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Volanesorsen
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Looking for Volanesorsen API 915430-78-3?
- Description:
- Here you will find a list of producers, manufacturers and distributors of Volanesorsen. You can filter on certificates such as GMP, FDA, CEP, Written Confirmation and more. Send inquiries for free and get in direct contact with the supplier of your choice.
- API | Excipient name:
- Volanesorsen
- Synonyms:
- Cas Number:
- 915430-78-3
- DrugBank number:
- DB15067
- Unique Ingredient Identifier:
- 2O4BE0K238
General Description:
Volanesorsen, identified by CAS number 915430-78-3, is a notable compound with significant therapeutic applications. Volanesorsen is an antisense oligonucleotide that binds to apoC-III mRNA to prevent its translation. It is indicated to treat familial chylomicronemia, a genetic condition that prevents breakdown of triglycerides and chylomicrons. This drug is not commonly prescribed as it is used as an adjunct to diet in patients at high risk for pancreatitis, who have had inadequate response to triglyceride lowering therapy. Volanesorsen was granted a conditional approval by the European Medicines Agency.
Indications:
This drug is primarily indicated for: Volanesorsen is conditionally approved by the EMA as an adjunct to diet in adults with familial chylomicronemia, at high risk for pancreatitis, and who have had an inadequate response to diet and triglyceride lowering therapy. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.
Metabolism:
Volanesorsen undergoes metabolic processing primarily in: Volanesorsen is metabolized by endonucleases and exonucleases in a nonspecific manner. The unchanged parent drug is 26% recovered in the urine and pentamer to heptamer sized metabolites account for 55% of urinary recovery.[L16621. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.
Absorption:
The absorption characteristics of Volanesorsen are crucial for its therapeutic efficacy: Volanesorsen is approximately 80% bioavailable. A 285mg dose given weekly reaches a Cmax of 8.92 µg/mL, with an AUC of 136 µg\*h/mL. The drug's ability to rapidly penetrate into cells ensures quick onset of action.
Half-life:
The half-life of Volanesorsen is an important consideration for its dosing schedule: Volanesorsen has a half life of >2 weeks. This determines the duration of action and helps in formulating effective dosing regimens.
Protein Binding:
Volanesorsen exhibits a strong affinity for binding with plasma proteins: Volanesorsen is >98% bound to proteins in plasma. Though the exact proteins have not been identified. This property plays a key role in the drug's pharmacokinetics and distribution within the body.
Route of Elimination:
The elimination of Volanesorsen from the body primarily occurs through: Volanesorsen is predominantly eliminated in the urine, though <3% of a dose was recovered within 24 hours. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.
Volume of Distribution:
Volanesorsen is distributed throughout the body with a volume of distribution of: The volume of distribution at steady state is 330 L in patients with familial chylomicronemia. This metric indicates how extensively the drug permeates into body tissues.
Clearance:
The clearance rate of Volanesorsen is a critical factor in determining its safe and effective dosage: The exact rate of clearance of volanesorsen is unknown, however it is rapidly distributed to tissues and very slowly eliminated. It reflects the efficiency with which the drug is removed from the systemic circulation.
Pharmacodynamics:
Volanesorsen exerts its therapeutic effects through: Volanesorsen is an antisense oligonucleotide that prevents the translation of apoC-III. It has a long duration of action as it has a half life of >2 weeks. Patients should be counselled regarding the risk of thrombocytopenia, raised LDL-C levels, renal toxicity, hepatotoxicity, and immunogenicity. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.
Mechanism of Action:
Volanesorsen functions by: Volanesorsen is an antisense oligonucleotide that binds to apoC-III mRNA, leading to its degradation, and preventing translation of apoC-III protein. Normally, apoC-III would inhibit triglyceride metabolism and hepatic clearance of chylomicrons. Preventing translation of apoC-III allows for metabolism and breakdown of these triglycerides and chylomicrons. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.
Toxicity:
Categories:
Volanesorsen is categorized under the following therapeutic classes: Carbohydrates, Glycosides, Lipid Modifying Agents, Lipid Modifying Agents, Plain, Nucleic Acids, Nucleotides, and Nucleosides, Nucleotides, Polynucleotides. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.
Experimental Properties:
Further physical and chemical characteristics of Volanesorsen include:
- Molecular Formula: C230H320N63O125P19S19
Volanesorsen is a type of Lipid-lowering agents
Lipid-lowering agents are a category of pharmaceutical active ingredients (APIs) that are widely used in the treatment of hyperlipidemia, a condition characterized by elevated levels of lipids (such as cholesterol and triglycerides) in the blood. These agents play a crucial role in managing lipid abnormalities and reducing the risk of cardiovascular diseases.
One of the most commonly prescribed lipid-lowering agents is statins. Statins work by inhibiting an enzyme called HMG-CoA reductase, which is responsible for the production of cholesterol in the liver. By blocking this enzyme, statins effectively lower cholesterol levels in the bloodstream.
Another class of lipid-lowering agents is fibric acid derivatives, which primarily target triglyceride levels. These agents activate a nuclear receptor known as PPAR-alpha, which regulates lipid metabolism. By activating PPAR-alpha, fibric acid derivatives enhance the breakdown of triglycerides and increase the elimination of fatty acids from the bloodstream.
Additionally, bile acid sequestrants are often used as lipid-lowering agents. These agents bind to bile acids in the intestine, preventing their reabsorption. As a result, the liver utilizes more cholesterol to produce new bile acids, leading to a decrease in circulating cholesterol levels.
Lipid-lowering agents are available in various formulations, including tablets, capsules, and suspensions, allowing for convenient administration. They are usually prescribed alongside lifestyle modifications, such as dietary changes and regular exercise, to optimize the management of hyperlipidemia.
It is important to note that the use of lipid-lowering agents should be under the supervision of a healthcare professional, as they may have potential side effects and interactions with other medications. Proper monitoring of lipid levels and regular follow-up visits are essential for ensuring the effectiveness and safety of these pharmaceutical agents.
