DGIdb - TAMOXIFEN Drug Record

TAMOXIFEN chembl:CHEMBL83 ApprovedAntineoplastic

Alternate Names:

ICI-47699
ICI-46474
SOLTAMOX
NOLVADEX
TAMOXIFEN
TAMOXIFÈNE
1-P-BETA-DIMETHYLAMINOETHOXYPHENYL-TRANS-1,2-DIPHENYLBUT-1-ENE
TRANS-TAMOXIFEN
1-PARA-BETA-DIMETHYLAMINOETHOXYPHENYL-TRANS-1,2-DIPHENYLBUT-1-ENE
(Z)-2-(4-(1,2-DIPHENYL-1-BUTENYL)PHENOXY)-N,N-DIMETHYLETHANAMINE
TAMOXIFENO
(Z)-2-(PARA-(1,2-DIPHENYL-1-BUTENYL)PHENOXY)-N,N-DIMETHYLAMINE
TAMOXIFENUM
NOLVADEX®
SOLTAMOX®
ZD6157
TAMOXIFENE
drugbank:00675
rxcui:10324
chembl:CHEMBL83
chemidplus:10540-29-1
pubchem.compound:2733526

Drug Info:

Drug Class	antineoplastic agents, hormonal
Year of Approval	1977
FDA Approval	1977
Drug Class	small molecule
Drug Indications	Antineoplastic Agents, Hormonal

(10 More Sources)

Publications:

