Tamsulosin

Summary

Tamsulosin (CHEMBL836) is an approved small-molecule α-adrenergic antagonist (ATC G04CA02) targeting ADRA1A, ADRA1B, and ADRA1D; indicated across 11 conditions including benign prostatic hyperplasia and hyperplasia.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: G04CA02
• Targets: 3 (ADRA1A, ADRA1B, ADRA1D)
• Indications: 11 conditions
• Clinical trials: 152
• Chemistry: 408.5 Da · C20H28N2O5S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL836
Name	Tamsulosin
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	129211
ChEBI	CHEBI:9398
ATC	G04CA02
Molecular formula	C20H28N2O5S
Molecular weight	408.5
InChIKey	DRHKJLXJIQTDTD-OAHLLOKOSA-N

SMILES: CCOC1=CC=CC=C1OCCN[C@H](C)CC2=CC(=C(C=C2)OC)S(=O)(=O)N

IUPAC name: 5-[(2R)-2-[2-(2-ethoxyphenoxy)ethylamino]propyl]-2-methoxybenzenesulfonamide

ChEBI definition: A 5-(2-{[2-(2-ethoxyphenoxy)ethyl]amino}propyl)-2-methoxybenzenesulfonamide that has (R)-configuration. A specific α1 adrenoceptor antagonist used (generally as its hydrochloride salt, tamsulosin hydrochloride) in the treatment of prostatic hyperplasia, chronic prostatitis, urinary retention, and help with the passage of kidney stones.

Pharmacological roles (ChEBI): α-adrenergic antagonist, antineoplastic agent.

Also known as: HGP-0412, HIP-1402, HIP1402, Tamsulon, Tamsulosin, Tamsulosina, Tamsulosine, tamsulosin, SID50112696, TAMSULOSIN, Tamsulosin_HCL

Parent form; salt/anhydrous children: CHEMBL1200914

Patent coverage: 4,247 distinct patent families (14,566 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 14,363 (99%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
ADRA1A	α1A-adrenoceptor	Antagonist	10.7		P35348
ADRA1B	α1B-adrenoceptor	Inverse agonist	9.7	0%	P35368
ADRA1D	α1D-adrenoceptor	Antagonist	10.2	0.2%	P25100

Broader ChEMBL bioactivity targets: 26 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Alpha-2C adrenergic receptor, Alpha-2B adrenergic receptor, Adrenergic receptor alpha-1, Serotonin 1 (5-HT1) receptor, Beta-2 adrenergic receptor, Alpha-1 adrenergic receptor, Beta-1 adrenergic receptor, 5-hydroxytryptamine receptor 1A.

Bioactivity

ChEMBL activities: 81 potent at pChembl ≥ 5 of 82 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P23944	10.6	Kd	0.03	nM	CHEMBL_ACT_34233
ADRA1A	10.54	Ki	0.03	nM	CHEMBL_ACT_34224
P43140	10.52	Ki	0.03	nM	CHEMBL_ACT_841486
ADRA1D	10.4	Kd	0.04	nM	CHEMBL_ACT_1219213
ADRA1A	10.3	Ki	0.05	nM	CHEMBL_ACT_5098718
ADRA1D	10.24	Ki	0.06	nM	CHEMBL_ACT_34226
ADRA1A	10.15	EC50	0.07	nM	CHEMBL_ACT_16764856
P23944	10.15	Ki	0.07	nM	CHEMBL_ACT_841488
ADRA1D	10	Ki	0.1	nM	CHEMBL_ACT_5098706
P18130	9.9	Ki	0.13	nM	CHEMBL_ACT_1219212
P43140	9.89	Ki	0.13	nM	CHEMBL_ACT_12062949
ADRA1B	9.89	EC50	0.13	nM	CHEMBL_ACT_16764914
ADRA1A	9.89	Ki	0.13	nM	CHEMBL_ACT_689918
ADRA1A	9.89	Ki	0.13	nM	CHEMBL_ACT_689936
ADRA1D	9.82	IC50	0.15	nM	CHEMBL_ACT_22988544
O02824	9.8	Kd	0.16	nM	CHEMBL_ACT_1219214
ADRA1D	9.8	Ki	0.16	nM	CHEMBL_ACT_268557
ADRA1D	9.8	Kd	0.16	nM	CHEMBL_ACT_268558
ADRA1D	9.8	Ki	0.16	nM	CHEMBL_ACT_299389
ADRA1D	9.8	Kd	0.16	nM	CHEMBL_ACT_299393
ADRA1D	9.74	Ki	0.18	nM	CHEMBL_ACT_16576498
ADRA1D	9.74	Ki	0.18	nM	CHEMBL_ACT_689920
ADRA1A	9.72	Ki	0.19	nM	CHEMBL_ACT_1900452
ADRA1A	9.72	Ki	0.19	nM	CHEMBL_ACT_1962324
ADRA1A	9.72	Ki	0.19	nM	CHEMBL_ACT_2092304
ADRA1A	9.7	Ki	0.2	nM	CHEMBL_ACT_1431013
ADRA1D	9.7	Ki	0.2	nM	CHEMBL_ACT_1900515
ADRA1D	9.7	Ki	0.2	nM	CHEMBL_ACT_1962416
ADRA1D	9.7	Ki	0.2	nM	CHEMBL_ACT_2092306
ADRA1A	9.7	Ki	0.2	nM	CHEMBL_ACT_268555

