Silodosin

Summary

Silodosin (CHEMBL24778) is an approved small molecule (ATC G04CA04) targeting ADRA1A, ADRA1B, and ADRA1D; indicated across 6 conditions including benign prostatic hyperplasia and nephrolithiasis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: G04CA04
• Targets: 3 (ADRA1A, ADRA1B, ADRA1D)
• Indications: 6 conditions
• Clinical trials: 35
• Chemistry: 495.5 Da · C25H32F3N3O4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL24778
Name	Silodosin
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	5312125
ATC	G04CA04
Molecular formula	C25H32F3N3O4
Molecular weight	495.5
InChIKey	PNCPYILNMDWPEY-QGZVFWFLSA-N

SMILES: C[C@H](CC1=CC2=C(C(=C1)C(=O)N)N(CC2)CCCO)NCCOC3=CC=CC=C3OCC(F)(F)F

IUPAC name: 1-(3-hydroxypropyl)-5-[(2R)-2-[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethylamino]propyl]-2,3-dihydroindole-7-carboxamide

Also known as: KAD-3213, KMD-3213, Kso-0400, Rapaflo, Rapilif, Silodal, Silodosin, Silodosin recordati, Silodosina, Silodosine, Silodyx, Urief

Patent coverage: 759 distinct patent families (2,288 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 2,281 (100%) 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	10.4		P35348
ADRA1B	α1B-adrenoceptor	Antagonist	7.7	0%	P35368
ADRA1D	α1D-adrenoceptor	Antagonist	8.7	0.2%	P25100

Broader ChEMBL bioactivity targets: 24 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, 5-hydroxytryptamine receptor 1B, Alpha-2C adrenergic receptor, Alpha-2B adrenergic receptor, Sodium channel protein type 5 subunit alpha, 5-hydroxytryptamine receptor 1D, D(1A) dopamine receptor, Beta-2 adrenergic receptor, 5-hydroxytryptamine receptor 1A.

Bioactivity

ChEMBL activities: 39 potent at pChembl ≥ 5 of 45 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
ADRA1A	10.44	Ki	0.04	nM	CHEMBL_ACT_1430355
ADRA1A	10.4	Ki	0.04	nM	CHEMBL_ACT_269975
P43140	9.1	IC50	0.8	nM	CHEMBL_ACT_16748975
ADRA1A	8.74	IC50	1.8	nM	CHEMBL_ACT_16748783
ADRA1A	8.72	IC50	1.9	nM	CHEMBL_ACT_16598445
ADRA1D	8.7	Ki	2	nM	CHEMBL_ACT_269977
ADRA1A	8.54	AC50	2.9	nM	CHEMBL_ACT_25218507
HTR1A	8.52	AC50	3	nM	CHEMBL_ACT_25165580
ADRA1A	8.52	AC50	3	nM	CHEMBL_ACT_25219330
ADRA1D	8.2	IC50	6.3	nM	CHEMBL_ACT_16748898
ADRA1B	7.7	Ki	19.95	nM	CHEMBL_ACT_269976
ADRA1D	7.56	IC50	27.3	nM	CHEMBL_ACT_16598279
ADRA1A	7.52	Ki	30.28	nM	CHEMBL_ACT_25740712
ADRB2	7.48	Ki	32.83	nM	CHEMBL_ACT_25740718
ADRA1D	7.33	Ki	47.32	nM	CHEMBL_ACT_25740714
HTR1A	7.33	Ki	46.97	nM	CHEMBL_ACT_25740723
DRD3	7.32	AC50	48.3	nM	CHEMBL_ACT_25195062
DRD3	7.14	Ki	71.55	nM	CHEMBL_ACT_25740720
P15823	7.04	IC50	90.1	nM	CHEMBL_ACT_16748978
HTR1D	7.04	Ki	91.69	nM	CHEMBL_ACT_25740725
ADRA1B	6.94	IC50	116	nM	CHEMBL_ACT_16748861
ADRA1B	6.71	Ki	195.8	nM	CHEMBL_ACT_25740713
ADRB2	6.67	IC50	214.1	nM	CHEMBL_ACT_25751156
ADRA2C	6.44	Ki	360	nM	CHEMBL_ACT_25740717
HTR1B	6.43	Ki	373	nM	CHEMBL_ACT_25740724
HTR7	6.32	Ki	480.3	nM	CHEMBL_ACT_25740727
ADRA1B	6.27	IC50	541.4	nM	CHEMBL_ACT_16598354
ADRA2A	6.17	Ki	682.7	nM	CHEMBL_ACT_25740715
ADRA2B	6.11	Ki	786	nM	CHEMBL_ACT_25740716
DRD2	6	Ki	989.1	nM	CHEMBL_ACT_25740719

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

6 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
nephrolithiasis	3	MONDO:0008171	EFO:0004253
urolithiasis	3	MONDO:0024647	MONDO:0024647
prostatitis	2	MONDO:0005280	EFO:0003830
premature ejaculation	2	MONDO:0001780	EFO:0803321

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

Clinical trials

Total trials: 35.

