Details of the Drug
General Information of Drug (ID: DMJSBT6)
Drug Name |
Silodosin
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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
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Indication |
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Drug Type |
Small molecular drug
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Structure | ||||||||||||||||||||
3D MOL | 2D MOL | |||||||||||||||||||
#Ro5 Violations (Lipinski): 1 | Molecular Weight (mw) | 495.5 | ||||||||||||||||||
Topological Polar Surface Area (xlogp) | 3.6 | |||||||||||||||||||
Rotatable Bond Count (rotbonds) | 13 | |||||||||||||||||||
Hydrogen Bond Donor Count (hbonddonor) | 3 | |||||||||||||||||||
Hydrogen Bond Acceptor Count (hbondacc) | 9 | |||||||||||||||||||
ADMET Property |
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Chemical Identifiers |
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Cross-matching ID | ||||||||||||||||||||
Molecular Interaction Atlas of This Drug
Drug Therapeutic Target (DTT) |
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Drug Transporter (DTP) |
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Drug-Metabolizing Enzyme (DME) |
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Molecular Interaction Atlas (MIA) | ||||||||||||||||||||||||||||||||||||||||||
Molecular Expression Atlas of This Drug
The Studied Disease | Benign prostatic hyperplasia | |||||||||||||||||||||||||||||||||||||||||||||||||||||
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ICD Disease Classification | GA90 | |||||||||||||||||||||||||||||||||||||||||||||||||||||
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Molecular Expression Atlas (MEA) | ||||||||||||||||||||||||||||||||||||||||||||||||||||||
Drug-Drug Interaction (DDI) Information of This Drug
Coadministration of a Drug Treating the Disease Different from Silodosin (Comorbidity)
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Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug
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 | 2008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6. | ||||
3 | Silodosin: a selective alpha1A-adrenergic receptor antagonist for the treatment of benign prostatic hyperplasia. Clin Ther. 2009 Nov;31(11):2489-502. | ||||
4 | FDA Approved Drug Products: RAPAFLO (silodosin) Capsule for oral use | ||||
5 | Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose | ||||
6 | Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds | ||||
7 | Pharmacophore identification of alpha(1A)-adrenoceptor antagonists. Bioorg Med Chem Lett. 2005 Feb 1;15(3):657-64. | ||||
8 | Pharmacokinetics and disposition of silodosin (KMD-3213)]. Yakugaku Zasshi. 2006 Mar;126 Spec no.:237-45. | ||||
9 | 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. | ||||
10 | Silodosin for benign prostatic hyperplasia. Ann Pharmacother. 2010 Feb;44(2):302-10. | ||||
11 | Pharmacokinetics and disposition of silodosin (KMD-3213). Yakugaku Zasshi. 2006 Mar;126 Spec no.:237-45. | ||||
12 | 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. | ||||
13 | Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47. | ||||
14 | 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. | ||||
15 | Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9. | ||||
16 | 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. | ||||
17 | 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. | ||||
18 | Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6. | ||||
19 | 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. | ||||
20 | 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. | ||||
21 | Metabolism and transport of tamoxifen in relation to its effectiveness: new perspectives on an ongoing controversy. Future Oncol. 2014 Jan;10(1):107-22. | ||||
22 | 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. | ||||
23 | 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. | ||||
24 | PharmGKB summary: mycophenolic acid pathway. Pharmacogenet Genomics. 2014 Jan;24(1):73-9. | ||||
25 | Pitavastatin: a review in hypercholesterolemia. Am J Cardiovasc Drugs. 2017 Apr;17(2):157-168. | ||||
26 | Troglitazone glucuronidation in human liver and intestine microsomes: high catalytic activity of UGT1A8 and UGT1A10. Drug Metab Dispos. 2002 Dec;30(12):1462-9. | ||||
27 | Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions. Clin Pharmacokinet. 2005;44(5):467-94. | ||||
28 | Pharmacogenomics of statins: understanding susceptibility to adverse effects. Pharmgenomics Pers Med. 2016 Oct 3;9:97-106. | ||||
29 | 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. | ||||
30 | 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. | ||||
31 | Paraldehyde. J Appl Toxicol. 1991 Oct;11(5):379-81. | ||||
32 | OSHA Occupational Chemical Database: drug information. | ||||
33 | Natural alcohol exposure: is ethanol the main substrate for alcohol dehydrogenases in animals? Chem Biol Interact. 2011 May 30;191(1-3):14-25. | ||||
34 | Conformational changes and catalysis by alcohol dehydrogenase. Arch Biochem Biophys. 2010 Jan 1;493(1):3-12. | ||||
35 | Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007. | ||||
36 | MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8. | ||||
37 | 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. | ||||
38 | Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31. | ||||
39 | Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8. | ||||
40 | Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92. | ||||
41 | 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. | ||||
42 | 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. | ||||
43 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | ||||
44 | Pharma & Vaccines. Product Development Pipeline. April 29 2009. | ||||
45 | Clinical pipeline report, company report or official report of GlaxoSmithKline (2009). | ||||
46 | 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. | ||||
47 | 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. | ||||
48 | 5-HT1A receptor ligands and their therapeutic applications: review of new patents.Expert Opin Ther Pat. 2018 Sep;28(9):679-689. | ||||
49 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. J Med Chem. 1996 Jan 5;39(1):143-8. | ||||
50 | 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. | ||||
51 | Cerner Multum, Inc. "Australian Product Information.". | ||||
52 | Cerner Multum, Inc. "UK Summary of Product Characteristics.". | ||||
53 | Product Information. Balversa (erdafitinib). Janssen Products, LP, Horsham, PA. | ||||
54 | Product Information. Rapaflo (silodosin). Watson Pharmaceuticals, Corona, CA. | ||||
55 | Aronowitz JS, Chakos MH, Safferman AZ, Lieberman JA "Syncope associated with the combination of clozapine and enalapril." J Clin Psychopharmacol 14 (1994): 429-30. [PMID: 7884028] | ||||
56 | Chrysant SG "Experience with terazosin administered in combination with other antihypertensive agents." Am J Med 80 (1986): 55-61. [PMID: 2872808] | ||||
57 | Product Information. Harvoni (ledipasvir-sofosbuvir). Gilead Sciences, Foster City, CA. | ||||
58 | Product Information. Juxtapid (lomitapide). Aegerion Pharmaceuticals Inc, Cambridge, MA. | ||||
59 | Product Information. Tabrecta (capmatinib). Novartis Pharmaceuticals, East Hanover, NJ. | ||||
60 | Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN. | ||||
61 | Ban TA "Drug interactions with psychoactive drugs." Dis Nerv Syst 36 (1975): 164-6. [PMID: 1116424] | ||||
62 | Product Information. Varubi (rolapitant). Tesaro Inc., Waltham, MA. | ||||
63 | Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ. | ||||
64 | Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA. | ||||
65 | Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA. | ||||