Scott SA et al., 2009, Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness., Nat Chem Biol
Mc Ilroy et al., 2006, Tamoxifen-induced ER-alpha-SRC-3 interaction in HER2 positive human breast cancer; a possible mechanism for ER isoform specific recurrence., Endocr. Relat. Cancer
Girault et al., 2006, Role of estrogen receptor alpha transcriptional coregulators in tamoxifen resistance in breast cancer., Maturitas
Hayes et al., 2010, Estrogen receptor genotypes, menopausal status, and the effects of tamoxifen on lipid levels: revised and updated results., Clin. Pharmacol. Ther.
Sasson, 1991, Equilibrium binding analysis of estrogen agonists and antagonists: relation to the activation of the estrogen receptor., Pathol. Biol.
Chen et al., 2005, Potential of endogenous estrogen receptor beta to influence the selective ER modulator ERbeta complex., Int. J. Oncol.
Gruvberger-Saal et al., 2007, Estrogen receptor beta expression is associated with tamoxifen response in ERalpha-negative breast carcinoma., Clin. Cancer Res.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Horner-Glister et al., 2005, Influence of oestradiol and tamoxifen on oestrogen receptors-alpha and -beta protein degradation and non-genomic signalling pathways in uterine and breast carcinoma cells., J. Mol. Endocrinol.
Ntukidem NI et al., 2008, Estrogen receptor genotypes, menopausal status, and the lipid effects of tamoxifen., Clin Pharmacol Ther
Jain D et al., 2010, A mutant selective anti-estrogen is a pure antagonist on EREs and AP-1 response elements., Bioorg Med Chem Lett
Sridar C et al., 2012, Bioactivation of the cancer chemopreventive agent tamoxifen to quinone methides by cytochrome P4502B6 and identification of the modified residue on the apoprotein., Drug Metab Dispos
Robinson et al., 2013, Activating ESR1 mutations in hormone-resistant metastatic breast cancer., Nat. Genet.
Jeselsohn et al., 2014, Emergence of constitutively active estrogen receptor-α mutations in pretreated advanced estrogen receptor-positive breast cancer., Clin. Cancer Res.
Toy et al., 2013, ESR1 ligand-binding domain mutations in hormone-resistant breast cancer., Nat. Genet.
Ogawa T et al., 2006, m-Carborane bisphenol structure as a pharmacophore for selective estrogen receptor modulators., Bioorg Med Chem Lett
Rivera-Guevara C et al., 2010, Genomic action of permanently charged tamoxifen derivatives via estrogen receptor-alpha., Bioorg Med Chem
Cyrus et al., 2010, Jostling for position: optimizing linker location in the design of estrogen receptor-targeting PROTACs., ChemMedChem
Fabian et al., Chemoprevention for high-risk women: tamoxifen and beyond., Breast J
Osborne et al., 2003, Role of the estrogen receptor coactivator AIB1 (SRC-3) and HER-2/neu in tamoxifen resistance in breast cancer., J. Natl. Cancer Inst.
Ribas et al., 2015, AKT Antagonist AZD5363 Influences Estrogen Receptor Function in Endocrine-Resistant Breast Cancer and Synergizes with Fulvestrant (ICI182780) In Vivo., Mol. Cancer Ther.
Stendahl et al., 2004, Cyclin D1 overexpression is a negative predictive factor for tamoxifen response in postmenopausal breast cancer patients., Br. J. Cancer
Christov et al., 2003, Cell proliferation, apoptosis, and expression of cyclin D1 and cyclin E as potential biomarkers in tamoxifen-treated mammary tumors., Breast Cancer Res. Treat.
Han et al., Cyclin D1 expression and patient outcome after tamoxifen therapy in estrogen receptor positive metastatic breast cancer., Oncol. Rep.
Bhattacharyya et al., 1994, Protooncogene, growth factor, growth factor receptor, and estrogen and progesterone receptor gene expression in the immature rat uterus after treatment with estrogen and tamoxifen., J. Submicrosc. Cytol. Pathol.
Narod SA et al., 2000, Tamoxifen and risk of contralateral breast cancer in BRCA1 and BRCA2 mutation carriers: a case-control study. Hereditary Breast Cancer Clinical Study Group., Lancet
Pierce LJ et al., 2006, Ten-year multi-institutional results of breast-conserving surgery and radiotherapy in BRCA1/2-associated stage I/II breast cancer., J Clin Oncol
Gronwald J et al., 2006, Tamoxifen and contralateral breast cancer in BRCA1 and BRCA2 carriers: an update., Int J Cancer
Metcalfe K et al., 2004, Contralateral breast cancer in BRCA1 and BRCA2 mutation carriers., J Clin Oncol
Jones et al., 2005, Promotion of mammary cancer development by tamoxifen in a mouse model of Brca1-mutation-related breast cancer., Oncogene
Toimela et al., 1995, Retinal pigment epithelium cell culture as a model for evaluation of the toxicity of tamoxifen and chloroquine., Ophthalmic Res.
Suzuki et al., Effects of tamoxifen on mammary tumors and bone in 7,12-dimethylbenz-(a)anthracene-treated rats., Anticancer Res.
Vadlamudi et al., 1998, Role of female sex steroids in regulating cholesteryl ester transfer protein in transgenic mice., Metab. Clin. Exp.
Yamashita et al., 1993, Interleukin 6 stimulates the production of immunoreactive endothelin 1 in human breast cancer cells., Cancer Res.
Klein DJ et al., 2013, PharmGKB summary: tamoxifen pathway, pharmacokinetics., Pharmacogenet Genomics
