Repositioning Candidate Details
| Candidate ID: | R0343 |
| Source ID: | DB00950 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Fexofenadine |
| Synonyms: | 4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)-1-piperidinyl)butyl)-alpha,alpha-dimethylbenzeneacetic acid; Carboxyterfenadine; Fexofenadine; Terfenadine acid metabolite; Terfenadine carboxylate; Terfenadine-COOH |
| Molecular Formula: | C32H39NO4 |
| SMILES: | CC(C)(C(O)=O)C1=CC=C(C=C1)C(O)CCCN1CCC(CC1)C(O)(C1=CC=CC=C1)C1=CC=CC=C1 |
| Structure: |
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| DrugBank Description: | Fexofenadine is an over-the-counter second-generation antihistamine used in the treatment of various allergic symptoms. It is selective for the H<sub>1</sub> receptor, carries little-to-no activity at off-targets, and does not cross the blood-brain barrier - this is in contrast to previous first-generation antihistamines, such as , which readily bind to off-targets that contribute to side effects such as sedation. Fexofenadine is the major active metabolite of and is administered as a racemic mixture in which both enantiomers display approximately equivalent antihistamine activity. |
| CAS Number: | 83799-24-0 |
| Molecular Weight: | 501.6564 |
| DrugBank Indication: | In the United States, fexofenadine is indicated for the symptomatic treatment of allergic rhinitis in patients ≥2 years old and chronic idiopathic urticaria in patients ≥6 months old. In Canada, fexofenadine carries the same indications but is approved only for patients ≥12 years old. Fexofenadine is also available in combination with for the symptomatic treatment of season allergic rhinitis in patients ≥12 years old. |
| DrugBank Pharmacology: | Fexofenadine relieves allergy symptoms by antagonizing the actions of histamine, an endogenous compound predominantly responsible for allergic symptomatology. The relatively long duration of action of fexofenadine (approximately 24 hours) allows for once or twice daily dosing, and its rapid absorption allows for an onset of action within 1-3 hours. Fexofenadine should not be taken with fruit juice, as this may impair its absorption. |
| DrugBank MoA: | The H<sub>1</sub> histamine receptor is responsible for mediating hypersensitivity and allergic reactions. Exposure to an allergen results in degranulation of mast cells and basophils, which then release histamine and other inflammatory mediators. Histamine binds to, and activates, H<sub>1</sub> receptors, which results in the further release of pro-inflammatory cytokines, such as interleukins, from basophils and mast cells. These downstream effects of histamine binding are responsible for a wide variety of allergic symptoms, such as pruritus, rhinorrhea, and watery eyes. Fexofenadine is considered an “inverse agonist” of the H<sub>1</sub> receptor because it binds to and stabilizes the inactive form of the receptor, preventing its activation and subsequent downstream effects. It has a potent and selective affinity for H<sub>1</sub> receptors, and there is no evidence that it carries antidopaminergic, antiserotonergic, anticholinergic, sedative, or adrenergic blocking activity. Fexofenadine does not cross the blood-brain barrier and thus is unlikely to cause significant CNS effects. |
| Targets: | Histamine H1 receptor 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 |
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