General Information of Drug (ID: DMLT0E1)

Drug Name
Conjugated Estrogens Drug Info
Synonyms
Par Estro; evex; Premarin; Conestoral; NSC18313; Sodium estrone 3-monosulfate; Estrone, hydrogen sulfate sodium salt; AC1NS0NL; NSC-18313; sodium [(8R,9S,13S,14S)-13-methyl-17-oxo-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-yl] hydrogen sulfate; Estra-1,5(10)-trien-17-one, 3-(sulfooxy)-, sodium; Carentil; Congest; Estroplus; Evex; Menotabs; Oestrogen; Prelestrin; Presomil; Progens; Conjugated Equine Estrogens; Conjugated Estrogenic Substances; Conjugated estrogenic hormones; Conjugated oestrogens; Conjugated oestrogens [Steroidal oestrogens]; Steroidal estrogens; ASTA Medica Brand of Estrogens, Conjugated; Almirall Brand of Estrogens, Conjugated; Equine Estrogens, Conjugated; Estro-Feminal; Estrogenic Hormones, Conjugated; Estrogenic substances, conjugated; Estrogens, conjugated USP; Estrogens, conjugated [USP]; Estrogens, conjugated synthetic A; Estrogens, steroidal; Solvay Brand of Estrogens, Conjugated; Trianon Brand of Estrogens, Conjugated; Wyeth Brand of Estrogens, Conjugated; Estrogens, conjugated (USP); Estrogens, conjugated-equine; Mack Brand of Estrogens, Conjugated (USP); Major Brand of Estrogens, Conjugated (USP); Pasadena Brand of Estrogens, Conjugated (USP); Pharmacia Brand of Estrogens, Conjugated (USP); CES; Estra-1,3,5(10)-trien-17-one, 3-(sulfooxy)-, sodium salt; Sodium [(8R,9S,13S,14S)-13-methyl-17-oxo-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-yl] hydrogen sulfate
Indication
Disease Entry ICD 11 Status REF
Dyspareunia GA12 Approved [1]
Hot flushes GA30 Approved [2]
Menopause symptom GA30.0 Approved [3]
Vasomotor symptom CA08 Approved [4]
Therapeutic Class
Estrogens
Cross-matching ID
PubChem CID
45357473
TTD Drug ID
DMLT0E1
VARIDT Drug ID
DR00673
INTEDE Drug ID
DR0377

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Investigative Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Trilostane DMQZ9GF Cushing disease 5A70 Approved [10]
ARZOXIFENE DMOKCVI Breast cancer 2C60-2C65 Approved [11]
Estrogen DMGY0UT Menopause symptom GA30.0 Approved [12]
MF-101 DM8Z0I3 Hepatitis virus infection 1E50-1E51 Phase 3 [13]
Genistein DM0JETC Menopause symptom GA30.0 Phase 2/3 [14]
AUS-131 DMUXO3Z Hot flushes GA30 Phase 2 [15]
ERB-041 DMCEPUA Inflammatory bowel disease DD72 Phase 2 [16]
Erteberel DMU1XZD Prostate hyperplasia GA90 Phase 2 [17]
VG-101 DMAN21O Menopause symptom GA30.0 Phase 1/2 [18]
NARINGENIN DMHAZLM N. A. N. A. Phase 1 [19]
⏷ 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 [20]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [21]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [22]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [23]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [24]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [25]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [26]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [27]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [21]
Verapamil DMA7PEW Angina pectoris BA40 Approved [28]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 1A2 (CYP1A2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [29]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [30]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [31]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [32]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [33]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [34]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [26]
Oxaliplatin DMQNWRD Adenocarcinoma 2D40 Approved [35]
Verapamil DMA7PEW Angina pectoris BA40 Approved [36]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [37]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Beta-glucuronidase (uidA)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Irinotecan DMP6SC2 Adenocarcinoma 2D40 Approved [38]
SN-38G DM2UVNB N. A. N. A. Investigative [39]
Indomethacin glucuronide DMSBENK N. A. N. A. Investigative [40]
Ketoprofen glucuronide DMX2FL3 N. A. N. A. Investigative [41]
Drug(s) Affected By Estrogen receptor (ESR1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [42]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [43]
Gefitinib DM15F0X Colon adenocarcinoma Approved [44]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [45]
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [46]
Liraglutide DM3FXPS Non-insulin dependent diabetes 5A11 Approved [47]
Quercetin DM3NC4M Obesity 5B81 Approved [48]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [49]
Procaine DM4LSNE Anaesthesia 9A78.6 Approved [45]
Estrone DM5T6US Acne vulgaris ED80 Approved [50]
⏷ 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 beta (ESR2) TTOM3J0 ESR2_HUMAN Antagonist [5]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) Main DME DE4LYSA CP3A4_HUMAN Substrate [6]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Substrate [7]
Beta-glucuronidase (uidA) DE9RA0I BGLR_ECOLI Substrate [8]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Estrogen receptor (ESR1) OTKLU61J ESR1_HUMAN Drug Response [9]

References

