Repositioning Candidate Details
| Candidate ID: | R0093 |
| Source ID: | DB00341 |
| Source Type: | approved |
| Compound Type: | small molecule |
| Compound Name: | Cetirizine |
| Synonyms: | |
| Molecular Formula: | C21H25ClN2O3 |
| SMILES: | OC(=O)COCCN1CCN(CC1)C(C1=CC=CC=C1)C1=CC=C(Cl)C=C1 |
| Structure: |
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| DrugBank Description: | Cetirizine, also commonly known as _Zyrtec_, is an orally active second-generation histamine H1 antagonist proven effective in the treatment of various allergic symptoms, such as sneezing, coughing, nasal congestion, hives, and other symptoms [A175051], [A175054]. One of the most common uses for this drug is for a condition called _allergic rhinitis_. The prevalence of allergic rhinitis in the United States is about 15% according to physician diagnoses, and up to 30%, according to self-reported nasal symptoms. Allergic rhinitis is associated with multiple missed or unproductive days at work and school, problems with sleep, and other difficulties with day to day activities for many individuals [A175057]. Furthermore, some antihistamine agents that are used to treat this condition cause undesirable, sedating effects [A175060]. Cetirizine is one of the first second-generation H1 antihistamines (SGAHs)formulated to selectively inhibit the H1 receptor without sedating effects [A175054]. |
| CAS Number: | 83881-51-0 |
| Molecular Weight: | 388.888 |
| DrugBank Indication: | **Seasonal Allergic Rhinitis**: Indicated for the relief of symptoms associated with seasonal allergic rhinitis caused by allergens such as ragweed, grass and tree pollens in adults and children 2 years of age and above. Symptoms treated effectively include sneezing, rhinorrhea, nasal pruritus, ocular pruritus, tearing, and redness of the eyes [FDA label]. **Perennial allergic rhinitis**: This drug is indicated for the relief of symptoms associated with perennial allergic rhinitis due to allergens including dust mites, animal dander, and molds in adults and children 6 months of age and older. Symptoms treated effectively include sneezing, rhinorrhea, postnasal discharge, nasal pruritus, ocular pruritus, and tearing [FDA label]. **Chronic urticaria**: Cetirizine is indicated for the treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria in adults and children 6 months of age and older. It markedly reduces the occurrence, severity, and duration of hives and significantly reduces pruritus [FDA label]. |
| DrugBank Pharmacology: | **General effects and respiratory effects** Cetirizine, the active metabolite of the piperazine H<sub>1</sub>-receptor antagonist hydroxyzine, minimizes or eliminates the symptoms of chronic idiopathic urticaria, perennial allergic rhinitis, seasonal allergic rhinitis, allergic asthma, physical urticaria, and atopic dermatitis. The clinical efficacy of cetirizine for allergic respiratory diseases has been well established in numerous trials [FDA label]. **Effects on urticaria/anti-inflammatory effects** It has anti-inflammatory properties that may play a role in asthma management [A175051]. There is evidence that cetirizine improves symptoms of urticaria. Marked clinical inhibition of a wheal and flare response occurs in infants, children as well as adults within 20 minutes of one oral dose and lasts for 24 h [A175051]. Concomitant use of cetirizine reduces the duration and dose of topical anti-inflammatory formulas used for the treatment of atopic dermatitis [A175051]. |
| DrugBank MoA: | Cetirizine, a metabolite of _hydroxyzine_, is an antihistamine drug. Its main effects are achieved through selective inhibition of peripheral H1 receptors. The antihistamine activity of cetirizine has been shown in a variety of animal and human models. _In vivo_ and _ex vivo_ animal models have shown insignificant anticholinergic and antiserotonergic effects. In clinical studies, however, dry mouth was found to be more frequent with cetirizine than with a placebo. In vitro receptor binding studies have demonstrated no detectable affinity of cetirizine for histamine receptors other than the H1 receptors. Studies with radiolabeled cetirizine administration in the rat have demonstrated insignificant penetration into the brain. _Ex vivo_ studies in the mouse have shown that systemically administered cetirizine does not occupy cerebral H1 receptors significantly [FDA label]. |
| Targets: | Histamine H1 receptor |
| 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 | |
| T47 | Sialin | SLC17A5 | Target is a single protein chain | Q9NRA2 | SLC17A5_HUMAN | Details | |
| T15 | Steryl-sulfatase | STS | INHIBITOR | Hydrolase | P08842 | STS_HUMAN | Details |
| T49 | Apolipoprotein L1 | APOL1 | Target is a single protein chain | O14791 | APOL1_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 | |
| I05 | 784 | chronic kidney disease | "A kidney failure that is characterized by the gradual loss of kidney function." [url:https\://www.mayoclinic.org/diseases-conditions/chronic-kidney-disease/symptoms-causes/syc-20354521, url:https\://www.ncbi.nlm.nih.gov/books/NBK499861/] | Details |