Investigational Drug Details
| Drug ID: | D203 |
| Drug Name: | Tamsulosin |
| Synonyms: | |
| Type: | small molecule |
| DrugBank ID: | DB00706 |
| DrugBank Description: | Tamsulosin is a selective alpha-1A and alpha-1B adrenoceptor antagonist that exerts its greatest effect in the prostate and bladder, where these receptors are most common.[Label] It is indicated for the treatment of signs and symptoms of benign prostatic hypertrophy.[Label] Antagonism of these receptors leads to relaxation of smooth muscle in the prostate and detrusor muscles in the bladder, allowing for better urinary flow.[Label] Other alpha-1 adrenoceptor antagonists developed in the 1980s were less selective and more likely to act on the smooth muscle of blood vessels, resulting in hypotension.[A178351] Tamsulosin was first approved by the FDA on April 15, 1997.[L6238] |
| PubChem ID: | 129211 |
| CasNo: | 106133-20-4 |
| Repositioning for NAFLD: | Yes |
| SMILES: | CCOC1=CC=CC=C1OCCN[C@H](C)CC1=CC(=C(OC)C=C1)S(N)(=O)=O |
| Structure: |
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| InChiKey: | DRHKJLXJIQTDTD-OAHLLOKOSA-N |
| Molecular Weight: | 408.512 |
| DrugBank Targets: | Alpha-1A adrenergic receptor; Alpha-1D adrenergic receptor; Alpha-1B adrenergic receptor |
| DrugBank MoA: | Tamsulosin is a blocker of alpha-1A and alpha-1D adrenoceptors.[Label,A1078] About 70% of the alpha-1 adrenoceptors in the prostate are of the alpha-1A subtype.[Label] By blocking these adrenoceptors, smooth muscle in the prostate is relaxed and urinary flow is improved.[Label] The blocking of alpha-1D adrenoceptors relaxes the detrusor muscles of the bladder which prevents storage symptoms.[A1078] The specificity of tamsulosin focuses the effects to the target area while minimizing effects in other areas.[Label] |
| DrugBank Pharmacology: | Tamsulosin is an alpha adrenoceptor blocker with specificity for the alpha-1A and alpha-1D subtypes, which are more common in the prostate and submaxillary tissue.[A1078] The final subtype, alpha-1B, are most common in the aorta and spleen.[A1078] Tamsulosin binds to alpha-1A receptors 3.9-38 times more selectively than alpha-1B and 3-20 times more selectively than alpha-1D.[A1078] This selectivity allows for a significant effect on urinary flow with a reduced incidence of adverse reactions like orthostatic hypotension.[A1078] |
| DrugBank Indication: | Tamsulosin is indicated for the treatment of signs and symptoms of benign prostatic hyperplasia.[Label] Tamsulosin is also used off label for the treatment of ureteral stones, prostatitis, and female voiding dysfunction.[A178339,L6259] |
| Targets: | |
| Therapeutic Category: | |
| Clinical Trial Progress: | |
| Latest Progress: |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L3111 | NCT01088165 | PHASE4 | UNKNOWN | NO | 2010-05 | 2012-01-20 | Details |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
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| Article ID | PMID | Source | Title |
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