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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