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Lixisenatide | CAS No: 320367-13-3 | GMP-certified suppliers
A medication that improves glycemic control in adults with type 2 diabetes mellitus as an adjunct to diet, exercise, and insulin therapy for enhanced blood glucose management.
Therapeutic categories
Primary indications
- Lixisenatide is indicated as an adjunct to diet and exercise to improve glycemic control in adult patients with type II diabetes mellitus
- It is also available in combination with [insulin glargine] for the same indication
Product Snapshot
- Lixisenatide is a parenteral injectable peptide formulation administered via subcutaneous injection
- It is primarily used as an adjunct therapy for glycemic control in adult patients with type II diabetes mellitus
- The product is approved for use in key regulatory markets including the US, Canada, and the EU
Clinical Overview
Pharmacodynamically, lixisenatide activates the GLP-1 receptor, primarily located on pancreatic beta cells and throughout the gastrointestinal tract. This receptor activation leads to increased glucose-dependent insulin secretion through augmented exocytosis of insulin granules. Additionally, GLP-1 receptor engagement delays gastric emptying, which contributes to a reduction in postprandial blood glucose excursions.
The mechanism of action involves the stimulation of adenylyl cyclase following receptor binding, resulting in elevated intracellular cyclic adenosine monophosphate (cAMP). The increase in cAMP activates protein kinase A (PKA) and exchange proteins directly activated by cAMP (Epac1 and Epac2). These signaling pathways facilitate the release of calcium ions from intracellular stores via an amplification mechanism, enhancing glucose-stimulated insulin secretion.
Pharmacokinetic data indicate that lixisenatide is primarily eliminated via the renal route. Specific parameters such as absorption rates, bioavailability, and half-life are context-dependent and should be consulted from dedicated pharmacokinetic sources.
Safety profiles include considerations common to GLP-1 receptor agonists, such as potential gastrointestinal disturbances and the risk of hypoglycemia especially when used in combination with other antidiabetic agents. Pancreatitis and hypersensitivity reactions warrant monitoring during clinical use.
For API sourcing, rigorous quality control is critical given the peptide nature of lixisenatide, requiring adherence to stringent purity, stability, and assay standards. Compliance with Good Manufacturing Practice (GMP) is essential to ensure consistency in pharmacological activity and safety for pharmaceutical formulation.
Identification & chemistry
| Generic name | Lixisenatide |
|---|---|
| Molecule type | Biotech |
| CAS | 320367-13-3 |
| UNII | 74O62BB01U |
| DrugBank ID | DB09265 |
Pharmacology
| Summary | Lixisenatide is a glucagon-like peptide-1 (GLP-1) receptor agonist that enhances glucose-dependent insulin secretion via activation of adenylyl cyclase and downstream signaling pathways involving PKA, Epac1, and Epac2. This mechanism amplifies calcium release in pancreatic beta cells, promoting insulin exocytosis and lowering blood glucose levels. Additionally, lixisenatide delays gastric emptying through GLP-1 receptor activation in the gastrointestinal tract, contributing to improved postprandial glycemic control. |
|---|---|
| Mechanism of action | The activation of the GLP-1 receptor by lixisenatide results in the activation of adenylyl cyclase. This increases the concentration of cyclic adenosine monophosphate in the cell leading to the activation of protein kinase A (PKA) as well as Epac1 and Epac2. PKA, Epac1, and Epac2 are involved the in release of Ca2+ from the endoplasmic reticulum which is known as the "amplification" pathway which increases insulin release when the triggering pathway is activated. By activating this amplification pathway lixisenatide increases glucose stimulated insulin secretion. |
| Pharmacodynamics | Lixisenatide acts as an agonist at the GLP-1 receptor. In the pancreas, this agonism results in increased glucose-stimulated insulin exocytosis by beta islet cells. This produces a reduction in blood glucose due to increased glucose uptake by tissues. GLP-1 receptor activation in the GI tract results in delayed gastric emptying which is thought to mediate the effects of lixisenatide on postprandial blood glucose. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Glucagon-like peptide 1 receptor | Humans | agonist |
ADME / PK
| Absorption | Following subcutaneous administration, the median T<sub>max</sub> of lixisenatide ranged from 1-3.5 hours, with no clinically relevant differences in the rate of absorption noted between possible injection sites (i.e. thigh, abdomen, or arm). |
|---|---|
| Half-life | Following the administration of multiple doses in patients with type II diabetes mellitus, the mean terminal half-life of lixisenatide was approximately 3 hours. |
| Protein binding | Lixisenatide is approximately 55% bound to human plasma proteins. |
| Metabolism | Lixisenatide is likely catabolized via non-specific proteolytic degradation. |
| Route of elimination | Lixisenatide is presumably eliminated via glomerular filtration and proteolytic degradation. |
| Volume of distribution | The apparent volume of distribution following subcutaneous administration is approximately 100 L. |
| Clearance | The mean apparent clearance of lixisenatide is approximately 35 L/h. |
Formulation & handling
- Lixisenatide is a peptide-based biotech API formulated exclusively for subcutaneous injection in liquid solution form.
- Timing of administration relative to meals is critical due to its sensitivity to food intake, requiring dosing within one hour before the first meal.
- Handling considerations should address cold chain storage and protection from agitation to maintain stability and bioactivity.