Weng L et al., 2013, Genome-wide discovery of genetic variants affecting tamoxifen sensitivity and their clinical and functional validation., Ann Oncol
Berns et al., 2000, Complete sequencing of TP53 predicts poor response to systemic therapy of advanced breast cancer., Cancer Res.
Kretschmer XC et al., 2005, CAR and PXR: xenosensors of endocrine disrupters?, Chem Biol Interact
Harmsen et al., 2009, Nuclear receptor mediated induction of cytochrome P450 3A4 by anticancer drugs: a key role for the pregnane X receptor., Cancer Chemother. Pharmacol.
Nilsson et al., 2006, Estradiol and tamoxifen regulate endostatin generation via matrix metalloproteinase activity in breast cancer in vivo., Cancer Res.
Yu et al., 1994, Induction of prostate specific antigen production by steroids and tamoxifen in breast cancer cell lines., Breast Cancer Res. Treat.
Rokavec M et al., 2008, A polymorphism in the TC21 promoter associates with an unfavorable tamoxifen treatment outcome in breast cancer., Cancer Res
Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
Ingle JN et al., 2013, Selective estrogen receptor modulators and pharmacogenomic variation in ZNF423 regulation of BRCA1 expression: individualized breast cancer prevention., Cancer Discov
Eisen et al., 2002, Selective estrogen receptor (ER) modulators differentially regulate phospholipase D catalytic activity in ER-negative breast cancer cells., Mol. Pharmacol.
Gao T et al., 2014, CCNA2 is a prognostic biomarker for ER+ breast cancer and tamoxifen resistance., PLoS One
Grenman et al., 1987, In vitro effects of tamoxifen on UM-SCC head and neck cancer cell lines: correlation with the estrogen and progesterone receptor content., Int. J. Cancer
Osborne et al., 1997, Minor products of reaction of DNA with alpha-acetoxytamoxifen., Carcinogenesis
Kiyotani K et al., 2012, A genome-wide association study identifies locus at 10q22 associated with clinical outcomes of adjuvant tamoxifen therapy for breast cancer patients in Japanese., Hum Mol Genet
Liu et al., 2007, Downregulation of erbB3 abrogates erbB2-mediated tamoxifen resistance in breast cancer cells., Int. J. Cancer
Raspollini et al., 2005, HER-2/neu oncogene in uterine carcinosarcoma on tamoxifen therapy., Pathol. Res. Pract.
Kurokawa et al., 2001, Inhibition of erbB receptor (HER) tyrosine kinases as a strategy to abrogate antiestrogen resistance in human breast cancer., Clin. Cancer Res.
Levine et al., 1985, Effects of estrogen and tamoxifen on the regulation of dihydrofolate reductase gene expression in a human breast cancer cell line., Cancer Res.
Yager et al., 1986, Effects of ethinyl estradiol and tamoxifen on liver DNA turnover and new synthesis and appearance of gamma glutamyl transpeptidase-positive foci in female rats., Carcinogenesis
Kimura et al., 2008, Cell-lineage regulated myogenesis for dystrophin replacement: a novel therapeutic approach for treatment of muscular dystrophy., Hum. Mol. Genet.
Ciocca et al., 1998, Heat shock proteins hsp27 and hsp70: lack of correlation with response to tamoxifen and clinical course of disease in estrogen receptor-positive metastatic breast cancer (a Southwest Oncology Group Study)., Clin. Cancer Res.
Chiarenza et al., 2001, Tamoxifen inhibits nerve growth factor-induced proliferation of the human breast cancerous cell line MCF-7., Cancer Res.
Duggan C et al., 2003, Inherited and acquired risk factors for venous thromboembolic disease among women taking tamoxifen to prevent breast cancer., J Clin Oncol
Abramson N et al., 2006, Effect of Factor V Leiden and prothrombin G20210-->A mutations on thromboembolic risk in the national surgical adjuvant breast and bowel project breast cancer prevention trial., J Natl Cancer Inst
Hartmaier RJ et al., 2012, A SNP in steroid receptor coactivator-1 disrupts a GSK3β phosphorylation site and is associated with altered tamoxifen response in bone., Mol Endocrinol
Liel et al., 1992, Evidence that estrogens modulate activity and increase the number of 1,25-dihydroxyvitamin D receptors in osteoblast-like cells (ROS 17/2.8)., Endocrinology
Marttunen et al., 1998, Comparison of effects of tamoxifen and toremifene on bone biochemistry and bone mineral density in postmenopausal breast cancer patients., J. Clin. Endocrinol. Metab.
May et al., 2015, TFF3 is a valuable predictive biomarker of endocrine response in metastatic breast cancer., Endocr. Relat. Cancer
Hofstra et al., Combined treatment with goserelin and tamoxifen in patients with advanced chemotherapy resistant ovarian cancer., Anticancer Res.
Dejardin et al., 1991, Stimulatory effect of oestradiol-17 beta and tamoxifen on gross cystic disease fluid protein 15,000 production and mRNA levels in T47D human breast cancer cells., J. Mol. Endocrinol.
Akinmade et al., 2008, Phosphorylation of the ErbB3 binding protein Ebp1 by p21-activated kinase 1 in breast cancer cells., Br. J. Cancer
Robertson et al., 1998, Tamoxifen up-regulates oestrogen receptor-alpha, c-fos and glyceraldehyde 3-phosphate-dehydrogenase mRNAs in ovine endometrium., J. Steroid Biochem. Mol. Biol.
Zheng et al., 2014, Aurora-A is a determinant of tamoxifen sensitivity through phosphorylation of ERα in breast cancer., Oncogene