1 Drugs for menopausal symptoms. Med Lett Drugs Ther. 2020 Aug 10;62(1604):124-128.
2 Raloxifene. Drugs Aging. 1998 Apr;12(4):335-41; discussion 342.
3 ClinicalTrials.gov (NCT01613170) Premarin Versus Toviaz for Treatment of Overactive Bladder. U.S. National Institutes of Health.
4 Roles of hormone replacement therapy and iron in proliferation of breast epithelial cells with different estrogen and progesterone receptor status. Breast. 2008 Apr;17(2):172-9.
5 Differential biochemical and cellular actions of Premarin estrogens: distinct pharmacology of bazedoxifene-conjugated estrogens combination. Mol Endocrinol. 2009 Jan;23(1):74-85.
6 Conjugated oestrogens/bazedoxifene. Aust Prescr. 2017 Jun;40(3):114-115.
7 Effect of conjugated equine estrogens on oxidative metabolism in middle-aged and elderly postmenopausal women. J Clin Pharmacol. 2006 Nov;46(11):1299-307.
8 Long-term administration of conjugated estrogen and bazedoxifene decreased murine fecal beta-glucuronidase activity without impacting overall microbiome community. Sci Rep. 2018 May 25;8(1):8166.
9 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.
10 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
11 Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity. J Med Chem. 2007 May 31;50(11):2682-92.
12 Estrogen inhibits the vascular injury response in estrogen receptor beta-deficient female mice. Proc Natl Acad Sci U S A. 1999 Dec 21;96(26):15133-6.
13 MF101, a selective estrogen receptor beta modulator for the treatment of menopausal hot flushes: a phase II clinical trial. Menopause. 2009 May-Jun;16(3):458-65.
14 Company report (Axcentua)
15 S-equol, a potent ligand for estrogen receptor beta, is the exclusive enantiomeric form of the soy isoflavone metabolite produced by human intestinal bacterial flora. Am J Clin Nutr. 2005 May;81(5):1072-9.
16 Erb-041, an estrogen receptor-beta agonist, inhibits skin photocarcinogenesis in SKH-1 hairless mice by downregulating the WNT signaling pathway. Cancer Prev Res (Phila). 2014 Feb;7(2):186-98.
17 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031986)
18 Update on alternative therapies for vulvovaginal atrophy. Patient Prefer Adherence. 2011; 5: 533-536.
19 Subtle side-chain modifications of the hop phytoestrogen 8-prenylnaringenin result in distinct agonist/antagonist activity profiles for estrogen re... J Med Chem. 2006 Dec 14;49(25):7357-65.
20 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.
21 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
22 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.
23 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
24 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.
25 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.
26 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
27 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.
28 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.
29 Roles of cytochromes P450 1A2, 2A6, and 2C8 in 5-fluorouracil formation from tegafur, an anticancer prodrug, in human liver microsomes. Drug Metab Dispos. 2000 Dec;28(12):1457-63.
30 Effects of polyunsaturated fatty acids on prostaglandin synthesis and cyclooxygenase-mediated DNA adduct formation by heterocyclic aromatic amines in human adenocarcinoma colon cells. Mol Carcinog. 2004 Jul;40(3):180-8.
