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=CC(C(N)=O)=C2N(CCCO)CCC2=C1)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 66 Target ID: CHEMBL229 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022206s012lbl.pdf	Antagonist 2760		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 8360	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 1.22342395E12

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 n = 6 Health Status: healthy Age Group: 19 - 45 Sex: M Population Size: 6 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 Page: p.1242	healthy, 23 ± 1.4 n = 8 Health Status: healthy Age Group: 23 ± 1.4 Sex: M Population Size: 8 Sources: https://pubmed.ncbi.nlm.nih.gov/21804212 Page: p.1242	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 Page: p.1242
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 Page: p.6	unhealthy n = 466 Health Status: unhealthy Condition: Benign prostatic hyperplasia Sex: M Population Size: 466 Sources: https://allergan-web-cdn-prod.azureedge.net/allergancanadaspecialty/allergancanadaspecialty/media/actavis-canada-specialty/en/products/pms/rapaflo-pm_eng-12march2018.pdf Page: p.6	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 Page: p.6
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 Page: p.3	unhealthy Health Status: unhealthy Condition: Benign prostatic hyperplasia Sex: M Sources: https://www.ema.europa.eu/en/documents/product-information/silodyx-epar-product-information_en.pdf Page: p.3	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 Page: p.3

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 n = 6 Health Status: healthy Age Group: 19 - 45 Sex: M Population Size: 6 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 Page: p.1242	healthy, 23 ± 1.4 n = 8 Health Status: healthy Age Group: 23 ± 1.4 Sex: M Population Size: 8 Sources: https://pubmed.ncbi.nlm.nih.gov/21804212 Page: p.1242
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 Page: p.1242	healthy, 23 ± 1.4 n = 8 Health Status: healthy Age Group: 23 ± 1.4 Sex: M Population Size: 8 Sources: https://pubmed.ncbi.nlm.nih.gov/21804212 Page: p.1242
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 Page: p.1242	healthy, 23 ± 1.4 n = 8 Health Status: healthy Age Group: 23 ± 1.4 Sex: M Population Size: 8 Sources: https://pubmed.ncbi.nlm.nih.gov/21804212 Page: p.1242
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 Page: p.1242	healthy, 23 ± 1.4 n = 8 Health Status: healthy Age Group: 23 ± 1.4 Sex: M Population Size: 8 Sources: https://pubmed.ncbi.nlm.nih.gov/21804212 Page: p.1242
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 Page: p.1242	healthy, 23 ± 1.4 n = 8 Health Status: healthy Age Group: 23 ± 1.4 Sex: M Population Size: 8 Sources: https://pubmed.ncbi.nlm.nih.gov/21804212 Page: p.1242
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 Page: p.6	unhealthy n = 466 Health Status: unhealthy Condition: Benign prostatic hyperplasia Sex: M Population Size: 466 Sources: https://allergan-web-cdn-prod.azureedge.net/allergancanadaspecialty/allergancanadaspecialty/media/actavis-canada-specialty/en/products/pms/rapaflo-pm_eng-12march2018.pdf Page: p.6
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 Page: p.3	unhealthy Health Status: unhealthy Condition: Benign prostatic hyperplasia Sex: M Sources: https://www.ema.europa.eu/en/documents/product-information/silodyx-epar-product-information_en.pdf Page: p.3

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1709 inhibitor 1579 inducer 768	inhibitor 1752 inducer 383 substrate 1010	inhibitor 1837 substrate 1193	inhibitor 1599

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1509 CYP2A6 704 CYP2C19 1463 CYP2E1 876	UGT2B7 389 P-gp 1527 CYP1A1 348 CYP1A2 1032 CYP2A6 523 CYP2C19 985 CYP2E1 648 UGT1A1 418 UGT1A3 422 UGT1A6 307 UGT1A9 380 UGT1A10 290 UGT2B15 203	CYP1A2 689 CYP2C8 168 CYP2C19 290 P-gp 257

