DGIdb - FULVESTRANT Drug Record

FULVESTRANT chembl:CHEMBL1358 ApprovedAntineoplastic

Alternate Names:

FASLODEX
ICI-182780
ZD-9238
FULVESTRANT
ICI 182,780
SID29215034
chembl:CHEMBL1358
pubchem.compound:104741
chemidplus:129453-61-8
rxcui:282357
drugbank:00947

Drug Info:

Drug Class	antineoplastic agents, hormonal
Year of Approval	2002
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antineoplastic agent

(10 More Sources)

Publications:

Rivera-Guevara C et al., 2010, Genomic action of permanently charged tamoxifen derivatives via estrogen receptor-alpha., Bioorg Med Chem
Lin HR et al., 2007, Identification of a series of tetrahydroisoquinoline derivatives as potential therapeutic agents for breast cancer., Bioorg Med Chem Lett
Agouridas V et al., 2009, Effect of fluorination on the pharmacological profile of 11beta isomers of fulvestrant in breast carcinoma cells., J Med Chem
Lai A et al., 2015, Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts., J Med Chem
Calogeropoulou T et al., 2009, Novel dehydroepiandrosterone derivatives with antiapoptotic, neuroprotective activity., J Med Chem
De Savi C et al., 2015, Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist., J Med Chem
Jacquot Y et al., 2007, Synthesis, structure, and estrogenic activity of 4-amino-3-(2-methylbenzyl)coumarins on human breast carcinoma cells., Bioorg Med Chem
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.
Bundred et al., 2002, Fulvestrant (Faslodex): current status in the therapy of breast cancer., Expert Rev Anticancer Ther
Dow, 2002, Existing and emerging endocrine therapies for breast cancer., Cancer Nurs
Curran et al., 2001, Fulvestrant., Drugs
Elkak et al., 2001, Pure antiestrogens and breast cancer., Curr Med Res Opin
McKeage et al., 2004, Fulvestrant: a review of its use in hormone receptor-positive metastatic breast cancer in postmenopausal women with disease progression following antiestrogen therapy., Drugs
Jones et al., 2005, Effectiveness and tolerability of fulvestrant in postmenopausal women with hormone receptor-positive breast cancer., Clin. Breast Cancer
Morris et al., 2002, Fulvestrant ('Faslodex')--a new treatment option for patients progressing on prior endocrine therapy., Endocr. Relat. Cancer
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Kabos et al., 2010, Fulvestrant: a unique antiendocrine agent for estrogen-sensitive breast cancer., Expert Opin Pharmacother
Yang et al., 2016, Strategically Timing Inhibition of Phosphatidylinositol 3-Kinase to Maximize Therapeutic Index in Estrogen Receptor Alpha-Positive, PIK3CA-Mutant Breast Cancer., Clin. Cancer Res.
Alves et al., 2016, High CDK6 Protects Cells from Fulvestrant-Mediated Apoptosis and is a Predictor of Resistance to Fulvestrant in Estrogen Receptor-Positive Metastatic Breast Cancer., Clin. Cancer Res.
Morisseau C et al., 2013, Inhibition of soluble epoxide hydrolase by fulvestrant and sulfoxides., Bioorg Med Chem Lett
Spoerke et al., 2016, Heterogeneity and clinical significance of ESR1 mutations in ER-positive metastatic breast cancer patients receiving fulvestrant., Nat Commun
André F et al., 2019, Alpelisib for <i>PIK3CA</i>-Mutated, Hormone Receptor-Positive Advanced Breast Cancer., N Engl J Med
Ickenstein et al., 2002, Persistent suppression of hepatic CYP2A1 expression and serum triiodothyronine levels by tamoxifen in intact female rats: dose-response analysis and comparison with 4-hydroxytamoxifen, fulvestrant (ICI 182,780), and 17beta-estradiol-3-benzoate., J. Pharmacol. Exp. Ther.
Jiang XR et al., 2013, Synthesis of novel estrogen receptor antagonists using metal-catalyzed coupling reactions and characterization of their biological activity., J Med Chem
Dahm et al., 2006, Estrogens, selective estrogen receptor modulators, and a selective estrogen receptor down-regulator inhibit endothelial production of tissue factor pathway inhibitor 1., BMC Cardiovasc Disord
Turner NC et al., 2019, Cyclin E1 Expression and Palbociclib Efficacy in Previously Treated Hormone Receptor-Positive Metastatic Breast Cancer., J Clin Oncol
Eritja N et al., 2014, Combinatorial therapy using dovitinib and ICI182.780 (fulvestrant) blocks tumoral activity of endometrial cancer cells., Mol Cancer Ther

FULVESTRANT ESRRA

Interaction Score: 2.38

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23448346

Sources:
DTC
FULVESTRANT CCNE1

Interaction Score: 1.9

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
30807234

Sources:
CIViC
FULVESTRANT EPHX2

Interaction Score: 1.59

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23684894

Sources:
DTC
FULVESTRANT TFPI

Interaction Score: 0.95

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17029634

Sources:
NCI
FULVESTRANT ESR1

Interaction Score: 0.69

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name fulvestrant,Faslodex

Mechanism of Interaction Estrogen receptor antagonist

PMIDs:
20621492 17337183 19133777 25879485 19845386 26407012 17275315 24185512 24185510 12113237 12080538 11398912 11922402 15018596 15865850 12542403 11752352 20151846

