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

General Information of Drug (ID: DM6NTAS)

Drug Name
ERA-923 Drug Info
Synonyms
Pipendoxifene; UNII-TPC5Q8496G; 198480-55-6; CHEMBL44426; TPC5Q8496G; Pipendoxifene [INN]; ERA 923; AC1O5FKF; SCHEMBL134583; JICOGKJOQXTAIP-UHFFFAOYSA-N; ZINC602799; BDBM50099587; AKOS030631784; DB05414; 2-(4-hydroxyphenyl)-3-methyl-1-(4-(2-piperidin-1-yl-ethoxy)-benzyl)-1H-indol-5-ol; US8815934, No 97; US8815934, No 107; 2-(p-Hydroxyphenyl)-3-methyl-1-(p-(2-piperidinoethoxy)benzyl)indol-5-ol; 2-(4-hydroxyphenyl)-3-methyl-1-[[4-(2-piperidin-1-ylethoxy)phenyl]methyl]indol-5-ol
Indication
Disease Entry ICD 11 Status REF
Breast cancer 2C60-2C65 Discontinued in Phase 2 [1]
Cross-matching ID
PubChem CID
6433099
CAS Number
CAS 198480-55-6
TTD Drug ID
DM6NTAS

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Download the Complete Related Drug List
Drug(s) Targeting Estrogen receptor beta (ESR2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Conjugated Estrogens DMLT0E1 Dyspareunia GA12 Approved [4]
Trilostane DMQZ9GF Cushing disease 5A70 Approved [5]
ARZOXIFENE DMOKCVI Breast cancer 2C60-2C65 Approved [6]
Estrogen DMGY0UT Menopause symptom GA30.0 Approved [7]
MF-101 DM8Z0I3 Hepatitis virus infection 1E50-1E51 Phase 3 [8]
Genistein DM0JETC Menopause symptom GA30.0 Phase 2/3 [9]
AUS-131 DMUXO3Z Hot flushes GA30 Phase 2 [10]
ERB-041 DMCEPUA Inflammatory bowel disease DD72 Phase 2 [11]
Erteberel DMU1XZD Prostate hyperplasia GA90 Phase 2 [12]
VG-101 DMAN21O Menopause symptom GA30.0 Phase 1/2 [13]
⏷ 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 [14]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [15]
Estrone DM5T6US Acne vulgaris ED80 Approved [15]
Estradiol Valerate DM8MC6O Hormone replacement therapy 8E01 Approved [5]
Estradiol Acetate DM07U2A Hormone replacement therapy 8E01 Approved [5]
Estradiol Cypionate DM27Z5T Hormone replacement therapy 8E01 Approved [5]
Ethinyl Estradiol DMODJ40 Acne vulgaris ED80 Approved [16]
Raloxifene DMDKF3M Osteoporosis FB83.0 Approved [17]
Ospemifene DMC4GEI Dyspareunia GA12 Approved [18]
Toremifene DMQYUWG Breast cancer 2C60-2C65 Approved [19]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Retinoblastoma-associated protein (RB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Indomethacin DMSC4A7 Bursitis Approved [20]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [21]
Gefitinib DM15F0X Colon adenocarcinoma Approved [22]
Talazoparib DM1KS78 Breast cancer 2C60-2C65 Approved [23]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [24]
Trametinib DM2JGQ3 Melanoma 2C30 Approved [25]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [26]
Methotrexate DM2TEOL Anterior urethra cancer Approved [27]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [28]
Quercetin DM3NC4M Obesity 5B81 Approved [29]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Ribosomal protein S6 kinase beta-1 (RPS6KB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dexamethasone DMMWZET Acute adrenal insufficiency Approved [30]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [31]
Gefitinib DM15F0X Colon adenocarcinoma Approved [32]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [33]
Trametinib DM2JGQ3 Melanoma 2C30 Approved [25]
Quercetin DM3NC4M Obesity 5B81 Approved [34]
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [35]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [36]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [37]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [38]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By G1/S-specific cyclin-D1 (CCND1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Indomethacin DMSC4A7 Bursitis Approved [39]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [40]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [41]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [42]
Gefitinib DM15F0X Colon adenocarcinoma Approved [43]
Talazoparib DM1KS78 Breast cancer 2C60-2C65 Approved [23]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [44]
Selenium DM25CGV N. A. N. A. Approved [45]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [46]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [47]
⏷ Show the Full List of 10 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 Inhibitor [2]
Estrogen receptor beta (ESR2) TTOM3J0 ESR2_HUMAN Inhibitor [3]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
G1/S-specific cyclin-D1 (CCND1) OT8HPTKJ CCND1_HUMAN Gene/Protein Processing [2]
Retinoblastoma-associated protein (RB1) OTQJUJMZ RB_HUMAN Post-Translational Modifications [2]
Ribosomal protein S6 kinase beta-1 (RPS6KB1) OTAELNGX KS6B1_HUMAN Post-Translational Modifications [2]

