General Information of Drug (ID: DMOEM2I)

Drug Name
Estriol Drug Info
Synonyms
Aacifemine; Destriol; Estratriol; Estriel; Estriolo; Gynaesan; Hemostyptanon; Holin; Hormomed; Hormonin; Klimoral; Oestratriol; Oestriol; Oestriolum; Orestin; Orgastyptin; Overstin; Ovestin; Ovestrion; Stiptanon; Synapause; Theelol; Thulol; Tridestrin; Trihydroxyestrin; Trihydroxyoestrin; Triodurin; Triovex; Deuslon A; Estriolo [Italian]; Folicular hormone; Follicular hormone hydrate; Oestriol [Steroidal oestrogens]; A 13610; E0218; OE3; Deuslon-A; Estriel (TN); Estriol [USAN:JAN]; Estriol, unconjugated; Ortho-Gynest; Estriol (JP15/USP); Estra-1,3,5(10)-trien-3,16alpha,17beta-triol; Estra-1,3,5(10)-triene-3,16,17-triol; Estra-1,3,5(10)-triene-3,16alpha,17beta-triol; Oestra-1,3,5(10)-triene-3,16alpha,17beta-triol; Oestra-1,3,5(10)-triene-3,16-alpha,17-beta-triol; Estra-1,3,5(10)-trien-3,16.alpha., 17.beta.-triol; Estra-1,3,5(10)-trien-3,16.alpha.,17.beta.-triol; Estra-1,3,5(10)-triene-3,16.alpha., 17.beta.-triol; Estra-1,3,5(10)-triene-3,16.alpha.,17.beta.-triol; Oestra-1,3,5(10)-triene-3,16.alpha., 17.beta.-triol; Oestra-1,3,5(10)-triene-3,16.alpha.,17.beta.-triol; (16.alpha.,17.beta.)-Estra-1,3,5(10)-triene-3,16,17-triol; (16.alpha.,17.beta.)-Oestra-1,3,5(10)-triene-3,16,17-triol; (16alpha,17beta)-Estra-1,3,5(10)-triene-3,16,17-triol; (16alpha,17beta)-Oestra-1,3,5(10)-triene-3,16,17-triol; 1,3,5(10)-ESTRATRIENE-3,16,17-TRIOL; 1,3,5(10)-Estratriene-3,16-alpha,17beta-triol; 1,3,5(10)-Estratriene-3,16.alpha., 17.beta.-triol; 1,3,5(10)-Estratriene-3,16.alpha.,17.beta.-triol; 1,3,5(10)-Estratriene-3,16alpha,17beta-Triol; 1,3,5-Estratriene-3.beta.,16-.alpha.,17-.beta.-triol; 1,3,5-Estratriene-3beta,16alpha,17beta-triol; 1,3,5-Oestratriene-3-.beta.,16.alpha.,17.beta.-triol; 1,3,5-Oestratriene-3beta,16alpha,17beta-triol; 16,17-Epiestriol; 16-Epiestriol; 16-Hydroxyestradiol; 16-alpha,17-beta-Estriol; 16-alpha,17-beta-Oestriol; 16-alpha-Hydroxyestradiol; 16-alpha-Hydroxyoestradiol; 16.alpha.,17.beta.-Estriol; 16.alpha.,17.beta.-Oestriol; 16.alpha.-Estriol; 16.alpha.-Hydroxy-17.beta.-estradiol; 16.alpha.-Hydroxyestradiol; 16.alpha.-Hydroxyoestradiol; 16alpha,17beta-Estriol; 16alpha,17beta-Oestriol; 16alpha-Hydroxy-17beta-estradiol; 16alpha-Hydroxyestradiol; 16alpha-Hydroxyoestradiol; 3,16-alpha,17-beta-Estriol; 3,16-alpha,17-beta-Oestriol; 3,16-alpha,17-beta-Trihydroxy-delta-1,3,5-estratriene; 3,16-alpha,17-beta-Trihydroxy-delta-1,3,5-oestratriene; 3,16-alpha,17-beta-Trihydroxyestra-1,3,5(10)-triene; 3,16-alpha,17-beta-Trihydroxyoestra-1,3,5(10)-triene; 3,16.alpha.,17.beta.-Estriol; 3,16.alpha.,17.beta.-Trihydroxy-.delta.-1,3,5-estratriene; 3,16.alpha.,17.beta.-Trihydroxy-.delta.-1,3,5-oestratriene; 3,16.alpha.,17.beta.-Trihydroxy-1,3,5(10)-estratriene; 3,16.alpha.,17.beta.-Trihydroxyestra-1,3,5(10)-triene; 3,16alpha,17beta-Estriol; 3,16alpha,17beta-Trihydroxy-1,3,5(10)-estratriene; 3,16alpha,17beta-Trihydroxy-delta-1,3,5-oestratriene; 3,16alpha,17beta-trihydroxy-Delta(1,3,5)-estratriene
Indication
Disease Entry ICD 11 Status REF
Hormone deficiency 5A61.1 Approved [1] , [2] , [3]
Multiple sclerosis 8A40 Phase 2 [4]
Therapeutic Class
Estrogens
Cross-matching ID
PubChem CID
5756
ChEBI ID
CHEBI:27974
CAS Number
CAS 50-27-1
TTD Drug ID
DMOEM2I
VARIDT Drug ID
DR01435
INTEDE Drug ID
DR0646

