Bicisate API Manufacturers

compare suppliers & get competitive offers

teaser-1024x654-1
No suppliers found
Sorry, there are currently no suppliers listed for this ingredient. Hopefully we can help you with other ingredients.
Notify me!
Want to be the first to find out when a supplier for Bicisate is listed?

Join our notification list by following this page.

List your company
Are you a supplier of Bicisate or other APIs and are you looking to list your company on Pharmaoffer?

Click the button below to find out more

Find CDMO
Looking for a CDMO/CMO that can help you with your pharmaceutical needs?

Click the button below to switch over to the contract services area of Pharmaoffer.

Looking for Bicisate API 121251-02-3?

Description:
Here you will find a list of producers, manufacturers and distributors of Bicisate. 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:
Bicisate 
Synonyms:
 
Cas Number:
121251-02-3 
DrugBank number:
DB11164 
Unique Ingredient Identifier:
3JXF0Z0XOI

General Description:

Bicisate, identified by CAS number 121251-02-3, is a notable compound with significant therapeutic applications. Bicisate, also known as ethyl cysteinate dimer (ECD), is a N,N'-1,2-ethylene-di-yl-bis-L-cysteinate diethyl ester. It is used in conjunction with technetium Tc99m as a tracer to measure cerebral blood flow with single-photon emission computed tomography (SPECT). The complex of bicisate and technetium Tc99m as a kit was developed by Lantheus Medcl and FDA-approved on November 23, 1994.

Indications:

This drug is primarily indicated for: Bicisate as a complex with technetium Tc-99m is used in single photon emission computerized tomography (SPECT) as an adjunct to conventional CT or MRI in the localization of stroke in patients whom the presence of a stroke has already been diagnosed. It is not indicated to assess the functional viability of brain tissue or to distinguish between a stroke and other brain lesions. A stroke is defined as a condition in which the blood stops flowing to any part of the brain causing a damage to brain cells. The potential effect of a stroke depends on the part of the brain that was affected by it as well as the extension of the damage. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Bicisate undergoes metabolic processing primarily in: Bicisate is metabolized to form mono- and di-acids by the action of esterases. The exact metabolic transformation has not been elucidated. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Bicisate are crucial for its therapeutic efficacy: After intravenous administration, bicisate presents a very large brain extraction. About 5% of the administered dose remains in the blood one hour after administration. The highest concentration of radioactivity in blood was attained 0.5 minutes after intravenous injection and it represented 13.9% of the injected dose. After intravenous administration of bicisate, the permeability surface area was 0.48 ml.g/min. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Bicisate is an important consideration for its dosing schedule: The stability of bicisate is superior when compared to other brain radiopharmaceuticals. Thus, the reported half-life of bicisate is of 6.02 hours. When broadly studied in clinical trials, the pharmacokinetic profile fits a three-compartment model with half-lives of 43 seconds, 49.5 minutes and 533 minutes. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Bicisate exhibits a strong affinity for binding with plasma proteins: Bicisate and its major metabolites are not protein-bound. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Bicisate from the body primarily occurs through: Bicisate is primarily excreted by the kidneys. It has been reported that 50% of the dose is excreted in urine two hours after initial administration and even 74% of the administered dose is excreted in urine after 24 hours. Fecal excretion just accounts for 12.5% of the administered dose 48 hours after initial administration. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Bicisate is distributed throughout the body with a volume of distribution of: After intravenous administration of bicisate, the distribution volume was 0.74 L. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Bicisate is a critical factor in determining its safe and effective dosage: The clearance of bicisate from 1 to 24 hours, studied as a loss of hydrophilic tracer, is of approximate 3.5% per hour. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Bicisate exerts its therapeutic effects through: The neutral and lipophilic nature of bicisate provides it with high stability. This property is given by its N2S2 core. This characteristic has been proven to allow bicisate to be used even several hours after preparation and to present an easy passage through the blood-brain barrier. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Bicisate functions by: Bicisate is rapidly uptaken by the brain. The retention of bicisate in the brain is associated with stereospecific de-esterification to hydrophilic acid derivatives. Even though both DD and LL isomers demonstrate brain uptake, only the LL presents brain retention. Bicisate brain localization is performed by passive diffusion and the presence of slow hydrolysis in the blood and rapid hydrolysis in the brain. The hydrolysis of bicisate forms the monoacid and diacid bicisate derivatives. The formation of these derivatives results in high brain uptake and retention. The uptake of bicisate depends on the blood flow directed to the brain and thus the presence of a stroke will be translated into specific zones in the brain that would not include the complex of bicisate and technetium Tc-99m. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Bicisate belongs to the class of organic compounds known as alpha amino acid esters. These are ester derivatives of alpha amino acids, classified under the direct parent group Alpha amino acid esters. This compound is a part of the Organic compounds, falling under the Organic acids and derivatives superclass, and categorized within the Carboxylic acids and derivatives class, specifically within the Amino acids, peptides, and analogues subclass.

Categories:

Bicisate is categorized under the following therapeutic classes: Diagnostic Agents, Drugs that are Mainly Renally Excreted, Radioactive Diagnostic Agent. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.

Experimental Properties:

Further physical and chemical characteristics of Bicisate include:

  • Water Solubility: Insoluble
  • Melting Point: 196-198ºC

Bicisate is a type of Other substances


The pharmaceutical industry encompasses a diverse range of active pharmaceutical ingredients (APIs) that are used in the production of various medications. One category of APIs is known as other substances. This category includes substances that do not fall under the conventional classifications such as antibiotics, analgesics, or antihypertensives.

Other substances in pharmaceutical APIs consist of a broad array of chemical compounds with unique properties and applications. These substances play a crucial role in the formulation and development of specialized medications, catering to specific therapeutic needs. The category encompasses various substances like excipients, solvents, stabilizers, and pH adjusters.

Excipients are inert substances that aid in the manufacturing process and enhance the stability, bioavailability, and patient acceptability of pharmaceutical formulations. Solvents are used to dissolve other ingredients and facilitate their incorporation into the final product. Stabilizers ensure the integrity and shelf life of medications by preventing degradation or chemical changes. pH adjusters help maintain the desired pH level of a formulation, which can influence the drug's efficacy and stability.

Pharmaceutical manufacturers carefully select and incorporate specific other substances into their formulations, adhering to regulatory guidelines and quality standards. These substances undergo rigorous testing and evaluation to ensure their safety, efficacy, and compatibility with the desired pharmaceutical product. By employing other substances in API formulations, pharmaceutical companies can optimize drug delivery, improve patient compliance, and enhance therapeutic outcomes.

In summary, the other substances category of pharmaceutical APIs comprises a diverse range of chemicals, including excipients, solvents, stabilizers, and pH adjusters. These substances contribute to the formulation, stability, and performance of medications, enabling pharmaceutical manufacturers to develop specialized products that meet specific therapeutic requirements.