Repositioning Candidate Details
| Candidate ID: | R0265 |
| Source ID: | DB00751 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Epinastine |
| Synonyms: | (±)-epinastine; 3-amino-9,13b-dihydro-1H-dibenz(c,f)imidazo(1,5-a)azepine; Epinastine |
| Molecular Formula: | C16H15N3 |
| SMILES: | NC1=NCC2N1C1=CC=CC=C1CC1=CC=CC=C21 |
| Structure: |
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| DrugBank Description: | Epinastine is used for the prevention of itching associated with allergic conjunctivitis. It has a multi-action effect that inhibits the allergic response in 3 ways: 1. stabilizes mast cells by preventing mast cell degranulation to control the allergic response, 2. prevents histamine binding to both the H1- and H2-receptors to stop itching and provide lasting protection, and 3. prevents the release of proinflammatory chemical mediators from the blood vessel to halt progression of the allergic response. |
| CAS Number: | 80012-43-7 |
| Molecular Weight: | 249.3104 |
| DrugBank Indication: | For the prevention of itching associated with allergic conjunctivitis. |
| DrugBank Pharmacology: | Epinastine is an antihistamine and an inhibitor of histamine release from the mast cell for topical administration to the eyes. Epinastine is indicated for the prevention of itching associated with allergic conjunctivitis. Epinastine is a topically active, direct H<sub>1</sub>-receptor antagonist and an inhibitor of the release of histamine from the mast cell. Epinastine is selective for the histamine H<sub>1</sub>-receptor and has affinity for the histamine H2 receptor. Epinastine also possesses affinity for the a1-, a2-, and 5-HT<sub>2</sub> -receptors. Epinastine does not penetrate the blood/brain barrier and, therefore, is not expected to induce side effects of the central nervous system. |
| DrugBank MoA: | Epinastine has a multiaction effect that inhibits the allergic response in 3 ways: 1. stabilizes mast cells by preventing mast cell degranulation to control the allergic response, 2. prevents histamine binding to both the H1- and H<sub>2</sub>-receptors to stop itching and provide lasting protection, and 3. prevents the release of proinflammatory chemical mediators from the blood vessel to halt progression of the allergic response. |
| Targets: | Histamine H1 receptor antagonist; Histamine H2 receptor antagonist; Alpha-1A adrenergic receptor unknown; Alpha-2A adrenergic receptor unknown; 5-hydroxytryptamine receptor 2A antagonist; 5-hydroxytryptamine receptor 7 antagonist |
| Inclusion Criteria: | Therapeutic strategy associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
|---|---|---|---|---|---|
| S05 | Anti-inflammatory | inflammatory | Bile acid; TNF-a inhibitor; Dual PPAR-α and -δ agonists; Toll-Like Receptor; (TLR)-4 antagonist; Caspase inhibitor; ASK-1 inhibitor | Ursodeoxycholic Acid; Pentoxifylline; Elafibranor; JKB-121; Emricasan; Selonsertib; | Details |
| Diseases ID | DO ID | Disease Name | Definition | Class |
|---|