Fixed-dose combination of sitagliptin and metformin for the treatment of type 2 diabetes

Reynolds, Jonathan K.

doi:10.2147/dmsott.s4637

Cited by 5 publications

(4 citation statements)

References 43 publications

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“…In our study, sitagliptin, added to previously taken antidiabetic agents, proved to be effective in improving glycemic profile, reducing HbA 1c by À17.5%, FPG by À12.7%, PPG by À20.5%. Regarding insulin resistance, sitagliptin decreased FPI by À8.3% and HOMA-IR by À20.0%, confirming that what have been already reported in short-term studies [32,33] can be applied also after 2 years of treatment. Different from what we have previously reported [10], as regards body weight, this time, sitagliptin reduced body weight by À4.3%.…”

Section: Discussionsupporting

confidence: 84%

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Sitagliptin added to previously taken antidiabetic agents on insulin resistance and lipid profile: a 2‐year study evaluation

Derosa

Ragonesi²,

Fogari

et al. 2012

Fundamemntal Clinical Pharma

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The aim of this study was to evaluate whether the positive effects of sitagliptin on glycemic control and insulin resistance were maintained also after 2 years of therapy and whether sitagliptin could be effective also in improving lipid profile. In this randomized, double-blind, placebo-controlled trial, 205 patients with type 2 diabetes in therapy with different antidiabetic drugs were randomized to add sitagliptin 100 mg once a day or placebo to their current therapy. We evaluated at the baseline and after 6, 12, 18, and 24 months the following parameters: body mass index, glycated hemoglobin (HbA1c ), fasting plasma glucose (FPG), postprandial plasma glucose (PPG), fasting plasma insulin (FPI), homeostasis model assessment insulin resistance index (HOMA-IR), total cholesterol (TC), high-density lipoprotein cholesterol (HDL-C), low-density lipoprotein cholesterol (LDL-C), triglycerides (Tg). Sitagliptin, added to previously taken antidiabetic agents, proved to be effective in improving glycemic profile, reducing HbA1c by -17.5%, FPG by -12.7%, PPG by -20.5%. Regarding insulin resistance, sitagliptin decreased FPI by -8.3% and HOMA-IR by -20.0%, confirming that what have been already reported in short-term studies can be applied also after 2 years of treatment. Sitagliptin also reduced body weight by -4.3%. Our study also showed the positive effect of sitagliptin on lipid profile; in particular, sitagliptin decreased TC by -13.3%, LDL-C by -20.4%, and Tg by -32.3%, and also increased HDL-C by + 13.6%. Sitagliptin proved to be effective on glycemic profile and insulin resistance even after 2 years of therapy and to be effective in improving body weight and lipid profile.

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Section: Discussionsupporting

confidence: 84%

“…Sitagliptin 100 mg once daily produced a significant reduction in HbA 1c (0.65%, P < 0.001) and FPG (25.4 mg/dL, P < 0.001) compared with baseline. These data were confirmed also by two reviews conducted by Reynolds [32] and by Barnard et al [33] about the safety and efficacy of a fixed sitagliptin plus metformin combination.…”

Section: Discussionsupporting

confidence: 73%

Sitagliptin added to previously taken antidiabetic agents on insulin resistance and lipid profile: a 2‐year study evaluation

Derosa

Ragonesi²,

Fogari

et al. 2012

Fundamemntal Clinical Pharma

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“…Given that T2DM is a progressive disease, many patients may require additional agents to achieve their individualized glycemic goals over time. Many fixed-dose combinations, including dual DPP-4 inhibitor/metformin and triple DPP-4 inhibitor/sodium-glucose cotransporter 2 (SGLT-2) inhibitor/metformin, have been developed and approved for use in T2DM patients. However, these combinations require once-daily or twice-daily administration, which will reduce the advantages of intermittent administration of long-acting DPP-4 inhibitors. , In addition, there are some clinical results showing that once-weekly regimens do not have significantly higher adherence and persistence rates than once-daily regimens .…”