TAMOXIFEN PIP

Interaction Score: 2.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
1930624

Sources:
NCI
TAMOXIFEN LRMDA

Interaction Score: 2.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22180457

Sources:
PharmGKB
TAMOXIFEN RRAS2

Interaction Score: 2.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19047159

Sources:
PharmGKB
TAMOXIFEN E2F7

Interaction Score: 2.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23508821

Sources:
PharmGKB
TAMOXIFEN PLD1

Interaction Score: 1.42

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12237338 19136975

Sources:
DTC NCI
TAMOXIFEN TFF3

Interaction Score: 1.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25900183

Sources:
CIViC
TAMOXIFEN ZNF423

Interaction Score: 1.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23764426

Sources:
PharmGKB
TAMOXIFEN PLD2

Interaction Score: 1.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19136975

Sources:
DTC
TAMOXIFEN FMO1

Interaction Score: 0.71

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23962908

Sources:
PharmGKB
TAMOXIFEN NCOA1

Interaction Score: 0.53

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22174377

Sources:
PharmGKB
TAMOXIFEN F5

Interaction Score: 0.53

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
14512389 16818854

Sources:
PharmGKB FDA
TAMOXIFEN CCNA2

Interaction Score: 0.53

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24622579

Sources:
PharmGKB
TAMOXIFEN MUC16

Interaction Score: 0.27

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10629663

Sources:
NCI
TAMOXIFEN COL18A1

Interaction Score: 0.27

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16651433

Sources:
NCI
TAMOXIFEN FMO3

Interaction Score: 0.27

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23962908

Sources:
PharmGKB
TAMOXIFEN CCND1

Interaction Score: 0.27

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15138475 12602925 12469160

Sources:
NCI CIViC
TAMOXIFEN HSPB2

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9607585

Sources:
NCI
TAMOXIFEN MYOD1

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18511457

Sources:
NCI
TAMOXIFEN HEXB

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8577454

Sources:
NCI
TAMOXIFEN NCOA3

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12618500

Sources:
NCI
TAMOXIFEN ESR2

Interaction Score: 0.23

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Specific Action of the Ligand Agonist

PMIDs:
17158759 16822624 20827267 2011412 16010412 17404078 11752352 16326830 17713466 20659801

Sources:
DTC TdgClinicalTrial TEND GuideToPharmacology PharmGKB
TAMOXIFEN GPER1

Interaction Score: 0.21

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
TAMOXIFEN EDN1

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8425178

Sources:
NCI
TAMOXIFEN CETP

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9751231

Sources:
NCI
TAMOXIFEN GAPDH

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9883985

Sources:
NCI
TAMOXIFEN DHFR

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
3978632

Sources:
NCI
TAMOXIFEN GGT1

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
2877750

Sources:
NCI
TAMOXIFEN KLK3

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
7532467

Sources:
NCI
TAMOXIFEN ESR1

Interaction Score: 0.12

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Alteration ESR1:E380Q,.537.,.538.,L536.,P535H

Drug family Hormonal therapy

combination therapy [Tamoxifen,Letrozole,Anastrozole,Exemestane,Fulvestrant,LHRH analogues or antagonist]

PMIDs:
24185510 24398047 24185512 16735120 20659801 20621492 2011412 20512796 11906441 11752352 17713466

Sources:
DTC ClearityFoundationBiomarkers TdgClinicalTrial ClearityFoundationClinicalTrial CGI TEND CIViC GuideToPharmacology PharmGKB TTD FDA
TAMOXIFEN TGM2

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9067554

Sources:
NCI
TAMOXIFEN PGR

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
3793272

Sources:
ClearityFoundationBiomarkers NCI PharmGKB FDA
TAMOXIFEN BGLAP

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9543133

Sources:
NCI
TAMOXIFEN NRG1

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18283314

Sources:
NCI
TAMOXIFEN BRCA1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11130383 16636335 16331614 15197194 15750629

Sources:
NCI PharmGKB
TAMOXIFEN F2

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
TAMOXIFEN TYMS

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9615734

Sources:
NCI
TAMOXIFEN TGFB1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8019941

Sources:
NCI
TAMOXIFEN NF1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Alteration NF1:.