Target pathways

Aggregated over 3 target gene(s): ADRA1A, ADRA1B, ADRA1D.

Top Reactome pathways

9 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	3	ADRA1A, ADRA1B, ADRA1D
Signaling by GPCR	3	ADRA1A, ADRA1B, ADRA1D
Class A/1 (Rhodopsin-like receptors)	3	ADRA1A, ADRA1B, ADRA1D
Amine ligand-binding receptors	3	ADRA1A, ADRA1B, ADRA1D
GPCR downstream signalling	3	ADRA1A, ADRA1B, ADRA1D
Adrenoceptors	3	ADRA1A, ADRA1B, ADRA1D
G alpha (q) signalling events	3	ADRA1A, ADRA1B, ADRA1D
G alpha (12/13) signalling events	3	ADRA1A, ADRA1B, ADRA1D
GPCR ligand binding	3	ADRA1A, ADRA1B, ADRA1D

Dominant GO biological processes

GO term	Targets
signal transduction	3
G protein-coupled receptor signaling pathway	3
phospholipase C-activating G protein-coupled receptor signaling pathway	3
positive regulation of cytosolic calcium ion concentration	3
cell-cell signaling	3
positive regulation of MAPK cascade	3
adenylate cyclase-activating adrenergic receptor signaling pathway	3
neuron-glial cell signaling	3
adrenergic receptor signaling pathway	3
positive regulation of cardiac muscle hypertrophy	2
intracellular signal transduction	2
positive regulation of vasoconstriction	2
regulation of muscle contraction	2
regulation of vasoconstriction	2
regulation of cardiac muscle contraction	2

Indications & clinical

Indications

11 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
benign prostatic hyperplasia	4	MONDO:0010811	EFO:0000284
hyperplasia	3	MONDO:0005043	EFO:0000536
ureterolithiasis	3	MONDO:0007009	EFO:1001228
nephrolithiasis	3	MONDO:0008171	EFO:0004253
urolithiasis	3	MONDO:0024647	MONDO:0024647
premature ejaculation	3	MONDO:0001780	EFO:0803321
urinary tract infection	3	MONDO:0100338	EFO:0003103
erectile dysfunction	1	MONDO:0005362	EFO:0004234

3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 152.

