SILODOSIN

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C25H32F3N3O4
Molecular Weight	495.5345
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

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

InChI

InChIKey=PNCPYILNMDWPEY-QGZVFWFLSA-N

InChI=1S/C25H32F3N3O4/c1-17(30-8-12-34-21-5-2-3-6-22(21)35-16-25(26,27)28)13-18-14-19-7-10-31(9-4-11-32)23(19)20(15-18)24(29)33/h2-3,5-6,14-15,17,30,32H,4,7-13,16H2,1H3,(H2,29,33)/t17-/m1/s1

HIDE SMILES / InChI

Molecular Formula	C25H32F3N3O4
Molecular Weight	495.5345
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022206s012lbl.pdf | https://www.ncbi.nlm.nih.gov/pubmed/14725494 | https://www.ncbi.nlm.nih.gov/pubmed/7651358

Silodosin is a selective antagonsit of alpha-1a adrenergic receptor which was developed by Kissei Pharmaceutical. The drug was approved by FDA under the name Rapaflo for the treatment of signs and symptoms associated with benign prostatic hyperplasia.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Alpha-1a adrenergic receptor 67 Target ID: CHEMBL229 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022206s012lbl.pdf	Antagonist 2849		0.32 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Benign prostatic hyperplasia 28 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022206s012lbl.pdf	Palliative		Approved 8583	RAPAFLO Approved Use RAPAFLO, a selective alpha-1 adrenergic receptor antagonist, is indicated for the treatment of the signs and symptoms of benign prostatic hyperplasia (BPH). Launch Date 2008

C_max

Value	Dose	Co-administered	Analyte	Population
61.6 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022206s012lbl.pdf	8 mg 1 times / day steady-state, oral dose: 8 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		SILODOSIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
373.4 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022206s012lbl.pdf	8 mg 1 times / day steady-state, oral dose: 8 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		SILODOSIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
13.3 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022206s012lbl.pdf	8 mg 1 times / day steady-state, oral dose: 8 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		SILODOSIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
3% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022206s012lbl.pdf	8 mg 1 times / day steady-state, oral dose: 8 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		SILODOSIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
48 mg 1 times / day multiple, oral Highest studied dose Dose: 48 mg, 1 times / day Route: oral Route: multiple Dose: 48 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/21114397 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_MedR_P1.pdf#page=54	healthy, 19 - 45 Health Status: healthy Age Group: 19 - 45 Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/21114397 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_MedR_P1.pdf#page=54	DLT: Postural hypotension... Dose limiting toxicities: Postural hypotension Sources: https://pubmed.ncbi.nlm.nih.gov/21114397 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_MedR_P1.pdf#page=54
12 mg single, oral Highest studied dose Dose: 12 mg Route: oral Route: single Dose: 12 mg Sources: https://pubmed.ncbi.nlm.nih.gov/21804212	healthy, 23 ± 1.4 Health Status: healthy Age Group: 23 ± 1.4 Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/21804212	Other AEs: Nervous system disorder NOS, Fatigue... Other AEs: Nervous system disorder NOS (13%) Fatigue (13%) Dizziness (13%) Hematuria (13%) Leukocyturia (13%) Sources: https://pubmed.ncbi.nlm.nih.gov/21804212
8 mg 1 times / day multiple, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: https://allergan-web-cdn-prod.azureedge.net/allergancanadaspecialty/allergancanadaspecialty/media/actavis-canada-specialty/en/products/pms/rapaflo-pm_eng-12march2018.pdf	unhealthy Health Status: unhealthy Sex: M Sources: https://allergan-web-cdn-prod.azureedge.net/allergancanadaspecialty/allergancanadaspecialty/media/actavis-canada-specialty/en/products/pms/rapaflo-pm_eng-12march2018.pdf	Disc. AE: Retrograde ejaculation... AEs leading to discontinuation/dose reduction: Retrograde ejaculation (2.8%) Sources: https://allergan-web-cdn-prod.azureedge.net/allergancanadaspecialty/allergancanadaspecialty/media/actavis-canada-specialty/en/products/pms/rapaflo-pm_eng-12march2018.pdf
8 mg 1 times / day multiple, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: https://www.ema.europa.eu/en/documents/product-information/silodyx-epar-product-information_en.pdf	unhealthy Health Status: unhealthy Sex: M Sources: https://www.ema.europa.eu/en/documents/product-information/silodyx-epar-product-information_en.pdf	Other AEs: Intraoperative floppy iris syndrome... Other AEs: Intraoperative floppy iris syndrome Sources: https://www.ema.europa.eu/en/documents/product-information/silodyx-epar-product-information_en.pdf