Alteration NF1:del

Drug family Hormonal therapy

PMIDs:
None found

Sources:
CGI
TAMOXIFEN CYP2B6

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22942317

Sources:
DTC
TAMOXIFEN AURKA

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24166501

Sources:
CIViC
TAMOXIFEN NTRK1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11306479

Sources:
NCI
TAMOXIFEN ERBB2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy [Tamoxifen,Letrozole,Anastrozole,Exemestane,Fulvestrant,LHRH analogues or antagonist]

Drug family [Hormonal therapy]

Alteration ERBB2:norm;ESR1:over

PMIDs:
17266042 15901136 11916237

Sources:
NCI CGI
TAMOXIFEN CYP19A1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
TAMOXIFEN NR1I2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16054614 18839173

Sources:
PharmGKB
TAMOXIFEN ABCC2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
TAMOXIFEN PIK3CA

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy AZD5363 + Tamoxifen

Indication/Tumor Type estrogen-receptor positive breast cancer

Response Type predicted – sensitive

PMIDs:
26116361

Sources:
JAX-CKB
TAMOXIFEN TP53

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10786679

Sources:
DTC CIViC
TAMOXIFEN CYP1A2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300 23962908

Sources:
DTC PharmGKB
TAMOXIFEN CBX1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TAMOXIFEN CYP2C9

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
TAMOXIFEN VDR

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
1315250

Sources:
NCI
TAMOXIFEN ABCB1

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
TAMOXIFEN ATXN2

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TAMOXIFEN BAZ2B

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TAMOXIFEN IDH1

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TAMOXIFEN KDM4A

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TAMOXIFEN CYP3A4

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
TAMOXIFEN GMNN

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TAMOXIFEN CYP2D6

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
FDA
TAMOXIFEN EHMT2

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

TEND: TAMOXIFEN
- Version: 01-August-2011
Alternate Names:

TAMOXIFEN Primary Drug Name

Drug Info:

Year of Approval 1977

Drug Class antineoplastic agents, hormonal

Publications:
TdgClinicalTrial: TAMOXIFEN
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications Antineoplastic Agents, Hormonal

Drug Class small molecule

FDA Approval 1977

Publications:

NCI: TAMOXIFEN

Version: 14-September-2017

Alternate Names:

C855 NCI drug code

Drug Info:

Publications:

Eisen et al., 2002, Selective estrogen receptor (ER) modulators differentially regulate phospholipase D catalytic activity in ER-negative breast cancer cells., Mol. Pharmacol.

Grenman et al., 1987, In vitro effects of tamoxifen on UM-SCC head and neck cancer cell lines: correlation with the estrogen and progesterone receptor content., Int. J. Cancer

Osborne et al., 1997, Minor products of reaction of DNA with alpha-acetoxytamoxifen., Carcinogenesis

DTC: TAMOXIFEN

Version: 02-September-2020

Alternate Names:

CHEMBL83 ChEMBL Drug ID

Drug Info:

Publications:

Scott SA et al., 2009, Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness., Nat Chem Biol

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

Jain D et al., 2010, A mutant selective anti-estrogen is a pure antagonist on EREs and AP-1 response elements., Bioorg Med Chem Lett

CGI: Tamoxifen

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Jeselsohn et al., 2014, Emergence of constitutively active estrogen receptor-α mutations in pretreated advanced estrogen receptor-positive breast cancer., Clin. Cancer Res.

Toy et al., 2013, ESR1 ligand-binding domain mutations in hormone-resistant breast cancer., Nat. Genet.

Robinson et al., 2013, Activating ESR1 mutations in hormone-resistant metastatic breast cancer., Nat. Genet.