Phase distribution

Phase	Trials
PHASE4	47
PHASE3	33
Not specified	29
PHASE1	26
PHASE2	11
PHASE2/PHASE3	2
PHASE1/PHASE2	2
EARLY_PHASE1	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05551221	PHASE4	RECRUITING	The Efficacy and Safety of Silodosin Singly or Combined With Ningmitai Capsules in the Treatment of Benign Prostatic Hyperplasia
NCT07276919	PHASE4	NOT_YET_RECRUITING	Perioperative Tamsulosin for Treating Voiding Dysfunction Following Prostate Biopsy
NCT07308002	PHASE4	NOT_YET_RECRUITING	Intermittent vs Daily Tamsulosin for LUTS/BPH
NCT07310797	PHASE4	NOT_YET_RECRUITING	Comparison of Mirabegron and Tamsulosin for Ureteral Stone Expulsion
NCT07357324	PHASE4	RECRUITING	A Clinical Observation Study of a Chinese Patent Medicine Combined With Tamsulosin in Improving Sleep and Nocturia Symptoms After Enucleation of the Prostate
NCT07467343	PHASE4	NOT_YET_RECRUITING	Silodosin vs Tamsulosin for LUTS Due to BPH: A Randomized Crossover Trial
NCT00333112	PHASE4	COMPLETED	A Study to Evaluate Solifenacin Succinate in Combination With Tamsulosin for the Treatment of Residual Overactive Bladder Symptoms (OAB) in Men.
NCT00379067	PHASE4	COMPLETED	A Phase 4 Study With Tamsulosin OCAS to Assess Nighttime Voiding.
NCT00382265	PHASE4	COMPLETED	Tamsulosin for Urolithiasis in the Emergency Dept
NCT00451061	PHASE4	UNKNOWN	The Efficacy of Alpha-blockers for Expulsion of Distal Ureteral Stones
NCT00701779	PHASE4	COMPLETED	Dutasteride and Flex Dose of Tamsulosin on as Needed Basis, to Treat Benign Prostatic Hyperplasia
NCT01167062	PHASE4	UNKNOWN	Efficacy of Tamsulosin Oral-controlled Absorption System (OCAS) in the Treatment of Distal Ureteral Stones
NCT01294592	PHASE4	COMPLETED	Comparative Efficacy of Dutasteride Plus Tamulosin With Lifestyle Advice Versus Watchful Waiting Plus Lifestyle Advice in the Management of Treatment naïve Men With Moderately Symptomatic Benign Prostatic Hyperplasia and Prostate Enlargement
NCT01457573	PHASE4	COMPLETED	Pilot Trial Of Urinary Nerve Growth Factor (NGF) As Biomarker for Male Lower Urinary Tract Symptoms
NCT01673490	PHASE4	TERMINATED	Safety and Efficacy of 0.5mg Dutasteride and 0.4mg Tamsulosin Combination Once Daily for Six Months for Benign Prostatic Hyperplasia
NCT01736033	PHASE4	UNKNOWN	Advanced Benefits of Alpha-blocker Monotherapy on Lower Urinary Tracts Symptoms(LUTS) Patients
NCT01741454	PHASE4	COMPLETED	Treatment of Symptoms After Stent Placement for Urinary Tract Obstruction
NCT01880619	PHASE4	COMPLETED	Comparison of Tamsulosin and Solifenacin in Treatment of Ureteral Stent Symptoms
NCT02034604	PHASE4	COMPLETED	Efficacy and Safety of Naftopidil in Patient With Neurogenic Lower Urinary Tract Dysfunction Not Caused by Benign Prostatic Hyperplasia
NCT02095665	PHASE4	COMPLETED	Ureteral Stent-related Pain and Mirabegron (SPAM) Trial
NCT02180789	PHASE4	COMPLETED	A Study to Evaluate the Tolerability and Efficacy of Tamsulosin 0.4mg OCAS Formulation in Patients Who Are Unsatisfied With the Treatment of Tamsulosin 0.2mg Conventional Formulation
NCT02244229	PHASE4	COMPLETED	Study to Evaluate the Therapeutic Action of Tamsulosin and Finasteride in Symptomatic Benign Prostatic Hyperplasia (BPH) Patients
NCT02245490	PHASE4	COMPLETED	Study to Characterise the Effect of Tamsulosin on Lower Urinary Tract Symptoms (LUTS) and Detrusor Motor Activity in Patients Affected by Benign Prostatic Hyperplasia (BPH) and Storage Urinary Symptoms
NCT02279615	PHASE4	UNKNOWN	Efficacy And Safety Of Combination Therapy For Treatment Of Overactive Bladder In Male Patients With Benign Prostatic Hyperplasia.
NCT02369744	PHASE4	TERMINATED	Silodosin Versus Tamsulosin for Treatment of Ureteral Stones
NCT02443844	PHASE4	UNKNOWN	Comparison of Medical and Surgical Treatments of Benign Prostate Hyperplasia in Patients Who Have Low Grade Non Muscle Invasive Bladder Cancer for Tumour Recurrence and Progression
NCT02656173	PHASE4	COMPLETED	A Phase 4 Study to Evaluate the Efficacy, Safety, and Tolerability of Mirabegron in Male Subjects With Overactive Bladder (OAB) Symptoms, While Taking the Alpha Blocker for Benign Prostatic Hypertrophy (BPH)
NCT02715024	PHASE4	COMPLETED	Study to Evaluate the Clinical Efficacy and Safety of Tamsulosin Alone or in Combination With Solifenacin for the Treatment in Men With Lower Urinary Tract Symptoms Including Overactive Bladder Symptoms
NCT02919436	PHASE4	COMPLETED	Decreasing Rates of Intraurethral Catheterization Postoperatively in Spine Surgery
NCT02958878	PHASE4	COMPLETED	Preoperative Administration of Tamsulosin for Prevention of Post Operative Urinary Retention in Males Undergoing Elective Inguinal Hernia Repair
NCT03027115	PHASE4	UNKNOWN	Hernia Surgery Urinary Retention
NCT03144596	PHASE4	COMPLETED	The Effects of α-adrenergic Receptor Antagonists on Choroid and Pupil
NCT03614052	PHASE4	TERMINATED	Tamsulosin as Adjuvant Treatment Prior to Endoscopic Ureterolithotomy
NCT03750656	PHASE4	TERMINATED	Use of Hyoscyamine Versus Tamsulosin for Management of Ureteral Stent Irritation
NCT03808155	PHASE4	COMPLETED	Prevention of Postoperative Urinary Retention With Treatment of Tamsulosin 5 Days Prior to Lower Limb Arthroplasty
NCT03856242	PHASE4	COMPLETED	Benign Prostatic Hyperplasia and Ischemic Heart DIsease
NCT04107896	PHASE4	COMPLETED	Efficacy of Silodosin in the Treatment of Symptomatic Benign Prostatic Hyperplasia (BPH)
NCT04434378	PHASE4	TERMINATED	Tamsulosin to Prevent Postoperative Urinary Retention in Laparoscopic Inguinal Hernia Repair
NCT04682366	PHASE4	TERMINATED	The Effect of Tamsulosin on Postoperative Urinary Retention
NCT04819828	PHASE4	COMPLETED	Tamsulosin as Adjunctive Therapy After Extracorporeal Shock Wave Lithotripsy for Renal Stones