Phase distribution

Phase	Trials
PHASE4	12
PHASE3	10
PHASE2	6
Not specified	4
PHASE1/PHASE2	1
PHASE1	1
EARLY_PHASE1	1

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
NCT07467343	PHASE4	NOT_YET_RECRUITING	Silodosin vs Tamsulosin for LUTS Due to BPH: A Randomized Crossover Trial
NCT07614321	PHASE4	RECRUITING	Silodosin for Urinary Symptoms in Female Patients With Multiple Sclerosis
NCT01228370	PHASE4	COMPLETED	Efficacy and Safety of Silodosin on Voiding Dysfunction Associated With Neurogenic Bladder
NCT01259531	PHASE4	COMPLETED	Study of a α1A Adrenoceptor Selective Antagonist Silodosin to Treat Severe Benign Prostatic Hyperplasia(BPH)
NCT01260129	PHASE4	COMPLETED	Safety and Efficacy of QD Versus BID Silodosin With Lower Urinary Tract Symptoms Suggestive of BPH
NCT01533389	PHASE4	COMPLETED	Efficacy and Safety of Silodosin in the Treatment of Natural Expulsion in Patients With Ureteral Stones
NCT01757769	PHASE4	COMPLETED	Effectiveness and Safety of Silodosin in the Treatment of Benign Prostatic Hyperplasia
NCT02106182	PHASE4	COMPLETED	Efficacy and Safety of Silodosin on Nocturia for Patients With Benign Prostatic Hyperplasia
NCT02369744	PHASE4	TERMINATED	Silodosin Versus Tamsulosin for Treatment of Ureteral Stones
NCT04107896	PHASE4	COMPLETED	Efficacy of Silodosin in the Treatment of Symptomatic Benign Prostatic Hyperplasia (BPH)
NCT07134907	PHASE4	COMPLETED	The Efficacy and Safety of Qianweitai (Silodosin Capsule) Versus Tamsulosin in the Treatment of BPH
NCT00224107	PHASE3	COMPLETED	A New Drug for Benign Prostatic Hyperplasia (BPH) Compared With Placebo
NCT00224120	PHASE3	COMPLETED	A New Drug for Benign Prostatic Hyperplasia (BPH) Compared With Placebo
NCT00224133	PHASE3	COMPLETED	The Evaluation of the Safety of a New Drug for Benign Prostatic Hyperplasia Used for 9 Months
NCT00359905	PHASE3	COMPLETED	Evaluation of the Efficacy and Safety of Silodosin in the Treatment of the Signs and Symptoms of BPH
NCT01560091	PHASE3	WITHDRAWN	Differential Effect of Silodosin Versus Tamsulosin on Stone Clearance After Extra-corporeal Shock Wave Lithotripsy
NCT02090439	PHASE3	TERMINATED	Effectiveness of Silodosin in Medical Expulsive Therapy for Ureteral Pelvic Stone From 4 to 10 mm.
NCT02220829	PHASE3	COMPLETED	Comparative Study of Use of Alpha-Blockers to Treat Symptoms in Prostate Cancer Patients Undergoing Radiation Therapy
NCT05570084	PHASE3	UNKNOWN	Silodosin vs Tamsulosin as MET
NCT05921370	PHASE3	COMPLETED	Silodosin in Retrograde Intrarenal Surgery
NCT06114979	PHASE3	UNKNOWN	Silodosin vs Placebo in the Treatment of Female LUTS
NCT00740779	PHASE2	COMPLETED	Use of Silodosin to Treat Moderate to Severe Abacterial Chronic Prostatitis/Chronic Pelvic Pain Syndrome.
NCT00793819	PHASE2	COMPLETED	A Study of Silodosin 8 mg Daily for the Treatment of Nocturia in Men With Benign Prostatic Hyperplasia
NCT01144949	PHASE2	COMPLETED	Study of Silodosin to Facilitate Passage of Urinary Stones
NCT01222650	PHASE2	COMPLETED	A Comparative Study of KSO-0400 in BPH Patients With LUTS
NCT01539265	PHASE2	COMPLETED	A Dose-finding Study of Silodosin in Patients With Urinary Calculi
NCT02581826	PHASE2	UNKNOWN	Safety and Efficacy of Silodosin in the Treatment of Premature Ejaculation
NCT06381206	PHASE1/PHASE2	COMPLETED	Silodosin in Management of Lower Ureteral Stones
NCT05790902	PHASE1	COMPLETED	COMPARISON OF SILODOSIN AND TAMSULOSIN IN MEDICAL EXPULSIVE THERAPY OF DISTAL URETERIC CALCULI
NCT06282731	EARLY_PHASE1	COMPLETED	The Changes of Urine Growth Factors Level
NCT05789732	Not specified	COMPLETED	Silodosin, Tadalafil Alone vs. Silodosin Plus Tadalafil as MET for Lower Ureteric Stones
NCT05823662	Not specified	COMPLETED	Double J Stenting and Sildosin After URSL for Lower Ureteric Stones
NCT06332235	Not specified	UNKNOWN	Efficacy and Safety of Silodosin in the Treatment of Lower Urinary Tract Symptoms in Taiwanese Population.
NCT06999135	Not specified	COMPLETED	Comparison of Silodosin and Tamsulosin for Medical Expulsive Therapy in Patients With Ureteral 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 3 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
TAMSULOSIN	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