Repositioning Candidate Details
| Candidate ID: | R1346 |
| Source ID: | DB11164 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Bicisate |
| Synonyms: | -- |
| Molecular Formula: | C12H24N2O4S2 |
| SMILES: | CCOC(=O)[C@H](CS)NCCN[C@@H](CS)C(=O)OCC |
| Structure: |
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| DrugBank Description: | 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. |
| CAS Number: | 121251-02-3 |
| Molecular Weight: | 324.45 |
| DrugBank Indication: | 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. |
| DrugBank Pharmacology: | 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. |
| DrugBank MoA: | 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. |
| Targets: | -- |
| Inclusion Criteria: | Indication associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
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| Diseases ID | DO ID | Disease Name | Definition | Class | |
|---|---|---|---|---|---|
| I16 | 6713 | Cerebrovascular disease | An vascular disease that is characterized by dysfunction of the blood vessels supplying the brain. http://en.wikipedia.org/wiki/Cerebrovascular_disease, http://www.ncbi.nlm.nih.gov/books/NBK378/ | disease of anatomical entity/ cardiovascular system disease/ vascular disease/cerebrovascular disease | Details |