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP1A2 1673	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
CYP1A2 1673	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
CYP2A6 736	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
CYP2C19 1537	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
CYP2C19 1537	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
CYP2C8 955	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
CYP2C9 1803	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
CYP2C9 1803	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
CYP2D6 1875	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
CYP2E1 964	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
CYP3A4 1909	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
CYP3A4 1909	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 5, 12	no
P-gp 1626	inducer 1542 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 418	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0	no
UGT1A10 290	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0	no
UGT1A3 422	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0	no
UGT1A6 307	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0	no
UGT1A9 380	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 16.0	no
UGT2B15 203	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_PharmR_P1.pdf Page: 61.0	no
CYP1A1 348	substrate 3326 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 1032	substrate 3326 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 523	substrate 3326 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 985	substrate 3326 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 1010	substrate 3326 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 1193	substrate 3326 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 648	substrate 3326 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 389	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022206s000_ClinPharmR.pdf Page: 11.0	yes
CYP3A4 1709	substrate 3326 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 1527	substrate 3326 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 1632	inhibitor 1613 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
AK Scientific, Inc. (AKSCI)	66700	http://www.aksci.com/item_detail.php?cat=66700
Aaron Chemicals	AR001W9M	http://www.aaronchem.com/160970-54-7
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
Alfa Chemistry	AP160970547	https://reagents.alfa-chemistry.com/product/silodosin-cas-160970-54-7-5943.html
Alfa Chemistry	1051374-52-7	https://www.alfa-chemistry.com/cas_1051374-52-7.htm
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
BLD Pharm	BD161491	http://www.bldpharm.com/products/160970-54-7.html
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
CSNpharm	CSN12335	https://www.csnpharm.com/products/silodosin.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
DC Chemicals	DCAPI1485	http://www.dcchemicals.com/product_show-Silodosin.html
Hairui	HR117388	http://www.hairuichem.com/en/product/160970-54-7.html
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
abcr GmbH	AB479551	http://www.abcr.com/shop/en/AB479551
iChemical	EBD33557	http://www.ichemical.com/products/160970-54-7.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs

