Repositioning Candidate Details
| Candidate ID: | R0639 |
| Source ID: | DB04885 |
| Source Type: | investigational |
| Compound Type: | small molecule |
| Compound Name: | Cilansetron |
| Synonyms: | Cilansetron |
| Molecular Formula: | C20H21N3O |
| SMILES: | CC1=NC=CN1C[C@H]1CCC2=C(C3=CC=CC4=C3N2CCC4)C1=O |
| Structure: |
|
| DrugBank Description: | Cilansetron is a 5HT-3 antagonist made by Solvay Pharmaceuticals that is currently under trial phase in the EU and US. |
| CAS Number: | 120635-74-7 |
| Molecular Weight: | 319.4002 |
| DrugBank Indication: | For the treatment of symptoms associated with irritable bowel syndrome. |
| DrugBank Pharmacology: | Cilansetron is an orally formulated medication that blocks the action of 5-hydroxy-tryptamine 3 (5-HT3) receptors. Phase III studies of cilansetron had been suspended by Solvay in order to assess whether the drug possesses safety concerns similar to alosetron. Alosetron, also a 5-HT3 antagonist, was withdrawn from the market due to questions regarding its safety. Phase III testing with cilansetron has since resumed. In June 2005 the company announced that they were reviewing the priority of the cilansetron program. |
| DrugBank MoA: | Cilansetron is a potent and selective 5-HT<sub>3</sub> receptor antagonist. 5-HT<sub>3</sub> receptors are nonselective cation channels that are extensively distributed on enteric neurons in the human gastrointestinal tract, as well as other peripheral and central locations. Activation of these channels and the resulting neuronal depolarization affect the regulation of visceral pain, colonic transit and gastrointestinal secretions, processes that relate to the pathophysiology of irritable bowel syndrome (IBS). 5-HT<sub>3</sub> receptor antagonists such as cilansetron inhibit activation of non-selective cation channels which results in the modulation of the enteric nervous system. |
| Targets: | 5-hydroxytryptamine receptor 3A |
| Inclusion Criteria: | Indication associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
|---|
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
|---|