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Liraglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist that stimulates insulin secretion, inhibits glucagon secretion, delays gastric emptying, and reduces appetite by mimicking the effects of endogenous GLP-1 in humans, thereby effectively controlling blood sugar and weight. It was originally used to treat type 2 diabetes and was later approved for obesity management.
Liraglutide emerges from the structural modification process of human endogenous GLP-1. Through its structural design liraglutide replicates endogenous GLP-1 with key chemical modifications that boost its efficacy and stability which contributes to its importance as a treatment for type 2 diabetes and obesity. Liraglutide has a structure made up of 29 amino acid residues which are arranged in a helical polypeptide chain. The structure of liraglutide includes essential amino acids including arginine at position 34 and glutamic acid at position 26 which contribute to biological activity and GLP-1 receptor binding. The γ-carboxyl group of glutamic acid (Glu) at position 26 binds to lysine (Lys) in liraglutide through a C16 fatty acid chain (palmitic acid) to create an amide bond. The modification improves drug stability and prolongs its in vivo half-life for GLP-1 to 13 hours from the initial 2 hours. The drug's half-life is extended due to the substitution which allows it to bind to albumin more effectively.
CAT# | 10-101-59 |
Product Name | Liraglutide |
CAS No. | 204656-20-2 |
Sequence | HAEGTFTSDVSSYLEGQAAK [N-(1-oxohexadecyl)-L-γ-glutamyl] EFI AWLVRGRG |
M.W/Mr. | 3751.2 |
Molecular Formula | C172H265N43O51 |
The mechanism of action of liraglutide involves a variety of physiological effects mediated by GLP-1 receptors, including promoting insulin secretion, protecting pancreatic islet β cells, delaying gastric emptying, reducing appetite, lowering blood glucose, and cardiovascular protection. Together, these effects promote glycemic control and weight management in patients with diabetes, while also having potential therapeutic value for other metabolic diseases.
The mechanism of action of Liraglutide is mainly achieved by mimicking the biological function of endogenous GLP-1.
GLP-1 receptor activation
Liraglutide binds to and activates the GLP-1 receptor, thereby exerting a variety of physiological effects. GLP-1 receptors are widely distributed in the pancreas, intestine, central nervous system, and adipose tissue. In the pancreas, it stimulates the secretion of insulin by islet beta cells, while inhibiting the secretion of glucagon by alpha cells, thereby improving the balance of insulin secretion.
Promote the proliferation and protection of islet beta cells
Liraglutide promotes the proliferation and survival of islet beta cells by activating the PI3K/Akt/FoxO1 signaling pathway, thereby increasing the number and function of islet beta cells. In addition, it can also reduce the inflammatory response in adipose tissue and reduce the lipolysis of adipose cells, thereby indirectly improving the function of islet beta cells.
Delay stomach emptying and reduce appetite
In the central nervous system, liraglutide works by acting on GLP-1 receptors in the hypothalamus and back of the brain, suppressing appetite and delaying stomach emptying, making patients feel fuller for longer and thus reducing food intake.
Lower blood sugar and improve metabolism
Liraglutide is able to increase glucose-dependent insulin secretion while inhibiting glucose production in the liver, thereby reducing blood sugar levels. In addition, it has anti-inflammatory effects and is able to regulate the expression of inflammatory markers.
Cardiovascular protection
Liraglutide exerts anti-inflammatory, antioxidant, and cellular protective effects by activating multiple signaling pathways mediated by GLP-1 receptors, such as PI3K/Akt, thereby improving cardiovascular health.
Table.1 Cardiovascular disease (CVD) related peptides at Creative Peptides.
Liraglutide is mainly used to treat type 2 diabetes mellitus (T2DM) and obesity. Its mechanism of action includes increasing insulin secretion by activating GLP-1 receptors, inhibiting glucagon secretion, delaying gastric emptying, and reducing appetite.
Although Liraglutide is not currently approved for the treatment of type 1 diabetes, several studies are exploring its potential in this area. For example, the LEAD series of studies has shown that liraglutide can improve blood sugar control and restore glucose sensitivity to β cells in patients with type 1 diabetes. Another study found that the addition of liraglutide to insulin therapy was effective in improving metabolic parameters in patients with type 1 diabetes who were obese and had poor glycemic control. These studies provide an important basis for possible clinical applications in the future.
However, due to the lack of endogenous insulin secretion in patients with type 1 diabetes, direct use of liraglutide may not be a complete replacement for insulin therapy. As a result, current research is more focused on evaluating its effects as an adjunctive therapy, rather than replacing insulin altogether. Future studies are needed to further validate its safety and efficacy in patients with type 1 diabetes.
Liraglutide, an analog with 97% homology to human glucagon-like peptide (GLP-1) and acts as a GLP-1 receptor agonist, has been approved for the treatment of type 2 diabetes. This 97% homology was achieved by substituting arginine for lysine at position 34 of endogenous GLP-1. GLP-1 mimetics improve glycemic control through multiple mechanisms similar to the endogenous incretin hormone GLP-1. Liraglutide is the second in class of glucagon like peptide-1 (GLP-1) mimetics now available for the treatment of type 2 diabetes. The first product licensed was exenatide which is a twice-daily delivered functional partly dipeptidyl peptidase-IV (DPP-IV) resistant analogue of human GLP-1 which is now in established use.