AEs

AE	Significance	Dose	Population
Postural hypotension	DLT	48 mg 1 times / day multiple, oral Highest studied dose Dose: 48 mg, 1 times / day Route: oral Route: multiple Dose: 48 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/21114397 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_MedR_P1.pdf#page=54	healthy, 19 - 45 Health Status: healthy Age Group: 19 - 45 Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/21114397 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_MedR_P1.pdf#page=54
Dizziness	13%	12 mg single, oral Highest studied dose Dose: 12 mg Route: oral Route: single Dose: 12 mg Sources: https://pubmed.ncbi.nlm.nih.gov/21804212	healthy, 23 ± 1.4 Health Status: healthy Age Group: 23 ± 1.4 Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/21804212
Fatigue	13%	12 mg single, oral Highest studied dose Dose: 12 mg Route: oral Route: single Dose: 12 mg Sources: https://pubmed.ncbi.nlm.nih.gov/21804212	healthy, 23 ± 1.4 Health Status: healthy Age Group: 23 ± 1.4 Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/21804212
Hematuria	13%	12 mg single, oral Highest studied dose Dose: 12 mg Route: oral Route: single Dose: 12 mg Sources: https://pubmed.ncbi.nlm.nih.gov/21804212	healthy, 23 ± 1.4 Health Status: healthy Age Group: 23 ± 1.4 Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/21804212
Leukocyturia	13%	12 mg single, oral Highest studied dose Dose: 12 mg Route: oral Route: single Dose: 12 mg Sources: https://pubmed.ncbi.nlm.nih.gov/21804212	healthy, 23 ± 1.4 Health Status: healthy Age Group: 23 ± 1.4 Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/21804212
Nervous system disorder NOS	13%	12 mg single, oral Highest studied dose Dose: 12 mg Route: oral Route: single Dose: 12 mg Sources: https://pubmed.ncbi.nlm.nih.gov/21804212	healthy, 23 ± 1.4 Health Status: healthy Age Group: 23 ± 1.4 Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/21804212
Retrograde ejaculation	2.8% Disc. AE	8 mg 1 times / day multiple, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: https://allergan-web-cdn-prod.azureedge.net/allergancanadaspecialty/allergancanadaspecialty/media/actavis-canada-specialty/en/products/pms/rapaflo-pm_eng-12march2018.pdf	unhealthy Health Status: unhealthy Sex: M Sources: https://allergan-web-cdn-prod.azureedge.net/allergancanadaspecialty/allergancanadaspecialty/media/actavis-canada-specialty/en/products/pms/rapaflo-pm_eng-12march2018.pdf
Intraoperative floppy iris syndrome		8 mg 1 times / day multiple, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: https://www.ema.europa.eu/en/documents/product-information/silodyx-epar-product-information_en.pdf	unhealthy Health Status: unhealthy Sex: M Sources: https://www.ema.europa.eu/en/documents/product-information/silodyx-epar-product-information_en.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946 inhibitor 2252 inducer 1087	inhibitor 2438 inducer 440 substrate 1193	inhibitor 2507 substrate 1388	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 2153 CYP2A6 879 CYP2C19 2057 CYP2E1 1060	UGT2B7 456 P-gp 2052 CYP1A1 389 CYP1A2 1197 CYP2A6 626 CYP2C19 1119 CYP2E1 729 UGT1A1 479 UGT1A3 470 UGT1A6 343 UGT1A9 423 UGT1A10 331 UGT2B15 236	CYP1A2 832 CYP2C8 198 CYP2C19 329 P-gp 301