JAX-CKB: Tamoxifen
- Version: 27-September-2017
Alternate Names:

Drug Info:

Publications:

Ribas et al., 2015, AKT Antagonist AZD5363 Influences Estrogen Receptor Function in Endocrine-Resistant Breast Cancer and Synergizes with Fulvestrant (ICI182780) In Vivo., Mol. Cancer Ther.

PharmGKB: tamoxifen

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Narod SA et al., 2000, Tamoxifen and risk of contralateral breast cancer in BRCA1 and BRCA2 mutation carriers: a case-control study. Hereditary Breast Cancer Clinical Study Group., Lancet

Metcalfe K et al., 2004, Contralateral breast cancer in BRCA1 and BRCA2 mutation carriers., J Clin Oncol

Gronwald J et al., 2006, Tamoxifen and contralateral breast cancer in BRCA1 and BRCA2 carriers: an update., Int J Cancer

CIViC: TAMOXIFEN

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Stendahl et al., 2004, Cyclin D1 overexpression is a negative predictive factor for tamoxifen response in postmenopausal breast cancer patients., Br. J. Cancer

Robinson et al., 2013, Activating ESR1 mutations in hormone-resistant metastatic breast cancer., Nat. Genet.

Zheng et al., 2014, Aurora-A is a determinant of tamoxifen sensitivity through phosphorylation of ERα in breast cancer., Oncogene

GuideToPharmacology: 135651233
- Version: 29-September-2020
Alternate Names:

TAMOXIFEN GuideToPharmacology Ligand Name

Drug Info:

Publications:
TTD: Tamoxifen
- Version: 2020.06.01
Alternate Names:

D07KSG TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL83
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ClearityFoundationClinicalTrial: TAMOXIFEN
- Version: 15-June-2013
Alternate Names:

Drug Info:

Publications:
FDA: Tamoxifen
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:
ClearityFoundationBiomarkers: TAMOXIFEN
- Version: 26-July-2013
Alternate Names:

Drug Info:

Publications:

Specific Action of the Ligand	Antagonist
Endogenous Drug?	False
Specific Action of the Ligand	Agonist

Specific Action of the Ligand	Full agonist
Endogenous Drug?	False

Alteration	ESR1:E380Q,.537.,.538.,L536.,P535H
Drug family	Hormonal therapy
combination therapy	[Tamoxifen,Letrozole,Anastrozole,Exemestane,Fulvestrant,LHRH analogues or antagonist]

combination therapy	AZD5363 + Tamoxifen
Indication/Tumor Type	estrogen-receptor positive breast cancer
Response Type	predicted – sensitive

TAMOXIFEN Drug Record

TAMOXIFEN chembl:CHEMBL83 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 1930624

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22180457

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19047159

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23508821

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12237338 19136975

Sources: DTC NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25900183

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23764426

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19136975

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23962908

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22174377

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 14512389 16818854

Sources: PharmGKB FDA

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24622579

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10629663

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16651433

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23962908

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15138475 12602925 12469160

Sources: NCI CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9607585

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18511457

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 8577454

Interaction Types & Directionality:

n/a

PMIDs:
1930624

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
22180457

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
19047159

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
23508821

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
12237338 19136975

Sources:
DTC NCI

Interaction Types & Directionality:

n/a

PMIDs:
25900183

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
23764426

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
19136975

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
23962908

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
22174377

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
14512389 16818854

Sources:
PharmGKB FDA

Interaction Types & Directionality:

n/a

PMIDs:
24622579

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
10629663

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
16651433

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
23962908

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
15138475 12602925 12469160

Sources:
NCI CIViC

Interaction Types & Directionality:

n/a

PMIDs:
9607585

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
18511457

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
8577454

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
12618500

Sources:
NCI

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Specific Action of the Ligand Agonist

PMIDs:
17158759 16822624 20827267 2011412 16010412 17404078 11752352 16326830 17713466 20659801

Sources:
DTC TdgClinicalTrial TEND GuideToPharmacology PharmGKB

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
8425178

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
9751231

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
9883985

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
3978632

Sources:
NCI