Semaglutide, a glucagon like peptide-1 receptor agonist with cardiovascular benefits for management of type 2 diabetes

Mahapatra, Manoj Kumar; Karuppasamy, Muthukumar; Sahoo, Biswa Mohan

doi:10.1007/s11154-021-09699-1

Cited by 71 publications

(40 citation statements)

References 74 publications

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“…It reduces fasting and postprandial glucose levels by promoting insulin secretion in a glucose-dependent manner and suppressing hepatic gluconeogenesis through blunted glucagon release. Moreover, it improves both proinsulin to insulin ratio, which suggests improved β-cell function and insulin sensitivity through body weight and fat loss consequent to reduced energy intake and gastric motility[ 89 ].…”

Section: Details Concerning Semaglutide’s Pharmacologic Properties Fa...mentioning

confidence: 99%

Semaglutide-eye-catching results

Berković¹,

Strollo²

2023

World J Diabetes

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Semaglutide is a glucagon-like peptide-1 receptor agonist used either orally every day or subcutaneously once a week for the treatment of type 2 diabetes mellitus and, more recently, at higher doses, for the treatment of obesity. Both diseases are reaching epidemic proportions and often coexist, posing patients with a high risk for cardiovascular disease and death. Therefore, an agent such as semaglutide, which offers clinically significant weight loss and cardiovascular benefits, is essential and will be increasingly used in high-risk patients. However, during the SUSTAIN clinical trial program (Semaglutide Unabated Sustainability in treat-ment of type 2 diabetes), a safety issue concerning the progression and worsening of diabetic retinopathy emerged. The existing explanation so far mainly supports the role of the magnitude and speed of HbA1c reduction, a phenomenon also associated with insulin treatment and bariatric surgery. Whether and to which extent the effect is direct is still a matter of debate and an intriguing topic to investigate for suitable preventative and rehabilitative purposes. In this minireview, we will summarize the available data and suggest guidelines for a comprehensive semaglutide clinical utilization until new evidence becomes available.

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Section: Details Concerning Semaglutide’s Pharmacologic Properties Fa...mentioning

confidence: 99%

Semaglutide-eye-catching results

Berković¹,

Strollo²

2023

World J Diabetes

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“…Aib (2-aminoisobutyric acid) was used to replace the alanine residue at position 8 which prevents enzymatic degradation of the molecule by dipeptidyl peptidase-4 (DPP-4) inhibitor. In addition, lysine residue in position 34 was substituted by arginine and lysine residue at 26 th position was acylated and attached through a linker with a C18 di-acid chain, which enhances stronger binding to albumin [26,40]. Despite these changes, semaglutide is still exposed to rapid proteolytic degradation in the digestive tract, and oral administration could be difficult given to the acidic environment and low permeability of peptides through gastrointestinal epithelium [3,52].…”

Section: Challenges Of An Oral Peptide Developmentmentioning

confidence: 99%

Untitled

2023

FARMACIA

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Co-existing diabetes and obesity, frequently described by the term "diabesity", is a major health problem associated with increased long-term complications and mortality. The management of "diabesity" could be challenging, because several antidiabetic drugs cause weight gain. Glucagon-like peptide receptor agonists (GLP-1 RAs) have been demonstrated to be effective agents for achieving glycaemic control in addition to reducing body weight in patients with type 2 diabetes. Oral semaglutide, the first oral formulation of a GLP-1 RA, is an important therapeutic option for individuals with a preference for oral therapy. This medication was created by co-formulating the semaglutide molecule with an absorption enhancer (SNAC) to overcome the difficulties of oral peptide administration. The introduction of an oral GLP-1 RA broadens the therapeutic choices for patients and represents an important milestone in the management of "diabesity". RezumatCoexistența obezității și a diabetului zaharat, descrise frecvent prin termenul "diabesity" sau "diabezitate", reprezintă o problemă majoră de sănătate asociată cu creșterea complicațiilor și a mortalității pe termen lung. Managementul "diabezității" ar putea fi o provocare, deoarece mai multe medicamente antidiabetice pot determina creștere în greutate. S-a demonstrat că agoniştii receptorilor glucagon-like peptide-1 (GLP-1 RA) sunt eficienți pentru obținerea controlului glicemic pe lângă reducerea greutății corporale în cazul pacienților cu diabet zaharat tip 2. Semaglutida orală, prima formularea orală a GLP-1 RA, este o opțiune terapeutică importantă pentru persoanele cu preferință pentru terapia orală. Acest medicament a fost creat prin co-formularea moleculei de semaglutidă cu un amplificator de absorbție (SNAC) pentru a depăși dificultățile administrării orale a peptidelor. Introducerea unui agonist de receptor GLP-1 cu administrare orală, lărgește opțiunile terapeutice pentru pacienți și reprezintă un medicament cheie în tratamentul "diabezității".

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“…Interestingly, GLP-1R has been utilized to mediate tumor specificity for insulinoma that highly expresses GLP-1R during radiotherapy. A single injection of an Ahx-DTPA-(111)In)NH (2) In-labeled GLP-1R agonist markedly reduced tumor volume in a dose-dependent manner in a mouse model of insulinoma (94). Mechanistical studies suggest that GLP-1RAs may reduce tumor growth in prostate (95) and breast cancer (96,97).…”

Section: Tumorsmentioning

confidence: 99%

GLP-1 receptor agonist as a modulator of innate immunity

Mei

Wei

et al. 2022

Front. Immunol.

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Glucagon-like peptide-1 (GLP-1) is a 30-amino acid hormone secreted by L cells in the distal ileum, colon, and pancreatic α cells, which participates in blood sugar regulation by promoting insulin release, reducing glucagon levels, delaying gastric emptying, increasing satiety, and reducing appetite. GLP-1 specifically binds to the glucagon-like peptide-1 receptor (GLP-1R) in the body, directly stimulating the secretion of insulin by pancreatic β-cells, promoting proliferation and differentiation, and inhibiting cell apoptosis, thereby exerting a glycemic lowering effect. The glycemic regulating effect of GLP-1 and its analogues has been well studied in human and murine models in the circumstance of many diseases. Recent studies found that GLP-1 is able to modulate innate immune response in a number of inflammatory diseases. In the present review, we summarize the research progression of GLP-1 and its analogues in immunomodulation and related signal pathways.

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Semaglutide, a glucagon like peptide-1 receptor agonist with cardiovascular benefits for management of type 2 diabetes

Cited by 71 publications

References 74 publications

Semaglutide-eye-catching results

Semaglutide-eye-catching results

Untitled

GLP-1 receptor agonist as a modulator of innate immunity

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