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
Drug Status:
Approved Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [9]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [10]
Acetaminophen DMUIE76 Pain MG30-MG3Z Approved [11]
Etoposide DMNH3PG Solid tumour/cancer 2A00-2F9Z Approved [12]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [13]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [14]
Mycophenolate mofetil DMPQAGE Organ transplant rejection NE84 Approved [15]
Metronidazole DMTIVEN Amoebiasis 1A36 Approved [16]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [17]
Ethanol DMDRQZU Chronic pain MG30 Approved [18]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A7 (CYP3A7)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Progesterone DMUY35B Premature labour JB00 Approved [19]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [20]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [20]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [20]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [21]
Verapamil DMA7PEW Hypertension BA00-BA04 Approved [22]
Sorafenib DMS8IFC Hepatocellular carcinoma 2C12.02 Approved [20]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [20]
Irinotecan DMP6SC2 Colorectal cancer 2B91.Z Approved [20]
Metronidazole DMTIVEN Amoebiasis 1A36 Approved [23]
⏷ 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 Bacterial infection 1A00-1C4Z Approved [24]
Doxorubicin DMVP5YE Solid tumour/cancer 2A00-2F9Z Approved [25]
Methotrexate DM2TEOL leukaemia 2A60-2B33 Approved [26]
Folic acid DMEMBJC Folate-deficiency anemia 3A02.Y Approved [27]
Fluorouracil DMUM7HZ Solid tumour/cancer 2A00-2F9Z Approved [26]
Cisplatin DMRHGI9 Solid tumour/cancer 2A00-2F9Z Approved [26]
Progesterone DMUY35B Premature labour JB00 Approved [28]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [26]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [29]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [30]
⏷ 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 [31]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [5]
Estrone DM5T6US Menopausal and postmenopausal disorder GA30 Approved [5]
Estradiol valerate DM8MC6O Hormone replacement therapy 8E01 Approved [32]
Estradiol acetate DM07U2A Hormone replacement therapy 8E01 Approved [32]
Estradiol cypionate DM27Z5T Hormone replacement therapy 8E01 Approved [32]
Ethinyl estradiol DMODJ40 Female hypogonadism GA30.6 Approved [33]
Raloxifene DMDKF3M Osteoporosis FB83.0 Approved [34]
Ospemifene DMC4GEI Dyspareunia GA12 Approved [35]
Toremifene DMQYUWG Breast cancer 2C60-2C65 Approved [36]
⏷ 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 Agonist [5]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [6]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Substrate [7]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Substrate [8]

References

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2 Drug information of Estriol, 2008. eduDrugs.
3 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
4 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026520)
5 Reprint of Are all estrogens the same Maturitas. 2008 Sep-Oct;61(1-2):195-201.
6 P-glycoprotein (P-gp/MDR1)-mediated efflux of sex-steroid hormones and modulation of P-gp expression in vitro. Pharm Res. 2004 Jul;21(7):1284-93.
7 Stimulation of microsomal uridine diphosphate glucuronyltransferase by glucuronic acid derivatives. Biochem J. 1974 Apr;139(1):243-9.
8 Expression and cyclic variability of CYP3A4 and CYP3A7 isoforms in human endometrium and cervix during the menstrual cycle. Drug Metab Dispos. 2003 Jan;31(1):1-6.
9 Functional significance of UDP-glucuronosyltransferase variants in the metabolism of active tamoxifen metabolites. Cancer Res. 2009 Mar 1;69(5):1892-900.
10 Functional characterization of human and cynomolgus monkey UDP-glucuronosyltransferase 1A1 enzymes. Life Sci. 2010 Aug 14;87(7-8):261-8.
11 Effect of UDP-glucuronosyltransferase (UGT) 1A polymorphism (rs8330 and rs10929303) on glucuronidation status of acetaminophen. Dose Response. 2017 Sep 11;15(3):1559325817723731.
12 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.
13 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.
14 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.
15 Characterization of rat intestinal microsomal UDP-glucuronosyltransferase activity toward mycophenolic acid. Drug Metab Dispos. 2006 Sep;34(9):1632-9.
16 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.
17 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.
18 Identification and preliminary characterization of UDP-glucuronosyltransferases catalyzing formation of ethyl glucuronide. Anal Bioanal Chem. 2014 Apr;406(9-10):2325-32.
19 The role of cytochrome P450 3A (CYP3A) isoform(s) in oxidative metabolism of testosterone and benzphetamine in human adult and fetal liver. J Steroid Biochem Mol Biol. 1993 Jan;44(1):61-7.
20 Drug Interactions Flockhart Table
21 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
22 Prediction of cytochrome P450 3A inhibition by verapamil enantiomers and their metabolites. Drug Metab Dispos. 2004 Feb;32(2):259-66.
23 The role of human cytochrome P450 enzymes in the formation of 2-hydroxymetronidazole: CYP2A6 is the high affinity (low Km) catalyst. Drug Metab Dispos. 2013 Sep;41(9):1686-94.
24 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
25 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
26 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.
27 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
28 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
29 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
30 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.
31 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.
32 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
33 17alpha-Ethinylestradiol hinders nucleotide excision repair in zebrafish liver cells. Aquat Toxicol. 2009 Dec 13;95(4):273-8.
34 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).
35 Clinical pipeline report, company report or official report of Shionogi (2011).
36 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.