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 10 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

571 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
DIHYDROERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
ALFUZOSIN	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
AMLODIPINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
APRACLONIDINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
ASENAPINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
ATENOLOL	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
AZELASTINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
BREXPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
BRIMONIDINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
BUSPIRONE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
CARIPRAZINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
CISAPRIDE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
CLONIDINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
CLOZAPINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
DEXMEDETOMIDINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
DOPAMINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
DOXAZOSIN	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
EBASTINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
EPINEPHRINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
FENOLDOPAM	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
HALOPERIDOL	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
INDACATEROL	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
INDORAMIN	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
ISOPROTERENOL	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
LABETALOL	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
MOXISYLYTE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
NAFTOPIDIL	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
NEFAZODONE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
NOREPINEPHRINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
OLANZAPINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
OXYMETAZOLINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
PHENTOLAMINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
PRAZOSIN	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
QUETIAPINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
RISPERIDONE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
SERTINDOLE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
SILODOSIN	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
TEGASEROD	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
TERAZOSIN	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
TERFENADINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
TOLAZOLINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
VERAPAMIL	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
VILAZODONE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
XYLOMETAZOLINE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
ZIPRASIDONE	ChEMBL	Phase 4 (approved)	ADRA1A, ADRA1B, ADRA1D
BUNAZOSIN	ChEMBL	Phase 3	ADRA1A, ADRA1B, ADRA1D
IDAZOXAN	ChEMBL	Phase 3	ADRA1A, ADRA1B, ADRA1D
LATREPIRDINE	ChEMBL	Phase 3	ADRA1A, ADRA1B, ADRA1D
MEDETOMIDINE	ChEMBL	Phase 3	ADRA1A, ADRA1B, ADRA1D
YOHIMBINE	ChEMBL	Phase 3	ADRA1A, ADRA1B, ADRA1D
ABANOQUIL	ChEMBL	Phase 2	ADRA1A, ADRA1B, ADRA1D
CIRAZOLINE	ChEMBL	Phase 2	ADRA1A, ADRA1B, ADRA1D
DEXNIGULDIPINE	ChEMBL	Phase 2	ADRA1A, ADRA1B, ADRA1D
IPSAPIRONE	ChEMBL	Phase 2	ADRA1A, ADRA1B, ADRA1D
MAZAPERTINE	ChEMBL	Phase 2	ADRA1A, ADRA1B, ADRA1D
NIGULDIPINE	ChEMBL	Phase 2	ADRA1A, ADRA1B, ADRA1D
PIPEROXAN	ChEMBL	Phase 2	ADRA1A, ADRA1B, ADRA1D
PIZOTYLINE	ChEMBL	Phase 2	ADRA1A, ADRA1B, ADRA1D
SPIRAMIDE	ChEMBL	Phase 2	ADRA1A, ADRA1B, ADRA1D