Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMDKF3M)

Drug Name
Raloxifene Drug Info
Synonyms Raloxifene (extended-release, CDT)
Indication
Disease Entry ICD 11 Status REF
Osteoporosis FB83.0 Approved [1]
Cross-matching ID
PubChem CID
5035
ChEBI ID
CHEBI:8772
CAS Number
CAS 84449-90-1
TTD Drug ID
DMDKF3M
VARIDT Drug ID
DR01347
INTEDE Drug ID
DR1388
ACDINA Drug ID
D00579

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Download the Complete Related Drug List
Drug(s) Targeting Estrogen receptor (ESR)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [7]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [8]
Estrone DM5T6US Acne vulgaris ED80 Approved [8]
Estradiol Valerate DM8MC6O Hormone replacement therapy 8E01 Approved [9]
Estradiol Acetate DM07U2A Hormone replacement therapy 8E01 Approved [9]
Estradiol Cypionate DM27Z5T Hormone replacement therapy 8E01 Approved [9]
Ethinyl Estradiol DMODJ40 Acne vulgaris ED80 Approved [10]
Ospemifene DMC4GEI Dyspareunia GA12 Approved [11]
Toremifene DMQYUWG Breast cancer 2C60-2C65 Approved [12]
Mestranol DMG3F94 Contraception QA21 Approved [13]
⏷ 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 [14]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [15]
Methotrexate DM2TEOL Anterior urethra cancer Approved [16]
Folic Acid DMEMBJC Colorectal carcinoma Approved [17]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [16]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [16]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [18]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [16]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [19]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [20]
⏷ Show the Full List of 10 Drug(s)
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 [21]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [22]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [23]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [24]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [25]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [26]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [27]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [28]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [22]
Verapamil DMA7PEW Angina pectoris BA40 Approved [29]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By UDP-glucuronosyltransferase 1A1 (UGT1A1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [30]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [31]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [32]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [33]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [34]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [35]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [36]
Metronidazole DMTIVEN Abscess Approved [5]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [37]
Ethanol DMDRQZU Chronic pain MG30 Approved [38]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By UDP-glucuronosyltransferase 1A10 (UGT1A10)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [39]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [40]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [41]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [42]
Losartan DM72JXH Diabetic kidney disease GB61.Z Approved [29]
Naproxen DMZ5RGV Bursitis Approved [43]
Etodolac DM6WJO9 Osteoarthritis FA00-FA05 Approved [29]
Bazedoxifene DMY85QW Hot flushes GA30 Approved [44]
BCP-13498 DM2BO9W N. A. N. A. Phase 2 [45]
⏷ Show the Full List of 9 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas
Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Estrogen receptor (ESR) TTZAYWL ESR1_HUMAN Modulator [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [4]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Substrate [5]
UDP-glucuronosyltransferase 1A10 (UGT1A10) DEL5N6Y UD110_HUMAN Substrate [6]