31 Endoxifen and other metabolites of tamoxifen inhibit human hydroxysteroid sulfotransferase 2A1 (hSULT2A1). Drug Metab Dispos. 2014 Nov;42(11):1843-50.
32 Cytochrome P450 1A2 (CYP1A2) activity and risk factors for breast cancer: a cross-sectional study. Breast Cancer Res. 2004;6(4):R352-65.
33 PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses. Pharmacogenet Genomics. 2015 Aug;25(8):416-26.
34 The effect of apigenin on pharmacokinetics of imatinib and its metabolite N-desmethyl imatinib in rats. Biomed Res Int. 2013;2013:789184.
35 The influence of metabolic gene polymorphisms on urinary 1-hydroxypyrene concentrations in Chinese coke oven workers. Sci Total Environ. 2007 Aug 1;381(1-3):38-46.
36 Identification of P450 enzymes involved in metabolism of verapamil in humans. Naunyn Schmiedebergs Arch Pharmacol. 1993 Sep;348(3):332-7.
37 Metabolism and metabolic inhibition of xanthotoxol in human liver microsomes. Evid Based Complement Alternat Med. 2016;2016:5416509.
38 Involvement of beta-glucuronidase in intestinal microflora in the intestinal toxicity of the antitumor camptothecin derivative irinotecan hydrochloride (CPT-11) in rats. Cancer Res. 1996 Aug 15;56(16):3752-7.
39 Metabolism of irinotecan and its active metabolite SN-38 by intestinal microflora in rats. Oncol Rep. 2008 Oct;20(4):727-30.
40 Bidirectional interactions between indomethacin and the murine intestinal microbiota. Elife. 2015 Dec 23;4:e08973.
41 Bacterial beta-glucuronidase inhibition protects mice against enteropathy induced by indomethacin, ketoprofen or diclofenac: mode of action and pharmacokinetics. Xenobiotica. 2014 Jan;44(1):28-35.
42 Estrogen-like activity of metals in MCF-7 breast cancer cells. Endocrinology. 2003 Jun;144(6):2425-36. doi: 10.1210/en.2002-221054.
43 Cross-talk between non-genomic and genomic signalling pathways--distinct effect profiles of environmental estrogens. Toxicol Appl Pharmacol. 2010 Jun 1;245(2):160-70. doi: 10.1016/j.taap.2010.02.015. Epub 2010 Mar 4.
44 Bidirectional cross talk between ERalpha and EGFR signalling pathways regulates tamoxifen-resistant growth. Breast Cancer Res Treat. 2006 Mar;96(2):131-46. doi: 10.1007/s10549-005-9070-2. Epub 2005 Oct 27.
45 Sensitivity of human dental pulp cells to eighteen chemical agents used for endodontic treatments in dentistry. Odontology. 2013 Jan;101(1):43-51.
46 The dual ErbB1/ErbB2 inhibitor, lapatinib (GW572016), cooperates with tamoxifen to inhibit both cell proliferation- and estrogen-dependent gene expression in antiestrogen-resistant breast cancer. Cancer Res. 2005 Jan 1;65(1):18-25.
47 Antitumoral activity of liraglutide, a new DNMT inhibitor in breast cancer cells in vitro and in vivo. Chem Biol Interact. 2021 Nov 1;349:109641. doi: 10.1016/j.cbi.2021.109641. Epub 2021 Sep 14.
48 Estrogen receptor alpha mediates the proliferative but not the cytotoxic dose-dependent effects of two major phytoestrogens on human breast cancer cells. Mol Pharmacol. 2001 Sep;60(3):595-602.
49 Novel retinoic acid metabolism blocking agents have potent inhibitory activities on human breast cancer cells and tumour growth. Br J Cancer. 2007 Apr 23;96(8):1204-15. doi: 10.1038/sj.bjc.6603705. Epub 2007 Mar 27.
50 Prediction of the combined effects of multiple estrogenic chemicals on MCF-7 human breast cancer cells and a preliminary molecular exploration of the estrogenic proliferative effects and related gene expression. Ecotoxicol Environ Saf. 2018 Sep 30;160:1-9. doi: 10.1016/j.ecoenv.2018.05.025. Epub 2018 May 21.