Liraglutide CAS-204656-20-2 Beauty slimming can be customized raw materials weight loss

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Detailed Introduction to Liraglutide Peptide Products

Liraglutide, a synthetic peptide, is a glucagon-like peptide-1 (GLP-1) analog produced through recombinant DNA technology using Saccharomyces cerevisiae. As a long-acting GLP-1 receptor agonist,), with a molecular formula of C172H265N43O51 and a molecular weight of 3751.2. Appearing as a white powder, Liraglutide exhibits limited solubilityand sodium chloride solutions.

1. Pharmacological Mechanism

1. Interaction with GLP-1 Receptors: Sharing 97% sequence homology with human GLP-1, Liraglutide binds and activates GLP-1 receptors. GLP-1, an endogenous incretin hormone, stimulates insulin release in pancreatic β-cells via Gs protein activation and adenylyl cyclase coupling, increasing intracellular cyclic adenosine monophosphate (cAMP) levels in the presence of elevated glucose. Insulin secretion decreases as blood glucose returns to normal.

2. Regulation of Glucagon Secretion: Liraglutide suppresses excessive glucagon secretion in a glucose-dependent manner. It inhibits glucagon when blood glucose is high while allowing normal glucagon release during hypoglycemia.

3. Additional Hypoglycemic Effects: By slowing gastric emptying, Liraglutide reduces appetite, leading to decreased calorie intake, weight loss, and improved glycemic control.

2. Pharmacokinetic Properties

1. Absorption: After subcutaneous injection, Liraglutide is absorbed slowly, reaching peak plasma concentration within 8-12 hours. Its exposure increases proportionally with dosage, with an absolute bioavailability of approximately 55%.

2. Distribution: Highly bound to plasma proteins (>98%), Liraglutide has an apparent volume of distribution of 11-17 L after subcutaneous injection and 0.07 L/kg after intravenous injection.

3. Metabolism and Elimination: The primary plasma component is the unchanged drug. Liraglutide is metabolized similarly to large proteins, with an average clearance rate of 1.2 L/h and a half-life of about 13 hours. Only a small fraction of the administered radioactivity is excreted as Liraglutide-related metabolites in urine or feces.

3. Clinical Applications

1. Type 2 Diabetes Management: Indicated for adults with type 2 diabetes, especially those uncontrolled on maximum tolerated doses of metformin or sulfonylureas, Liraglutide can be used in combination with these medications. It effectively reduces both fasting and postprandial blood glucose levels, as well as glycated hemoglobin A1C (HbA1C). Administered subcutaneously once daily at any time, the starting dose is 0.6 mg, which can be increased to 1.2 mg after one week and to 1.8 mg for further glycemic control, with 1.8 mg being the recommended maximum daily dose.

2. Cardiovascular Risk Reduction: In adults with type 2 diabetes and cardiovascular disease, Liraglutide significantly reduces the risk of major adverse cardiovascular events (cardiovascular death, non-fatal myocardial infarction, or non-fatal stroke), playing a crucial role in comprehensive diabetes management.

4. Adverse Reactions

1. Gastrointestinal Symptoms: Nausea and diarrhea are very common, while vomiting, constipation, abdominal pain, and dyspepsia are also frequently reported. These symptoms typically subside within days or weeks of continuous treatment.

2. Hypoglycemia: Severe hypoglycemia is rare during monotherapy or when combined with oral hypoglycemic agents other than sulfonylureas. However, the risk increases when used with sulfonylureas, necessitating potential dose adjustments.

3. Immunogenicity: Antibodies develop in 8.6% of patients on average, but usually do not impair treatment efficacy.

4. Pancreatitis: A small number of acute pancreatitis cases have been reported during long-term clinical trials.

5. Allergic Reactions: Post-marketing reports include urticaria, rash, itching, and, rarely, severe symptoms such as hypotension, palpitations, dyspnea, and edema.

5. Contraindications

1. Contraindicated in patients with known Liraglutide or its excipients.

2. Not suitable for type 1 diabetes or diabetic ketoacidosis treatment.

3. Prohibited in individuals with a history or family history of medullary thyroid carcinoma (MTC) or multiple endocrine neoplasia syndrome type 2 (MEN2).

6. Precautions for Special Populations

1. Pregnancy and Lactation: Insufficient data exist for pregnant women, and animal studies suggest reproductive toxicity; thus, it is contraindicated during pregnancy and breastfeeding.

2. Pediatrics: Safety and efficacy in children under 18 remain unestablished.

3. Elderly: Limited experience in patients ≥75 years old  careful assessment.

4. Renal Impairment: No dose adjustment is needed for mild cases; use is not recommended in severe cases, including end-stage renal disease.

5. Hepatic Impairment: Limited clinical experience; not recommended for use.

6. Other Conditions: Use in patients with inflammatory bowel disease or diabetic gastroparesis is not advised due to limited data.

Since its approval by the European Commission for type 2 diabetes treatment in July 2009, Liraglutide has been marketed in 105 countries, with over 1.2 million global users. As research progresses, its clinical value and potential applications are expected to expand further.

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