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
CYP2A6 911	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
CYP2C19 2141	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
CYP2C8 1117	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
CYP2E1 1146	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
P-gp 1932	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5.0	no	no (co-administration study) Comment: silodosin did not significantly affect the PK of digoxin Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5.0

Drug as victim

Target	Modality	Activity	Clinical evidence
UGT1A1 479	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0	no
UGT1A10 331	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0	no
UGT1A3 470	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0	no
UGT1A6 343	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0	no
UGT1A9 423	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0	no
UGT2B15 236	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_PharmR_P1.pdf Page: 61.0	no
CYP1A1 389	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0	no	no (co-administration study) Comment: furafylline did not affect silodosin metabolism Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0
CYP1A2 1197	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0	no	no (co-administration study) Comment: furafylline did not affect silodosin metabolism Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0
CYP2A6 626	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0	no	no (co-administration study) Comment: coumarin did not affect silodosin metabolism Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0
CYP2C19 1119	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0	no	no (co-administration study) Comment: S-mephenytoin did not affect silodosin metabolism Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0
CYP2C9 1193	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0	no	no (co-administration study) Comment: sulfafenazole did not affect silodosin metabolism Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0
CYP2D6 1388	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0	no	no (co-administration study) Comment: quinidine did not affect silodosin metabolism Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0
CYP2E1 729	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0	no	no (co-administration study) Comment: diethyldithiocarbamate did not affect silodosin metabolism Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0
UGT2B7 456	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 11.0	yes
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 11, 12	yes	yes (co-administration study) Comment: ketaconzaole increased sildosin Cmax by 3.8-fold and AUC by 3.2-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 11, 12
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 17.0	yes	yes (co-administration study) Comment: ketaconzaole increased sildosin Cmax by 3.8-fold and AUC by 3.2-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 17.0