References

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2 Combination therapy for treating breast cancer using antiestrogen, ERA-923, and the mammalian target of rapamycin inhibitor, temsirolimus. Endocr Relat Cancer. 2006 Sep;13(3):863-73.
3 Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. J Med Chem. 2001 May 24;44(11):1654-7.
4 Differential biochemical and cellular actions of Premarin estrogens: distinct pharmacology of bazedoxifene-conjugated estrogens combination. Mol Endocrinol. 2009 Jan;23(1):74-85.
5 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
6 Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity. J Med Chem. 2007 May 31;50(11):2682-92.
7 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.
8 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.
9 Company report (Axcentua)
10 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.
11 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.
12 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031986)
13 Update on alternative therapies for vulvovaginal atrophy. Patient Prefer Adherence. 2011; 5: 533-536.
14 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.
15 Reprint of Are all estrogens the same Maturitas. 2008 Sep-Oct;61(1-2):195-201.
16 17alpha-Ethinylestradiol hinders nucleotide excision repair in zebrafish liver cells. Aquat Toxicol. 2009 Dec 13;95(4):273-8.
17 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).
18 Clinical pipeline report, company report or official report of Shionogi (2011).
19 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.
20 Indomethacin inhibits cell growth of medullary thyroid carcinoma by reducing cell cycle progression into S phase. Exp Biol Med (Maywood). 2008 Nov;233(11):1433-40. doi: 10.3181/0804-RM-127. Epub 2008 Sep 12.
21 Therapeutically activating RB: reestablishing cell cycle control in endocrine therapy-resistant breast cancer. Endocr Relat Cancer. 2011 Apr 28;18(3):333-45. doi: 10.1530/ERC-10-0262. Print 2011 Jun.
22 Effects and mechanisms of betulinic acid on improving EGFR TKI-resistance of lung cancer cells. Environ Toxicol. 2018 Nov;33(11):1153-1159.
23 BMN 673 (talazoparib): A potent PARP inhibitor for triple negative breast cancer with different genetic profile. J Biochem Mol Toxicol. 2019 May;33(5):e22286. doi: 10.1002/jbt.22286. Epub 2019 Jan 23.
24 Microarray analysis of H2O2-, HNE-, or tBH-treated ARPE-19 cells. Free Radic Biol Med. 2002 Nov 15;33(10):1419-32.
25 Combination small molecule MEK and PI3K inhibition enhances uveal melanoma cell death in a mutant GNAQ- and GNA11-dependent manner. Clin Cancer Res. 2012 Aug 15;18(16):4345-55. doi: 10.1158/1078-0432.CCR-11-3227. Epub 2012 Jun 25.
26 Sulindac induces specific degradation of the HPV oncoprotein E7 and causes growth arrest and apoptosis in cervical carcinoma cells. Cancer Lett. 2007 Jan 8;245(1-2):103-11. doi: 10.1016/j.canlet.2005.12.034. Epub 2006 Feb 20.
27 Melanoma coordinates general and cell-specific mechanisms to promote methotrexate resistance. Exp Cell Res. 2012 Jun 10;318(10):1146-59.
28 HMG-CoA reductase inhibitor simvastatin inhibits cell cycle progression at the G1/S checkpoint in immortalized lymphocytes from Alzheimer's disease patients independently of cholesterol-lowering effects. J Pharmacol Exp Ther. 2008 Jan;324(1):352-9. doi: 10.1124/jpet.107.128959. Epub 2007 Oct 10.
