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)
Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Solid tumour/cancer 2A00-2F9Z Approved [7]
Progesterone DMUY35B Premature labour JB00 Approved [8]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [9]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [10]
Acetaminophen DMUIE76 Pain MG30-MG3Z Approved [11]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [12]
Etoposide DMNH3PG Solid tumour/cancer 2A00-2F9Z Approved [13]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [14]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [8]
Verapamil DMA7PEW Hypertension BA00-BA04 Approved [15]
⏷ 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 [16]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [17]
Acetaminophen DMUIE76 Pain MG30-MG3Z Approved [18]
Etoposide DMNH3PG Solid tumour/cancer 2A00-2F9Z Approved [19]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [20]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [21]
Mycophenolate mofetil DMPQAGE Organ transplant rejection NE84 Approved [22]
Metronidazole DMTIVEN Amoebiasis 1A36 Approved [5]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [23]
Ethanol DMDRQZU Chronic pain MG30 Approved [24]
⏷ 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 [25]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [26]
Mycophenolate mofetil DMPQAGE Organ transplant rejection NE84 Approved [27]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [28]
Losartan DM72JXH Hypertension BA00-BA04 Approved [15]
Naproxen DMZ5RGV Osteoarthritis FA00-FA05 Approved [29]
Etodolac DM6WJO9 Pain MG30-MG3Z Approved [15]
Bazedoxifene DMY85QW Osteopetrosis LD24.10 Approved [30]
BCP-13498 DM2BO9W Anaesthesia 9A78.6 Phase 2 [31]
⏷ Show the Full List of 9 Drug(s)
Drug(s) Transported By P-glycoprotein 1 (ABCB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Bacterial infection 1A00-1C4Z Approved [32]
Doxorubicin DMVP5YE Solid tumour/cancer 2A00-2F9Z Approved [33]
Methotrexate DM2TEOL leukaemia 2A60-2B33 Approved [34]
Folic acid DMEMBJC Folate-deficiency anemia 3A02.Y Approved [35]
Fluorouracil DMUM7HZ Solid tumour/cancer 2A00-2F9Z Approved [34]
Cisplatin DMRHGI9 Solid tumour/cancer 2A00-2F9Z Approved [34]
Progesterone DMUY35B Premature labour JB00 Approved [36]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [34]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [37]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [38]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Estrogen receptor (ESR)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [39]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [40]
Estrone DM5T6US Menopausal and postmenopausal disorder GA30 Approved [40]
Estradiol valerate DM8MC6O Hormone replacement therapy 8E01 Approved [41]
Estradiol acetate DM07U2A Hormone replacement therapy 8E01 Approved [41]
Estradiol cypionate DM27Z5T Hormone replacement therapy 8E01 Approved [41]
Ethinyl estradiol DMODJ40 Female hypogonadism GA30.6 Approved [42]
Ospemifene DMC4GEI Dyspareunia GA12 Approved [43]
Toremifene DMQYUWG Breast cancer 2C60-2C65 Approved [44]
Mestranol DMG3F94 Contraception QA21 Approved [45]
⏷ 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
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.
4 The role of P-glycoprotein in the bioactivation of raloxifene. Drug Metab Dispos. 2006 Dec;34(12):2073-8.
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 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.
8 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
9 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.
10 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
11 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.
12 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.
13 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
14 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.
15 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.
16 Functional significance of UDP-glucuronosyltransferase variants in the metabolism of active tamoxifen metabolites. Cancer Res. 2009 Mar 1;69(5):1892-900.
17 Functional characterization of human and cynomolgus monkey UDP-glucuronosyltransferase 1A1 enzymes. Life Sci. 2010 Aug 14;87(7-8):261-8.
18 Effect of UDP-glucuronosyltransferase (UGT) 1A polymorphism (rs8330 and rs10929303) on glucuronidation status of acetaminophen. Dose Response. 2017 Sep 11;15(3):1559325817723731.
19 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.
20 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.
21 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.
22 Characterization of rat intestinal microsomal UDP-glucuronosyltransferase activity toward mycophenolic acid. Drug Metab Dispos. 2006 Sep;34(9):1632-9.
23 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.
24 Identification and preliminary characterization of UDP-glucuronosyltransferases catalyzing formation of ethyl glucuronide. Anal Bioanal Chem. 2014 Apr;406(9-10):2325-32.
25 Glucuronidation of active tamoxifen metabolites by the human UDP glucuronosyltransferases. Drug Metab Dispos. 2007 Nov;35(11):2006-14.
26 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.
27 [Pharmacology of mycophenolate mofetil: recent data and clinical consequences]. Nephrologie. 2001;22(7):331-7.
28 Troglitazone glucuronidation in human liver and intestine microsomes: high catalytic activity of UGT1A8 and UGT1A10. Drug Metab Dispos. 2002 Dec;30(12):1462-9.
29 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.
30 In vitro metabolism, permeability, and efflux of bazedoxifene in humans. Drug Metab Dispos. 2010 Sep;38(9):1471-9.
31 UDP-glucuronosyltransferases and clinical drug-drug interactions. Pharmacol Ther. 2005 Apr;106(1):97-132.
32 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
33 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
34 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.
35 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
36 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
37 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
38 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.
39 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.
40 Reprint of Are all estrogens the same Maturitas. 2008 Sep-Oct;61(1-2):195-201.
41 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
42 17alpha-Ethinylestradiol hinders nucleotide excision repair in zebrafish liver cells. Aquat Toxicol. 2009 Dec 13;95(4):273-8.
43 Clinical pipeline report, company report or official report of Shionogi (2011).
44 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.
45 Short-term effects of environmentally relevant concentrations of EDC mixtures on Mytilus galloprovincialis digestive gland. Aquat Toxicol. 2008 May 30;87(4):272-9.