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_PharmR_P1.pdf Page: 2, 31

Sourcing

Vendor/Aggregator	ID	URL
AA Blocks	AA001VHU	https://www.aablocks.com/goods/Goods/detail?id=AA001VHU
Aaron Chemicals	AR001W9M	http://www.aaronchem.com/160970-54-7
abcr GmbH	AB479551	http://www.abcr.com/shop/en/AB479551
AbMole Bioscience	M3551	http://www.abmole.com/products/silodosin.html
Achemo Scientific Limited	AC-63538	http://www.achemo.com/search/?Keyword= 160970-54-7
Achemtek	0101-002081	http://www.achemtek.com/160970-54-7
Acorn PharmaTech	ACN-S002529	http://www.acornpharmatech.com/
Active Biopharma	ABP000202	http://www.activebiopharma.com/160970-54-7
AK Scientific, Inc. (AKSCI)	66700	http://www.aksci.com/item_detail.php?cat=66700
Alfa Chemistry	1051374-52-7	https://www.alfa-chemistry.com/cas_1051374-52-7.htm
Alfa Chemistry	AP160970547	https://reagents.alfa-chemistry.com/product/silodosin-cas-160970-54-7-5943.html
Allbio Pharm Co., Ltd	AF15549	http://www.allbiopharm.com/product/n/AF15549
Alsachim	1524	http://www.alsachim.com/product-C2122-glo.bal-view.html
Ambeed	A632990	https://www.ambeed.com/products/160970-54-7.html
Angel Pharmatech	AG-19708	http://www.angelpharmatech.com/160970-54-7.html
ApexBio Technology	A8521	http://www.apexbt.com/silodosin.html
Aurora Fine Chemicals LLC	A24.077.565	http://online.aurorafinechemicals.com/info?ID=A24.077.565
Aurum Pharmatech LLC	W-5225	http://www.Aurumpharmatech.com/Product/ProductDetails/W_5225
AvaChem Scientific	2658	http://www.avachem.com/productSearch.asp?2658
Axon MedChem	3112	https://www.axonmedchem.com/product/3112
BioChemPartner	BCP02143	http://www.biochempartner.com/160970-54-7-BCP02143
BioSynth	Q-102517	https://www.biosynth.com/en/products/chemical-intermediates/advanced-intermediates/products/Q-102517.html
BLD Pharm	BD161491	http://www.bldpharm.com/products/160970-54-7.html
Chem Scene	CS-0284	http://www.chemscene.com/160970-54-7.html
ChemFaces	CFN90002	http://www.chemfaces.com/natural/Silodosin-CFN90002.html
ChemMol	30116026	http://www.chemmol.com/chemmol/30116026.html
ChemMol	49401385	http://www.chemmol.com/chemmol/49401385.html
Chemspace	CSSB00016998219	https://chem-space.com/CSSB00016998219
Clearsynth	CS-O-11743	https://www.clearsynth.com/en/CSO11743.html
CSNpharm	CSN12335	https://www.csnpharm.com/products/silodosin.html
DC Chemicals	DCAPI1485	http://www.dcchemicals.com/product_show-Silodosin.html
Hairui	HR117388	http://www.hairuichem.com/en/product/160970-54-7.html
iChemical	EBD33557	http://www.ichemical.com/products/160970-54-7.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs
Lab Network	LN01296344	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01296344
MedChem Express	HY-10122	https://www.medchemexpress.com/Silodosin.html
OChem	24781	http://www.ocheminc.com/index.php?act=psearch&pid=970S649
Renno Tech	RL02066	http://www.rennotech.com/product_show.asp?id=2315
Selleck Chemicals	S1613	http://www.selleckchem.com/products/Silodosin(Rapaflo).html
Sigma-Aldrich	SML2142_SIGMA	https://www.sigmaaldrich.com/catalog/product/sigma/sml2142?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Smolecule	S543190	http://www.smolecule.com/products/s543190
Synblock Inc	SB19320	http://www.synblock.com/product/160970-54-7.html
THE BioTek	bt-283302	https://www.thebiotek.com/product/inhibitors/bt-283302
Tocris	6663	https://www.tocris.com/products/silodosin_6663
TripleBond	CS0060	http://www.triplebond-canada.com/prod/1593/
VladaChem	VL281883-10MG	https://www.vladachem.com/product.php?products=160970-54-7

