin for more than 24 weeks were selected. The patients were separated into two groups, sitagliptin (100 mg once daily, n=93) and vildagliptin (50 mg twice daily, n=77). We compared the effect of each DPP-4 inhibitor on metabolic parameters, including the fasting plasma glucose (FPG), postprandial glucose (PPG), glycated hemoglobin (HbA1c), and glycated albumin (GA) levels, and lipid parameters at baseline and after 24 weeks of treatment. RESULTS: The HbA1c, FPG, and GA levels were similar between the two groups at baseline, but the sitagliptin group displayed a higher PPG level (P=0.03). After 24 weeks of treatment, all of the glucose-related parameters were significantly decreased in both groups (P=0.001). The levels of total cholesterol and triglycerides were only reduced in the vildagliptin group (P=0.001), although the sitagliptin group received a larger quantity of statins than the vildagliptin group (P=0.002).The mean change in the glucose- and lipid-related parameters after 24 weeks of treatment were not significantly different between the two groups (P=not significant). Neither sitagliptin nor vildagliptin treatment was associated with a reduction in the high sensitive C-reactive protein level (P=0.714). CONCLUSION: Vildagliptin and sitagliptin exert a similar effect on metabolic parameters, but vildagliptin exerts a more potent beneficial effect on lipid parameters.

Progress in dipeptidyl peptidase-4 and its inhibitors / 中国药学杂志

OBJECTIVE: To review the structures of dipeptidyl peptidase-4 (DPP-4) and its inhibitors and introduce the evaluation methods of several marketed inhibitors. METHODS: Preparation of this review is based on searching, categorizing, analyzing and summarizing of diplomatic and international literatures about DPP-4 and its inhibitors. RESULTS AND CONCLUSION: DPP-4 has attracted a lot of attention as a new target of type 2 diabetes, and some drug candidates have been developed and entered clinical phases. The structure-activity relationship study of various reported inhibitors could promote the development of more efficient DPP-4 inhibitors.

The new choice for the treatment of type 2 diabetes-DPP-4 inhibitors / 中国药学杂志

OBJECTIVE: To review the epidemiological status of type 2 diabetes (T2DM) and therapeutic applications of incre-tin-based novel oral hypoglycemic agents. METHODS: Based on the literatures in recent years, the mechanism and clinical evidence of DPP-4 inhibitors, particularly sitagliptin, in diabetes management were reviewed and introduced, especially sitagliptin. RESULTS AND CONCLUSION: DPP-4 inhibitors have many advantages and a good future in diabetes care, as either monotherapy or combination therapy. DPP-4 inhibitors have good safety profile and are recommend by some academic organizations.

DPP-4 inhibitors and glucose homeostasis - From cell to bedside / 中华内分泌代谢杂志

Type 2 Diabetes is the consequence of the disturbances of both α- and β-cell secretions.Glucagon-like peptide-1 ( GLP-1 ),which regulates the function of alpha and beta cells,has led to the emergence of a new class of oral anti-diabetic drugs.DPP-4 inhibitors,which increase the concentration of GLP-1 and consequently improve HbAlC,have become a choice for patients in different stages of diabetes.

Safety and tolerability of DPP-4 inhibitors / 中华内分泌代谢杂志

Safety and tolerability of anti-diabetic drugs should be among the most concern when it comes to management of Type 2 Diabetes.With the understanding of functions of incretin and degrading enzyme dipeptidepeptidase (DPP-4),several DPP-4 inhibitors with different chemical structures are now available.They are welltolerated with few weight gain,hypoglycemia or adverse effects.Therefore,DPP-4 inhibitors are considered to be among the ideal anti-hyperglycemic agents.