PubMed

Title	Date	PubMed
KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues.	1995 Aug	7651358
Carvedilol selectively inhibits oscillatory intracellular calcium changes evoked by human alpha1D- and alpha1B-adrenergic receptors.	2004 Sep 1	15306222
Cardiovascular effects of the selective alphalA-adrenoceptor antagonist silodosin (KMD-3213), a drug for the treatment of voiding dysfunction.	2006	17225563
[Duration of action of silodosin (KMD-3213) against phenylephrine-induced increase in intraurethral pressure in rats].	2006 Mar	16518088
[Effect of silodosin on intraurethral pressure increase induced by hypogastric nerve stimulation in dogs with benign prostatic hyperplasia].	2006 Mar	16518087
[Effects of silodosin (KMD-3213) on phenylephrine-induced increase in intraurethral pressure and blood pressure in rats--study of the selectivity for lower urinary tract].	2006 Mar	16518086
[Alpha1-adrenoceptor subtypes and alpha1-adrenoceptor antagonists].	2006 Mar	16518082
Search for new alpha1a-adrenoceptor-selective antagonist for treating lower urinary tract symptoms associated with benign prostatic hyperplasia.	2007 Apr	19675810
Silodosin, a novel selective alpha 1A-adrenoceptor selective antagonist for the treatment of benign prostatic hyperplasia.	2007 Dec	18042003
Expressions and mechanical functions of alpha1-adrenoceptor subtypes in hamster ureter.	2007 Nov 14	17658513
Alpha1-adrenoceptors and ejaculatory function.	2007 Oct	17603543
Different affinities of native alpha1B-adrenoceptors for ketanserin between intact tissue segments and membrane preparations.	2008 Apr 28	18336813
[Multi-center trial on the early effects of silodosin on lower urinary tract symptoms associated with benign prostatic hyperplasia].	2008 Dec	19174997
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 Feb 2	18078926
Gateways to clinical trials.	2008 Jun	18806898
The involvement of urothelial alpha1A adrenergic receptor in controlling the micturition reflex.	2008 Oct	18997438
Early efficacy of silodosin in patients with lower urinary tract symptoms suggestive of benign prostatic hyperplasia.	2008 Oct	18775032
Ejaculatory dysfunction caused by the new alpha1-blocker silodosin: A preliminary study to analyze human ejaculation using color Doppler ultrasonography.	2008 Oct	18721206
Computational studies of the binding site of alpha1A-adrenoceptor antagonists.	2008 Oct	18626669
Inhibition of Seminal emission is the main cause of anejaculation induced by a new highly selective alpha1A-blocker in normal volunteers.	2008 Sep	18399947
Effects of four different alpha(1)-adrenoceptor antagonists on alpha-adrenoceptor agonist-induced contractions in isolated mouse and hamster ureters.	2009 Aug	19783871
Mechanical function and gene expression of alpha(1)-adrenoceptor subtypes in dog intravesical ureter.	2009 Aug	19371927
Gene expressions and mechanical functions of α1-adrenoceptor subtypes in mouse ureter.	2009 Dec	19259685
Efficacy of alpha-Adrenergic Receptor Blockers in the Treatment of Male Lower Urinary Tract Symptoms.	2009 Fall	20126606
Silodosin (Rapaflo) for benign prostatic hyperplasia.	2009 Jan 12	19122568
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 Jun	19371887
Short- and long-term effects of silodosin, a selective alpha 1A-adrenoceptor antagonist, on ejaculatory function in rats.	2009 Jun	19220259
Effects of silodosin and tamsulosin on the urethra and cardiovascular system in young and old dogs with benign prostatic hyperplasia.	2009 Jun 24	19389393
New drugs: milnacipran hydrochloride, fesoterodine fumarate, and silodosin.	2009 Mar-Apr	19289354
Orgasm is preserved regardless of ejaculatory dysfunction with selective alpha1A-blocker administration.	2009 Sep-Oct	19536124
Urodynamic effects of silodosin, a new alpha 1A-adrenoceptor selective antagonist, for the treatment of benign prostatic hyperplasia.	2010 Apr	19693954
Silodosin for the treatment of benign prostatic hyperplasia: pharmacology and cardiovascular tolerability.	2010 Dec	21114397
Ejaculation disorder is associated with increased efficacy of silodosin for benign prostatic hyperplasia.	2010 Dec	20472263
(RS)-1-[5-(2-Chloro-prop-yl)indolin-1-yl]ethanone.	2010 Dec 8	21522761
Silodosin for benign prostatic hyperplasia.	2010 Feb	20071497
Visualization and tissue distribution of alpha1L-adrenoceptor in human prostate by the fluorescently labeled ligand Alexa-488-silodosin.	2010 Feb	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 Jan	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 Jan	19914658
(RS)-1-(1-Acetyl-indolin-5-yl)-2-chloro-propan-1-one.	2010 Jun 9	21587848
Lack of pharmacodynamic interaction of silodosin, a highly selective alpha1a-adrenoceptor antagonist, with the phosphodiesterase-5 inhibitors sildenafil and tadalafil in healthy men.	2010 Mar	20080287
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 May	20220748
Gateways to clinical trials.	2010 Nov	21225019
Short-term effects of crossover treatment with silodosin and tamsulosin hydrochloride for lower urinary tract symptoms associated with benign prostatic hyperplasia.	2010 Oct	20735791
Role of supraspinal and spinal alpha1-adrenergic receptor subtypes in micturition reflex in conscious rats.	2010 Oct	20668103
Silodosin in the treatment of benign prostatic hyperplasia.	2010 Oct 27	21116335

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 `Wed Jul 05 23:17:41 UTC 2023` Edited by `admin` on `Wed Jul 05 23:17:41 UTC 2023`
Record UNII	CUZ39LUY82
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

SILODOSIN

Official Name

English

RAPAFLO

Brand 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)