PubMed

Title	Date	PubMed
(RS)-1-[5-(2-Chloro-prop-yl)indolin-1-yl]ethanone.	2010-12-08	21522761
Silodosin for the treatment of benign prostatic hyperplasia: pharmacology and cardiovascular tolerability.	2010-12	21114397
Ejaculation disorder is associated with increased efficacy of silodosin for benign prostatic hyperplasia.	2010-12	20472263
Gateways to clinical trials.	2010-11	21225019
Silodosin in the treatment of benign prostatic hyperplasia.	2010-10-27	21116335
Editorial comment to short-term effects of crossover treatment with silodosin and tamsulosin hydrochloride for lower urinary tract symptoms associated with benign prostatic hyperplasia.	2010-10	20887633
Short-term effects of crossover treatment with silodosin and tamsulosin hydrochloride for lower urinary tract symptoms associated with benign prostatic hyperplasia.	2010-10	20735791
Role of supraspinal and spinal alpha1-adrenergic receptor subtypes in micturition reflex in conscious rats.	2010-10	20668103
Selective α1A-blocker improves bladder storage function in rats via suppression of C-fiber afferent activity.	2010-10	19834713
Gateways to clinical trials.	2010-09-21	20852754
(RS)-1-(1-Acetyl-indolin-5-yl)-2-chloro-propan-1-one.	2010-06-09	21587848
Effects of the selective alpha 1a-adrenoceptor antagonist silodosin on ECGs of healthy men in a randomized, double-blind, placebo- and moxifloxacin-controlled study.	2010-05	20220748
Torsades de Pointes induced by a combination of garenoxacin and disopyramide and other cytochrome P450, family 3, subfamily A polypeptide-4-influencing drugs during hypokalemia due to licorice.	2010-04	19915794
Urodynamic effects of silodosin, a new alpha 1A-adrenoceptor selective antagonist, for the treatment of benign prostatic hyperplasia.	2010-04	19693954
Impact of dry ejaculation caused by highly selective alpha1A-blocker: randomized, double-blind, placebo-controlled crossover pilot study in healthy volunteer men.	2010-03	20102447
Lack of pharmacodynamic interaction of silodosin, a highly selective alpha1a-adrenoceptor antagonist, with the phosphodiesterase-5 inhibitors sildenafil and tadalafil in healthy men.	2010-03	20080287
Silodosin for benign prostatic hyperplasia.	2010-02	20071497
Visualization and tissue distribution of alpha1L-adrenoceptor in human prostate by the fluorescently labeled ligand Alexa-488-silodosin.	2010-02	20034639
[Investigation of adverse events and the continuance rate of silodosin in all patients who received silodosin for lower urinary tract symptoms suggestive of benign prostatic hyperplasia].	2010-01	20158073
Effects of silodosin and naftopidil on the distal ureter and cardiovascular system in anesthetized dogs: comparison of potential medications for distal ureteral stone passage.	2010-01	19914658
The add-on effect of solifenacin for patients with remaining overactive bladder after treatment with tamsulosin for lower urinary tract symptoms suggestive of benign prostatic obstruction.	2010	20981257
Efficacy of silodosin for relieving benign prostatic obstruction: prospective pressure flow study.	2009-12	19837428
Silodosin in the treatment of the signs and symptoms of benign prostatic hyperplasia: a 9-month, open-label extension study.	2009-12	19815265
Gene expressions and mechanical functions of α1-adrenoceptor subtypes in mouse ureter.	2009-12	19259685
Determination of silodosin in human plasma by liquid chromatography-tandem mass spectrometry.	2009-11-01	19782650
Silodosin: a selective alpha1A-adrenergic receptor antagonist for the treatment of benign prostatic hyperplasia.	2009-11	20109995
Effects of four different alpha(1)-adrenoceptor antagonists on alpha-adrenoceptor agonist-induced contractions in isolated mouse and hamster ureters.	2009-08	19783871
Mechanical function and gene expression of alpha(1)-adrenoceptor subtypes in dog intravesical ureter.	2009-08	19371927
Effects of silodosin and tamsulosin on the urethra and cardiovascular system in young and old dogs with benign prostatic hyperplasia.	2009-06-24	19389393
Orgasm is preserved regardless of ejaculatory dysfunction with selective alpha1A-blocker administration.	2009-06-19	19536124
Rapid efficacy of the highly selective alpha1A-adrenoceptor antagonist silodosin in men with signs and symptoms of benign prostatic hyperplasia: pooled results of 2 phase 3 studies.	2009-06	19371887
Short- and long-term effects of silodosin, a selective alpha 1A-adrenoceptor antagonist, on ejaculatory function in rats.	2009-06	19220259
New drugs: milnacipran hydrochloride, fesoterodine fumarate, and silodosin.	2009-03-18	19289354
Silodosin (Rapaflo) for benign prostatic hyperplasia.	2009-01-12	19122568
Efficacy of alpha-Adrenergic Receptor Blockers in the Treatment of Male Lower Urinary Tract Symptoms.	2009	20126606
[Multi-center trial on the early effects of silodosin on lower urinary tract symptoms associated with benign prostatic hyperplasia].	2008-12	19174997
The involvement of urothelial alpha1A adrenergic receptor in controlling the micturition reflex.	2008-10	18997438
Early efficacy of silodosin in patients with lower urinary tract symptoms suggestive of benign prostatic hyperplasia.	2008-10	18775032
Ejaculatory dysfunction caused by the new alpha1-blocker silodosin: A preliminary study to analyze human ejaculation using color Doppler ultrasonography.	2008-10	18721206
Computational studies of the binding site of alpha1A-adrenoceptor antagonists.	2008-10	18626669
Inhibition of Seminal emission is the main cause of anejaculation induced by a new highly selective alpha1A-blocker in normal volunteers.	2008-09	18399947
Gateways to clinical trials.	2008-06	18806898
Different affinities of native alpha1B-adrenoceptors for ketanserin between intact tissue segments and membrane preparations.	2008-04-28	18336813
In vivo study on the effects of alpha1-adrenoceptor antagonists on intraurethral pressure in the prostatic urethra and intraluminal pressure in the vas deferens in male dogs.	2008-02-02	18078926
Silodosin, a novel selective alpha 1A-adrenoceptor selective antagonist for the treatment of benign prostatic hyperplasia.	2007-12	18042003
Expressions and mechanical functions of alpha1-adrenoceptor subtypes in hamster ureter.	2007-11-14	17658513
Alpha1-adrenoceptors and ejaculatory function.	2007-10	17603543
Prediction of alpha1-adrenoceptor occupancy in the human prostate from plasma concentrations of silodosin, tamsulosin and terazosin to treat urinary obstruction in benign prostatic hyperplasia.	2007-07	17603160
Search for new alpha1a-adrenoceptor-selective antagonist for treating lower urinary tract symptoms associated with benign prostatic hyperplasia.	2007-04	19675810
KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues.	1995-08	7651358

