Repositioning Candidate Details
| Candidate ID: | R0112 |
| Source ID: | DB00402 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Eszopiclone |
| Synonyms: | |
| Molecular Formula: | C17H17ClN6O3 |
| SMILES: | CN1CCN(CC1)C(=O)O[C@@H]1N(C(=O)C2=NC=CN=C12)C1=NC=C(Cl)C=C1 |
| Structure: |
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| DrugBank Description: | Eszopiclone, marketed by Sepracor under the brand-name Lunesta, is a nonbenzodiazepine hypnotic drug used to treat insomnia. It is the active stereoisomer of zopiclone, belonging to the class of drugs known as _cyclopyrrolones_.[A179638,L6850] Cyclopyrrolone drugs demonstrate high efficacy and low toxicity[A179827], offering a safer alternative to other drugs used for insomnia. One major benefit of eszopiclone is that it is approved by the FDA for the long-term treatment of insomnia. This sets it apart from many other hypnotic sedatives, which are generally approved only for the relief of short-term (6-8 weeks) insomnia. Eszopiclone was initially approved by the FDA in 2004.[L6769] |
| CAS Number: | 138729-47-2 |
| Molecular Weight: | 388.808 |
| DrugBank Indication: | Eszopiclone is indicated for the treatment of insomnia.[L6769] |
| DrugBank Pharmacology: | Eszopiclone rapidly induces sleep and decreases sleep latency. It also aids in the maintenance of sleep, preventing frequent awakenings.[A179659,A179662,L6769] This drug has shown anticonvulsant and muscle relaxant properties in animals but is used in humans for its sedating effects.[A179827] Eszopiclone is a central nervous system depressant with various effects. These include changes in alertness and motor coordination and the risk of next morning impairment, increasing with the amount of eszopiclone administered. Exercise caution and advise against driving a motor vehicle or activities that require full mental alertness the next morning.[L6769] Complex sleep behaviors may result from eszopiclone use. Eszopiclone should be discontinued in these cases.[L6874] Avoid the use of alcohol and other CNS depressants when eszopiclone is administered. Advise patients to skip the eszopiclone dose if alcohol has been consumed before bed or during the evening. Use the smallest dose of eszopiclone as possible, especially in elderly patients, who may experience exaggerated drug effects. Though the potential for dependence and abuse with eszopiclone is lower than for other hypnotic drugs, this drug has been abused and is known to cause dependence.[L6868] |
| DrugBank MoA: | The exact mechanism of action of eszopiclone is unknown at this time but is thought to occur via binding with the GABA receptor complexes at binding sites located near benzodiazepine receptors, possibly explaining its hypnotic and sedative effects.[A179659,L6769] It has particular affinity for GABA-A (or GABAA) receptor subunits 1, 3 and 5.[A179788,A15625,A15626] Eszopiclone increases GABA-A channel currents significantly.[A179788] GABA-A channels are major inhibitory channels that cause CNS depression when their receptors are activated.[A179800] |
| Targets: | Gamma-aminobutyric acid receptor subunit alpha-1; GABA-A receptor (anion channel); Gamma-aminobutyric acid receptor subunit alpha-2; Gamma-aminobutyric acid receptor subunit alpha-3; Gamma-aminobutyric acid receptor subunit alpha-5 |
| Inclusion Criteria: |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
|---|
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name | |
|---|---|---|---|---|---|---|---|
| T03 | Angiotensin-converting enzyme | ACE | INHIBITOR | Target is a single protein chain | P12821 | ACE_HUMAN | Details |
| T06 | Sulfonylurea receptor 1 | ABCC8 | Target is a single protein chain | Q09428 | ABCC8_HUMAN | Details | |
| T13 | Renin | REN | INHIBITOR | Target is a single protein chain | P00797 | REN_HUMAN | Details |
| T47 | Sialin | SLC17A5 | Target is a single protein chain | Q9NRA2 | SLC17A5_HUMAN | Details | |
| T15 | Steryl-sulfatase | STS | INHIBITOR | Hydrolase | P08842 | STS_HUMAN | Details |
| Diseases ID | DO ID | Disease Name | Definition | Class | |
|---|---|---|---|---|---|
| I02 | 1184 | nephrotic syndrome | "A nephrosis characterized by marked increase in glomerular protein permeability resulting in marked elevation of urine protein levels, hypoalbuminemia, hyperlipidemia, and hypercoagulability." [url:https\://en.wikipedia.org/wiki/Nephrotic_syndrome, url:https\://www.niddk.nih.gov/health-information/kidney-disease/nephrotic-syndrome-adults] | Details |