29 Inhibition of prostate cancer cell colony formation by the flavonoid quercetin correlates with modulation of specific regulatory genes. Clin Diagn Lab Immunol. 2004 Jan;11(1):63-9. doi: 10.1128/cdli.11.1.63-69.2004.
30 Rapamycin sensitizes multiple myeloma cells to apoptosis induced by dexamethasone. Blood. 2004 Apr 15;103(8):3138-47. doi: 10.1182/blood-2003-05-1543. Epub 2003 Dec 24.
31 Antidepressant drug sertraline modulates AMPK-MTOR signaling-mediated autophagy via targeting mitochondrial VDAC1 protein. Autophagy. 2021 Oct;17(10):2783-2799. doi: 10.1080/15548627.2020.1841953. Epub 2020 Nov 9.
32 EGFR tyrosine kinase inhibitors activate autophagy as a cytoprotective response in human lung cancer cells. PLoS One. 2011;6(6):e18691. doi: 10.1371/journal.pone.0018691. Epub 2011 Jun 2.
33 Oxidative stress induces parallel autophagy and mitochondria dysfunction in human glioma U251 cells. Toxicol Sci. 2009 Aug;110(2):376-88. doi: 10.1093/toxsci/kfp101. Epub 2009 May 18.
34 Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.
35 SU5416 inhibited VEGF and HIF-1alpha expression through the PI3K/AKT/p70S6K1 signaling pathway. Biochem Biophys Res Commun. 2004 Nov 12;324(2):471-80. doi: 10.1016/j.bbrc.2004.09.082.
36 Differential modulation of PI3-kinase/Akt pathway during all-trans retinoic acid- and Am80-induced HL-60 cell differentiation revealed by DNA microarray analysis. Biochem Pharmacol. 2004 Dec 1;68(11):2177-86.
37 D-glucosamine down-regulates HIF-1alpha through inhibition of protein translation in DU145 prostate cancer cells. Biochem Biophys Res Commun. 2009 Apr 24;382(1):96-101. doi: 10.1016/j.bbrc.2009.02.129. Epub 2009 Feb 28.
38 Arsenic trioxide inhibits translation of mRNA of bcr-abl, resulting in attenuation of Bcr-Abl levels and apoptosis of human leukemia cells. Cancer Res. 2003 Nov 15;63(22):7950-8.
39 The nonsteroidal anti-inflammatory drugs aspirin and indomethacin attenuate beta-catenin/TCF-4 signaling. Oncogene. 2001 Feb 1;20(5):645-53. doi: 10.1038/sj.onc.1204123.
40 Novel mechanism of cannabidiol-induced apoptosis in breast cancer cell lines. Breast. 2018 Oct;41:34-41. doi: 10.1016/j.breast.2018.06.009. Epub 2018 Jun 22.
41 -Carotene Induces Apoptosis in Human Esophageal Squamous Cell Carcinoma Cell Lines via the Cav-1/AKT/NF-B Signaling Pathway. J Biochem Mol Toxicol. 2016 Mar;30(3):148-57. doi: 10.1002/jbt.21773. Epub 2016 Jan 6.
42 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.
43 Dasatinib (BMS-354825) selectively induces apoptosis in lung cancer cells dependent on epidermal growth factor receptor signaling for survival. Cancer Res. 2006 Jun 1;66(11):5542-8. doi: 10.1158/0008-5472.CAN-05-4620.
44 Resveratrol attenuates senescence of adipose-derived mesenchymal stem cells and restores their paracrine effects on promoting insulin secretion of INS-1 cells through Pim-1. Eur Rev Med Pharmacol Sci. 2016;20(6):1203-13.
45 Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
46 Ribavirin augments doxorubicin's efficacy in human hepatocellular carcinoma through inhibiting doxorubicin-induced eIF4E activation. J Biochem Mol Toxicol. 2018 Jan;32(1). doi: 10.1002/jbt.22007. Epub 2017 Nov 7.
47 Cell cycle effects of nonsteroidal anti-inflammatory drugs and enhanced growth inhibition in combination with gemcitabine in pancreatic carcinoma cells. J Pharmacol Exp Ther. 2001 Sep;298(3):976-85.