Regulatory status
| Lifecycle | The API is approaching market maturity as key patents in the United States are set to expire between March 2024 and April 2025. It is currently marketed in the US, Canada, and the EU, where patent protections may influence generic entry timelines. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Lixisenatide is represented by multiple originator companies with branded products available primarily in the US, Canada, and EU markets. The presence of several US patents expiring in 2024 and 2025 indicates that generic competition is either imminent or already emerging in these regions. This suggests a shift in the supply landscape toward increased availability of generic APIs following patent expirations. |
|---|
Safety
| Toxicity | Thyroid C-cell adenomas occurred in rats when exposed to >15 times human exposure of 20mcg/day. Overdose is associated with GI side effects typical of GLP-1 receptor agonists. |
|---|
- Animal studies demonstrated thyroid C-cell adenomas in rats at exposure levels exceeding 15 times the human dose of 20 mcg/day
- Overdose may result in gastrointestinal adverse effects consistent with GLP-1 receptor agonist class-related toxicity
- Handle with care to minimize occupational exposure, considering potential endocrine-related safety concerns observed in preclinical models
Lixisenatide is a type of GLP1 agonists
GLP-1 agonists, short for glucagon-like peptide-1 agonists, are a subcategory of pharmaceutical APIs (active pharmaceutical ingredients) commonly used in the treatment of type 2 diabetes mellitus. These medications mimic the actions of GLP-1, a naturally occurring hormone in the body that helps regulate blood sugar levels.
GLP-1 agonists work by binding to GLP-1 receptors in the pancreas, promoting insulin secretion and inhibiting glucagon release. This mechanism of action leads to improved glucose control, reduced fasting and postprandial blood glucose levels, and decreased hemoglobin A1c levels.
One of the key advantages of GLP-1 agonists is their ability to promote weight loss in patients with type 2 diabetes. These medications slow down gastric emptying, increase satiety, and reduce food intake, resulting in modest but significant weight reduction.
Additionally, GLP-1 agonists have shown cardiovascular benefits, including a reduction in the risk of major adverse cardiovascular events, such as heart attack and stroke. They also exhibit a lower risk of hypoglycemia compared to some other antidiabetic medications.
Some commonly prescribed GLP-1 agonists include exenatide, liraglutide, dulaglutide, and semaglutide. These APIs are typically administered via subcutaneous injection, either once or twice daily, or in some cases, as weekly formulations.
In conclusion, GLP-1 agonists are a valuable class of pharmaceutical APIs used in the management of type 2 diabetes. Their mechanism of action, which includes glucose control, weight loss promotion, and cardiovascular benefits, makes them a favorable choice for patients seeking effective and safe antidiabetic therapy.
Lixisenatide (GLP1 agonists), classified under Anti-diabetics
Anti-diabetics, belonging to the pharmaceutical API (Active Pharmaceutical Ingredient) category, are a group of compounds designed to manage and treat diabetes mellitus, a chronic metabolic disorder characterized by high blood sugar levels. These medications play a vital role in controlling diabetes and preventing complications associated with the disease.
Anti-diabetics encompass a wide range of drug classes, including biguanides, sulfonylureas, thiazolidinediones, dipeptidyl peptidase-4 (DPP-4) inhibitors, sodium-glucose cotransporter-2 (SGLT2) inhibitors, and glucagon-like peptide-1 (GLP-1) receptor agonists. Each class works through different mechanisms to regulate blood sugar levels and improve insulin sensitivity.
Biguanides, such as metformin, reduce glucose production by the liver and enhance insulin sensitivity in peripheral tissues. Sulfonylureas, like glipizide, stimulate insulin secretion from pancreatic beta cells. Thiazolidinediones, including pioglitazone, improve insulin sensitivity in muscle and adipose tissues. DPP-4 inhibitors, such as sitagliptin, increase insulin release and inhibit glucagon secretion. SGLT2 inhibitors, like dapagliflozin, decrease renal glucose reabsorption, leading to increased urinary glucose excretion. GLP-1 receptor agonists, such as exenatide, enhance insulin secretion, suppress glucagon release, slow gastric emptying, and promote satiety.
These anti-diabetic APIs serve as the foundational ingredients for the formulation of various oral tablets, capsules, and injectable medications used in the treatment of diabetes. By targeting different aspects of glucose regulation, they help patients achieve and maintain optimal blood sugar levels, thus reducing the risk of diabetic complications, such as cardiovascular disease, neuropathy, and nephropathy.
It is crucial for healthcare professionals to prescribe and administer these anti-diabetic medications appropriately, considering factors like the patient's medical history, co-existing conditions, and potential drug interactions. Regular monitoring of blood glucose levels and close medical supervision are necessary to ensure effective diabetes management.
In conclusion, anti-diabetics form a critical category of pharmaceutical APIs used for the treatment of diabetes. These compounds, encompassing various drug classes, work through distinct mechanisms to regulate blood sugar levels and improve insulin sensitivity. By facilitating glucose control, anti-diabetic APIs help mitigate the risk of complications associated with diabetes mellitus, ultimately promoting better health outcomes for patients.
Lixisenatide API manufacturers & distributors
Compare qualified Lixisenatide API suppliers worldwide. We currently have 1 companies offering Lixisenatide API, with manufacturing taking place in 1 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Medilux Labs | Producer | India | India | CoA, GMP | 10 products |
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