Repositioning Candidate Details
| Candidate ID: | R0325 |
| Source ID: | DB00885 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Pemirolast |
| Synonyms: | -- |
| Molecular Formula: | C10H8N6O |
| SMILES: | CC1=CC=CN2C(=O)C(=CN=C12)C1=NNN=N1 |
| Structure: |
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| DrugBank Description: | Pemirolast potassium is a slightly yellow powder that is soluble in water. It is a mast cell stabilizer that acts as an antiallergic agent. As an ophthalmic aqueous sterile solution, pemirolast is used for the prevention of itching of the eyes caused by allergies such as hay fever, and allergic conjunctivitis. Pemirolast is potentially useful for prophylaxis of pulmonary hypersensitivity reactions to drugs such as paclitaxel. |
| CAS Number: | 69372-19-6 |
| Molecular Weight: | 228.2101 |
| DrugBank Indication: | For the prevention of itching of the eyes caused by allergies such as hay fever, and allergic conjunctivitis |
| DrugBank Pharmacology: | Pemirolast is used for the prophylactic treatment of itching of the eye associated with allergic conjunctivitis. Pemirolast potassium is a mast cell stabilizer that inhibits the <i>in vivo</i> Type I immediate hypersensitivity reaction. Pemirolast inhibits the antigen-induced release of inflammatory mediators (e.g., histamine, leukotriene C4, D4, E4) from human mast cells. Allergic reactions lead to cell-degranulation and the release of histamine (and other chemical mediators) from the mast cell or basophil. Once released, histamine can react with local or widespread tissues through histamine receptors. Histamine, acting on H<sub>1</sub>-receptors, produces pruritis and vasodilatation (allowing blood fluids to enter the area to cause swelling). Pemirolast is a histamine H1 antagonist. It competes with histamine for the normal H<sub>1</sub>-receptor sites on effector cells of blood vessels to provide effective, temporary relief of watery and itchy eyes. |
| DrugBank MoA: | Pemirolast binds to the histamine H<sub>1</sub> receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. Pemirolast has also been observed to inhibit antigen-stimulated calcium ion influx into mast cells through the blockage of calcium channels. Pemirolast inhibits the chemotaxis of eosinophils into ocular tissue, and prevents inflammatory mediator release from human eosinophils. |
| Targets: | -- |
| 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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