Section: Discussionmentioning

confidence: 99%

Development of Long-Acting Dipeptidyl Peptidase-4 Inhibitors: Structural Evolution and Long-Acting Determinants

Li,

Deng,

et al. 2023

J. Med. Chem.

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Considerable effort has been made to achieve less frequent dosing in the development of DPP-4 inhibitors. Enthusiasm for long-acting DPP-4 inhibitors is based on the promise that such agents with less frequent dosing regimens are associated with improved patient adherence, but the rational design of long-acting DPP-4 inhibitors remains a major challenge. In this Perspective, the development of longacting DPP-4 inhibitors is comprehensively summarized to highlight the evolution of initial lead compounds on the path toward developing long-acting DPP-4 inhibitors over nearly three decades. The determinants for long duration of action are then examined, including the nature of the target, potency, binding kinetics, crystal structures, selectivity, and preclinical and clinical pharmacokinetic and pharmacodynamic profiles. More importantly, several possible approaches for the rational design of long-acting drugs are discussed. We hope that this information will facilitate the design and development of safer and more effective long-acting DPP-4 inhibitors and other oral drugs. ■ SIGNIFICANCE• The evolution of initial lead compounds on the path toward developing long-acting DPP-4 inhibitors over nearly three decades is reviewed. • The determinants for long duration of action are examined, including the nature of the target, potency, binding kinetics, crystal structures, selectivity, and preclinical and clinical PK and PD profiles. • Possible approaches for the rational design of longacting drugs are discussed.

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“…The drug has been used as monotherapy as well as combination therapy (along with other class of anti-diabetic drugs) intending to achieve synergistic efficacy. For example, a sitagliptin and metformin combination (Janumet, Merck) was made available and approved in 2009 [9] .…”

Section: Classification Of the Drugmentioning

confidence: 99%

Double Edge Effect of Dpp4 Inhibitor Sitagliptin, a Type-2 Anti-Diabetic Drug, on Inflammation, Injury and Cancer

Giri¹,

Sarkar²,

Dey³

et al. 2017

JSRB

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Maintaining a healthy glycaemic condition is associated with so many more other protective/precautionary attributes. Recent advancement in the field of drug discovery have led us find more and more options to choose from. DPP-4 inhibitor sitagliptin makes sustained expression of incretins GLP-1 and GIP that in turn establishes glycaemic control. But recent reports claimed pro-inflammatory as well as pro-carcinogenic action of the drug after prolonged use in T2DM patients. Interestingly, in those cases also, the effector molecule responsible is said to be the incretin GLP-1. The same molecule has been hypothesized for being responsible to cause thyroid C-cell carcinomas. In vitro investigations using human cell lines did not show any clues in support of carcinoma formation. Instead, the DPP-4 inhibitory action of sitagliptin serves in other complications associated with T2DM. In any tissue injury due to hypoxic stress in T2DM, sitagliptin serves in the tissue repair mechanisms via its DPP-4 inhibiting property. Consequently, DPP-4, for not being able to be active in presence of sitagliptin, fails to truncate the CXCL-12/SDF-1 and therefore helps in the homing of HPCs/EPCs to repair the injured tissue. In conclusion, it can be said that more research is definitely required to be confirmed about the pre-cancerous activity of the drug, and to make the drug more usable in favour of the other beneficial effects of it.

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Fixed-dose combination of sitagliptin and metformin for the treatment of type 2 diabetes

Cited by 5 publications

References 43 publications

Sitagliptin added to previously taken antidiabetic agents on insulin resistance and lipid profile: a 2‐year study evaluation

Sitagliptin added to previously taken antidiabetic agents on insulin resistance and lipid profile: a 2‐year study evaluation

Development of Long-Acting Dipeptidyl Peptidase-4 Inhibitors: Structural Evolution and Long-Acting Determinants

Double Edge Effect of Dpp4 Inhibitor Sitagliptin, a Type-2 Anti-Diabetic Drug, on Inflammation, Injury and Cancer

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