Liraglutide contains a fatty acid molecule that binds to albumin and prolongs the half-life of the structure. Receptors for GLP-1 are found in pancreatic alpha and beta cells; the central and peripheral nervous systems; and the heart, lungs, and gastrointestinal (GI) tract. Several studies have demonstrated that GLP-1 receptor agonists may improve pancreatic beta cell function, which may delay disease progression if maintained over the long term. Through the messenger intracellular cyclic adenosine monophosphate (cAMP), liraglutide causes insulin to be secreted in the presence of elevated glucose levels. Because of the receptor locations, liraglutide also inhibits glucagon secretion and delays gastric emptying.
Table.2 Peptides in diabetes at Creative Peptides.
Liraglutide has been shown to aid in weight loss, improving both patient satisfaction and health-related quality of life. It has proven effective in inducing and sustaining weight loss in obese patients, including those with conditions such as hypertension, dyslipidemia, type 2 diabetes, and obstructive sleep apnea. Studies indicate that the weight loss achieved with liraglutide is greater than that with orlistat or lorcaserin, although it is slightly less than the weight loss observed with the phentermine/topiramate combination treatment. However, liraglutide is associated with a higher discontinuation rate due to adverse effects (primarily gastrointestinal) when compared to other weight loss medications like lorcaserin, with the latter showing the lowest discontinuation rate. Despite these concerns, liraglutide remains a valuable option in the physician's toolkit for addressing the growing obesity epidemic, both in the U.S. and globally.
In a 56-week randomized controlled trial, a 3 mg dose of liraglutide led to a ≥5% weight loss in 54.3% of patients, compared to just 21.4% in the placebo group. Moreover, liraglutide has been shown to improve blood glucose control and cardiovascular health in patients with type 2 diabetes. However, its use is not without side effects, including nausea, constipation, and fatigue. Despite these, most patients tolerate the medication well, with many maintaining weight loss benefits over the long term. It is important to note that the effectiveness of liraglutide may vary among individuals, with some patients needing additional lifestyle changes, such as diet and exercise, to achieve optimal results.
Overall, liraglutide is an effective weight management medication, particularly for overweight or obese individuals with related metabolic conditions. However, further research is needed to assess its long-term efficacy and safety, especially regarding its effects on cardiovascular morbidity and mortality in a diverse population.
Liraglutide promotes weight loss through a variety of mechanisms that are primarily related to its role as a glucagon-like peptide-1 (GLP-1) receptor agonist.
Slows down gastric emptying: Liraglutide slows the rate of gastric emptying, which increases satiety and reduces food intake. This effect helps to reduce total daily caloric intake, which in turn promotes weight loss.
Appetite suppression: Liraglutide reduces appetite by stimulating satiety-related areas in the central nervous system, making patients feel satiety earlier, thereby reducing the amount of food eaten.
Increases insulin secretion: Liraglutide stimulates insulin secretion while inhibiting glucagon secretion. This balance helps to lower blood sugar levels and reduces hunger due to high blood sugar, which indirectly reduces caloric intake.
Reduces fat accumulation: Studies have shown that liraglutide can reduce the accumulation of adipose tissue, especially visceral fat. Not only does this help with weight loss, but it may also improve metabolic health.
Reduced leptin levels: The study found that mice treated with liraglutide had significantly lower levels of leptin, a hormone that promotes appetite and fat storage. Therefore, lowering leptin levels may be one of the important factors in promoting weight loss.
Liraglutide holds promising research significance beyond its current clinical applications. Ongoing studies are exploring its potential in neuroprotection, liver disease, and cardiovascular health, highlighting its anti-inflammatory and metabolic regulatory properties. Further investigation may reveal expanded therapeutic uses, such as adjunctive therapy for type 1 diabetes and treatments for metabolic syndrome-related disorders, paving the way for innovative interventions in metabolic and chronic disease management.
1. What does liraglutide do for weight loss?
Liraglutide helps with weight loss by increasing feelings of fullness, reducing hunger, and slowing gastric emptying, which collectively leads to reduced calorie intake.
2. Is liraglutide the same as Ozempic?
No, liraglutide is not the same as Ozempic. Liraglutide is branded as Saxenda or Victoza, while Ozempic contains semaglutide. Both are GLP-1 receptor agonists.
3. Is liraglutide a GLP-1?
Yes, liraglutide is a GLP-1 receptor agonist that mimics the action of natural incretin hormones to regulate blood sugar and promote weight loss.
4. What type of drug is liraglutide?
Liraglutide is a GLP-1 receptor agonist used for managing type 2 diabetes (Victoza) and for chronic weight management (Saxenda) in overweight or obese individuals.
References
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