Patents

Sample Use Guides

In Vivo Use Guide

The recommended dose is 8 mg orally once daily with a meal. The dose can be reduced to 4 mg for those with moderate renal impairment.

Route of Administration: Oral

In Vitro Use Guide

Human prostate tissue were treated with silodosin at 3 uM added 15 min before application of noradrenaline (30 uM) to study the inhibition of noradrenaline-activated Transcription Factors Elk1 and SRF.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:09:49 GMT 2025` Edited by `admin` on `Mon Mar 31 18:09:49 GMT 2025`
Record UNII	CUZ39LUY82
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

RAPAFLO

Preferred Name

English

SILODOSIN

Official Name

English

SILODOSIN [ORANGE BOOK]

Common Name

English

KSO-0400

Common Name

English

URIEF

Brand Name

English

SILODOSIN [EMA EPAR]

Common Name

English

(-)-1-(3-HYDROXYPROPYL)-5-((2R)-2-((2-(2-(2,2,2-TRIFLUOROETHOXY)PHENOXY)ETHYL)AMINO)PROPYL)-2,3-DIHYDRO-1H-INDOLE-7-CARBOXAMIDE

Systematic Name

English

2,3-DIHYDRO-1-(3-HYDROXYPROPYL)-5-((2R)-2-((2-(2-(2,2,2-TRIFLUOROETHOXY)PHENOXY)ETHYL)AMINO)PROPYL)-1H-INDOLE-7-CARBOXAMIDE

Systematic Name

English

KAD-3213

Code

English

SILODOSIN [JAN]

Common Name

English

silodosin [INN]

Common Name

English

SILODOSIN [MI]

Common Name

English

SILODYX

Brand Name

English

RAPILIF

Brand Name

English

SILODOSIN [VANDF]

Common Name

English

Silodosin [WHO-DD]

Common Name

English

KMD-3213

Code

English

SILODAL

Brand Name

English

SILODOSIN [MART.]

Common Name

English

UROREC

Brand Name

English

Classification Tree Code System Code

EMA ASSESSMENT REPORTS

UROREC (AUTHORIZED: PROSTATIC HYPERPLASIA)