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
2 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. (Target id: 620).
3 Influence of hepatic and intestinal efflux transporters and their genetic variants on the pharmacokinetics and pharmacodynamics of raloxifene in osteoporosis treatment. Transl Res. 2012 Oct;160(4):298-308.
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5 Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios. Drug Metab Dispos. 2004 Nov;32(11):1201-8.
6 Characterization of raloxifene glucuronidation: potential role of UGT1A8 genotype on raloxifene metabolism in vivo. Cancer Prev Res (Phila). 2013 Jul;6(7):719-30.
7 Modulators of vascular sex hormone receptors and their effects in estrogen-deficiency states associated with menopause. Recent Pat Cardiovasc Drug Discov. 2008 Nov;3(3):165-86.
8 Reprint of Are all estrogens the same Maturitas. 2008 Sep-Oct;61(1-2):195-201.
9 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
10 17alpha-Ethinylestradiol hinders nucleotide excision repair in zebrafish liver cells. Aquat Toxicol. 2009 Dec 13;95(4):273-8.
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12 Effect of selective estrogen receptor modulators on cell proliferation and estrogen receptor activities in normal human prostate stromal and epithe... Prostate Cancer Prostatic Dis. 2009;12(4):375-81.
13 Short-term effects of environmentally relevant concentrations of EDC mixtures on Mytilus galloprovincialis digestive gland. Aquat Toxicol. 2008 May 30;87(4):272-9.
14 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
15 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
16 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.
17 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
18 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
19 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
20 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.
21 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.
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23 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.
24 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
25 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.
26 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.
27 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
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29 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.
30 Functional significance of UDP-glucuronosyltransferase variants in the metabolism of active tamoxifen metabolites. Cancer Res. 2009 Mar 1;69(5):1892-900.
31 Functional characterization of human and cynomolgus monkey UDP-glucuronosyltransferase 1A1 enzymes. Life Sci. 2010 Aug 14;87(7-8):261-8.
32 Effect of UDP-glucuronosyltransferase (UGT) 1A polymorphism (rs8330 and rs10929303) on glucuronidation status of acetaminophen. Dose Response. 2017 Sep 11;15(3):1559325817723731.
33 UDP-glucuronosyltransferase 1A1 is the principal enzyme responsible for etoposide glucuronidation in human liver and intestinal microsomes: structural characterization of phenolic and alcoholic glucuronides of etoposide and estimation of enzyme kinetics. Drug Metab Dispos. 2007 Mar;35(3):371-80.
34 Interindividual variability in pharmacokinetics of generic nucleoside reverse transcriptase inhibitors in TB/HIV-coinfected Ghanaian patients: UGT2B7*1c is associated with faster zidovudine clearance and glucuronidation. J Clin Pharmacol. 2009 Sep;49(9):1079-90.
35 Effect of aging on glucuronidation of valproic acid in human liver microsomes and the role of UDP-glucuronosyltransferase UGT1A4, UGT1A8, and UGT1A10. Drug Metab Dispos. 2009 Jan;37(1):229-36.
36 Characterization of rat intestinal microsomal UDP-glucuronosyltransferase activity toward mycophenolic acid. Drug Metab Dispos. 2006 Sep;34(9):1632-9.
37 Substrate-dependent modulation of UDP-glucuronosyltransferase 1A1 (UGT1A1) by propofol in recombinant human UGT1A1 and human liver microsomes. Basic Clin Pharmacol Toxicol. 2007 Sep;101(3):211-4.
38 Identification and preliminary characterization of UDP-glucuronosyltransferases catalyzing formation of ethyl glucuronide. Anal Bioanal Chem. 2014 Apr;406(9-10):2325-32.
39 Glucuronidation of active tamoxifen metabolites by the human UDP glucuronosyltransferases. Drug Metab Dispos. 2007 Nov;35(11):2006-14.
40 UDP glucuronosyltransferase (UGT) 1A6 pharmacogenetics: II. Functional impact of the three most common nonsynonymous UGT1A6 polymorphisms (S7A, T181A, and R184S). J Pharmacol Exp Ther. 2005 Jun;313(3):1340-6.
41 [Pharmacology of mycophenolate mofetil: recent data and clinical consequences]. Nephrologie. 2001;22(7):331-7.
42 Troglitazone glucuronidation in human liver and intestine microsomes: high catalytic activity of UGT1A8 and UGT1A10. Drug Metab Dispos. 2002 Dec;30(12):1462-9.
43 S-Naproxen and desmethylnaproxen glucuronidation by human liver microsomes and recombinant human UDP-glucuronosyltransferases (UGT): role of UGT2B7 in the elimination of naproxen. Br J Clin Pharmacol. 2005 Oct;60(4):423-33.
44 In vitro metabolism, permeability, and efflux of bazedoxifene in humans. Drug Metab Dispos. 2010 Sep;38(9):1471-9.
45 UDP-glucuronosyltransferases and clinical drug-drug interactions. Pharmacol Ther. 2005 Apr;106(1):97-132.