General Information of Drug (ID: DMJSBT6)

Drug Name
SILODOSIN Drug Info
Synonyms
Silodosin; 160970-54-7; Rapaflo; Urief; Silodyx; Urorec; KMD-3213; Silodosin-d6; UNII-CUZ39LUY82; KMD 3213; KAD 3213; CUZ39LUY82; CHEMBL24778; KAD-3213; (R)-1-(3-hydroxypropyl)-5-(2-((2-(2-(2,2,2-trifluoroethoxy)phenoxy)ethyl)amino)propyl)indoline-7-carboxamide; 1-(3-hydroxypropyl)-5-[(2R)-2-[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethylamino]propyl]-2,3-dihydroindole-7-carboxamide; 160970-64-9; Q-102517; Rapflo
Indication
Disease Entry ICD 11 Status REF
Benign prostatic hyperplasia GA90 Approved [1]
Cross-matching ID
PubChem CID
5312125
ChEBI ID
CHEBI:135929
CAS Number
CAS 160970-54-7
TTD Drug ID
DMJSBT6
VARIDT Drug ID
DR00285
INTEDE Drug ID
DR1482
ACDINA Drug ID
D01426

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Discontinued Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
NAFTOPIDIL DMQ8R4E Hypertension BA00-BA04 Approved [2]
Tamsulosin DM5QF9V Benign prostatic hyperplasia GA90 Approved [8]
Xatral DMLHOA0 Benign prostatic hyperplasia GA90 Approved [9]
Dutasteride + tamsulosin DM6P8HU Benign prostatic hyperplasia GA90 Phase 3 [10]
Besipirdine DMLVNTA Cognitive impairment 6D71 Phase 3 [11]
MEDETOMIDINE DMX9Y7V Pain MG30-MG3Z Phase 2 [12]
PMID30124346-Compound-LDT8 DM5MUNG Benign prostatic hyperplasia GA90 Patented [13]
PMID30124346-Compound-LDT66 DMJMTNL Benign prostatic hyperplasia GA90 Patented [13]
TIOSPIRONE DME5QDP N. A. N. A. Discontinued in Phase 3 [14]
Sunepitron DM6M8ZX N. A. N. A. Discontinued in Phase 3 [15]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By P-glycoprotein 1 (ABCB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Acute otitis media AB00 Approved [16]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [17]
Methotrexate DM2TEOL Anterior urethra cancer Approved [18]
Folic Acid DMEMBJC Colorectal carcinoma Approved [19]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [18]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [18]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [20]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [18]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [21]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [22]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Verapamil DMA7PEW Angina pectoris BA40 Approved [23]
Digoxin DMQCTIH Arrhythmia BC9Z Approved [23]
Vinblastine DM5TVS3 Advanced cancer 2A00-2F9Z Approved [23]
Paclitaxel DMLB81S Breast carcinoma Approved [23]
Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [24]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [25]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [26]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [27]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [28]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [29]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [30]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [31]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [25]
Verapamil DMA7PEW Angina pectoris BA40 Approved [32]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [33]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [34]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [32]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [35]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [36]
Ibuprofen DM8VCBE Dysmenorrhea GA34.3 Approved [32]
PITAVASTATIN CALCIUM DM1UJO0 Dyslipidemia 5C80-5C81 Approved [37]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [38]
Ezetimibe DM7A8TW Atherosclerosis BD40 Approved [39]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [40]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Aldehyde dehydrogenase 2 (ALDH2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Benzyl alcohol DMBVYDI Head and body lice 1G00.0 Approved [41]
Amyl nitrite DMJKO05 Angina pectoris BA40 Approved [42]
Paraldehyde DMOC1BX Insomnia 7A00-7A0Z Approved [43]
Pentaerythritol tetranitrate DMZ9MO5 Angina pectoris BA40 Approved [44]
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ethanol DMDRQZU Chronic pain MG30 Approved [45]
NADH DM5NM6E Parkinson disease 8A00.0 Approved [46]
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tamsulosin DM5QF9V Benign prostatic hyperplasia GA90 Approved [47]
Gabapentin DM6T924 Complex partial seizure 8A68.0 Approved [48]
Verapamil DMA7PEW Angina pectoris BA40 Approved [49]
Epinephrine DM3KJBC Acute asthma CA23 Approved [7]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [50]
Oxymetazoline DM8ZXT6 Arrhythmia BC9Z Approved [47]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [51]
Quinidine DMLPICK N. A. N. A. Approved [49]
Norepinephrine DMOUC09 Alopecia ED70 Approved [52]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [53]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Adrenergic receptor alpha-1A (ADRA1A) TTNGILX ADA1A_HUMAN Inhibitor [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Multidrug resistance protein 3 (ABCB4) DTZRMK5 MDR3_HUMAN Substrate [3]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [4]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [5]
UDP-glucuronosyltransferase 2B7 (UGT2B7) Main DME DEB3CV1 UD2B7_HUMAN Substrate [6]
Alcohol dehydrogenase class-I alpha (ADH1A) DEE5M8O ADH1A_HUMAN Substrate [6]
Aldehyde dehydrogenase 2 (ALDH2) DEWYTJB ALDH2_HUMAN Substrate [6]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Alpha-1A adrenergic receptor (ADRA1A) OTUIWCL5 ADA1A_HUMAN Protein Interaction/Cellular Processes [7]

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 493).
2 Pharmacophore identification of alpha(1A)-adrenoceptor antagonists. Bioorg Med Chem Lett. 2005 Feb 1;15(3):657-64.
3 Pharmacokinetics and disposition of silodosin (KMD-3213)]. Yakugaku Zasshi. 2006 Mar;126 Spec no.:237-45.
4 The influence of UGT2B7, UGT1A8, MDR1, ALDH, ADH, CYP3A4 and CYP3A5 genetic polymorphisms on the pharmacokinetics of silodosin in healthy Chinese volunteers. Drug Metab Pharmacokinet. 2013;28(3):239-43.
5 Silodosin for benign prostatic hyperplasia. Ann Pharmacother. 2010 Feb;44(2):302-10.
6 Pharmacokinetics and disposition of silodosin (KMD-3213). Yakugaku Zasshi. 2006 Mar;126 Spec no.:237-45.
7 Carvedilol selectively inhibits oscillatory intracellular calcium changes evoked by human alpha1D- and alpha1B-adrenergic receptors. Cardiovasc Res. 2004 Sep 1;63(4):662-72. doi: 10.1016/j.cardiores.2004.05.014.
8 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
9 Pharma & Vaccines. Product Development Pipeline. April 29 2009.
10 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
11 Alpha-Adrenergic activity and cardiovascular effects of besipirdine HCl (HP 749) and metabolite P7480 in vitro and in the conscious rat and dog. J Pharmacol Exp Ther. 1997 Apr;281(1):337-46.
12 A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic recep... J Med Chem. 1994 Jul 22;37(15):2328-33.
13 5-HT1A receptor ligands and their therapeutic applications: review of new patents.Expert Opin Ther Pat. 2018 Sep;28(9):679-689.
14 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. J Med Chem. 1996 Jan 5;39(1):143-8.
15 An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment o... J Med Chem. 2006 Jun 1;49(11):3116-35.
16 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
17 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
18 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
19 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
20 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
21 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
22 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
23 MDR3 P-glycoprotein, a phosphatidylcholine translocase, transports several cytotoxic drugs and directly interacts with drugs as judged by interference with nucleotide trapping. J Biol Chem. 2000 Aug 4;275(31):23530-9.
24 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
25 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
26 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
27 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
28 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
29 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
30 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
31 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
32 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
33 Metabolism and transport of tamoxifen in relation to its effectiveness: new perspectives on an ongoing controversy. Future Oncol. 2014 Jan;10(1):107-22.
34 Determination of UDP-glucuronosyltransferase UGT2B7 activity in human liver microsomes by ultra-performance liquid chromatography with MS detection. J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Jul 1;870(1):84-90.
35 Pharmacokinetic and pharmacodynamic interaction of lorazepam and valproic acid in relation to UGT2B7 genetic polymorphism in healthy subjects. Clin Pharmacol Ther. 2008 Apr;83(4):595-600.
36 PharmGKB summary: mycophenolic acid pathway. Pharmacogenet Genomics. 2014 Jan;24(1):73-9.
37 Pitavastatin: a review in hypercholesterolemia. Am J Cardiovasc Drugs. 2017 Apr;17(2):157-168.
38 Troglitazone glucuronidation in human liver and intestine microsomes: high catalytic activity of UGT1A8 and UGT1A10. Drug Metab Dispos. 2002 Dec;30(12):1462-9.
39 Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions. Clin Pharmacokinet. 2005;44(5):467-94.
40 Pharmacogenomics of statins: understanding susceptibility to adverse effects. Pharmgenomics Pers Med. 2016 Oct 3;9:97-106.
41 Effects of ALDH2, CYP1A1, and CYP2E1 genetic polymorphisms and smoking and drinking habits on toluene metabolism in humans. Toxicol Appl Pharmacol. 1995 Aug;133(2):295-304.
42 Mitochondrial aldehyde dehydrogenase mediates vasodilator responses of glyceryl trinitrate and sodium nitrite in the pulmonary vascular bed of the rat. Am J Physiol Heart Circ Physiol. 2010 Sep;299(3):H819-26.
43 Paraldehyde. J Appl Toxicol. 1991 Oct;11(5):379-81.
44 OSHA Occupational Chemical Database: drug information.
45 Natural alcohol exposure: is ethanol the main substrate for alcohol dehydrogenases in animals? Chem Biol Interact. 2011 May 30;191(1-3):14-25.
46 Conformational changes and catalysis by alcohol dehydrogenase. Arch Biochem Biophys. 2010 Jan 1;493(1):3-12.
47 Cell membrane chromatography competitive binding analysis for characterization of 1A adrenoreceptor binding interactions. Anal Bioanal Chem. 2011 Jul;400(10):3625-33. doi: 10.1007/s00216-011-5026-z. Epub 2011 May 5.
48 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
49 Effects of quinidine and verapamil on human cardiovascular alpha1-adrenoceptors. Circulation. 1998 Apr 7;97(13):1227-30. doi: 10.1161/01.cir.97.13.1227.
50 Adipogenic Effects and Gene Expression Profiling of Firemaster? 550 Components in Human Primary Preadipocytes. Environ Health Perspect. 2017 Sep 14;125(9):097013. doi: 10.1289/EHP1318.
51 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
52 The alpha 1-adrenergic receptor that mediates smooth muscle contraction in human prostate has the pharmacological properties of the cloned human alpha 1c subtype. Mol Pharmacol. 1994 Apr;45(4):703-8.
53 Multiple microRNAs function as self-protective modules in acetaminophen-induced hepatotoxicity in humans. Arch Toxicol. 2018 Feb;92(2):845-858.