Sources:
TALC DTC TdgClinicalTrial ChemblInteractions TEND CIViC PharmGKB TTD FDA OncoKB
FULVESTRANT CDK6

Interaction Score: 0.59

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27252418

Sources:
CIViC
FULVESTRANT ESR2

Interaction Score: 0.39

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Notes

Mechanism of Interaction Estrogen receptor antagonist

Direct Interaction yes

PMIDs:
19845386

Sources:
TALC DTC ChemblInteractions PharmGKB
FULVESTRANT FGFR2

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24448819

Sources:
CIViC
FULVESTRANT PGR

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
FULVESTRANT PIK3CA

Interaction Score: 0.17

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Fulvestrant + GDC-0941

Indication/Tumor Type estrogen-receptor positive breast cancer

Response Type no benefit

PMIDs:
27174596 31091374

Sources:
JAX-CKB CIViC OncoKB
FULVESTRANT PTEN

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Fulvestrant + GDC-0941

Indication/Tumor Type estrogen-receptor positive breast cancer

Response Type sensitive

PMIDs:
26733612

Sources:
JAX-CKB
FULVESTRANT ERBB2

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
FULVESTRANT CYP1A2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12130719

Sources:
NCI

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

FULVESTRANT Primary Drug Name

Drug Info:

Year of Approval 2002

Drug Class antineoplastic agents, hormonal

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

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small Molecule

FDA Approval approved

Publications:

NCI: FULVESTRANT

Version: 14-September-2017

Alternate Names:

C1379 NCI drug code

Drug Info:

Publications:

Ickenstein et al., 2002, Persistent suppression of hepatic CYP2A1 expression and serum triiodothyronine levels by tamoxifen in intact female rats: dose-response analysis and comparison with 4-hydroxytamoxifen, fulvestrant (ICI 182,780), and 17beta-estradiol-3-benzoate., J. Pharmacol. Exp. Ther.

Dahm et al., 2006, Estrogens, selective estrogen receptor modulators, and a selective estrogen receptor down-regulator inhibit endothelial production of tissue factor pathway inhibitor 1., BMC Cardiovasc Disord

DTC: FULVESTRANT

Version: 02-September-2020

Alternate Names:

CHEMBL1358 ChEMBL Drug ID

Drug Info:

Publications:

Calogeropoulou T et al., 2009, Novel dehydroepiandrosterone derivatives with antiapoptotic, neuroprotective activity., J Med Chem

Agouridas V et al., 2009, Effect of fluorination on the pharmacological profile of 11beta isomers of fulvestrant in breast carcinoma cells., J Med Chem

De Savi C et al., 2015, Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist., J Med Chem

JAX-CKB: Fulvestrant

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Yang et al., 2016, Strategically Timing Inhibition of Phosphatidylinositol 3-Kinase to Maximize Therapeutic Index in Estrogen Receptor Alpha-Positive, PIK3CA-Mutant Breast Cancer., Clin. Cancer Res.

Spoerke et al., 2016, Heterogeneity and clinical significance of ESR1 mutations in ER-positive metastatic breast cancer patients receiving fulvestrant., Nat Commun

PharmGKB: fulvestrant

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

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.

CIViC: FULVESTRANT

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

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

André F et al., 2019, Alpelisib for <i>PIK3CA</i>-Mutated, Hormone Receptor-Positive Advanced Breast Cancer., N Engl J Med

Eritja N et al., 2014, Combinatorial therapy using dovitinib and ICI182.780 (fulvestrant) blocks tumoral activity of endometrial cancer cells., Mol Cancer Ther

TTD: Fulvestrant
- Version: 2020.06.01
Alternate Names:

D0JO7Y TTD Drug ID

Drug Info:

Publications:
TALC: FULVESTRANT
- Version: 12-May-2016
Alternate Names:

FULVESTRANT Primary Drug Name

FULVESTRANT Drug Generic Name

FASLODEX Drug Trade Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1358
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
OncoKB: Fulvestrant
- Version: 23-July-2020
Alternate Names:

Drug Info:

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

Drug Info:

Publications:
MyCancerGenomeClinicalTrial: FULVESTRANT
- Version: 30-February-2014
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL1358
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Novel drug target	Established target
Trial Name	fulvestrant,Faslodex
Mechanism of Interaction	Estrogen receptor antagonist

Notes
Mechanism of Interaction	Estrogen receptor antagonist
Direct Interaction	yes

combination therapy	Fulvestrant + GDC-0941
Indication/Tumor Type	estrogen-receptor positive breast cancer
Response Type	no benefit

FULVESTRANT	Primary Drug Name
FULVESTRANT	Drug Generic Name
FASLODEX	Drug Trade Name

FULVESTRANT Drug Record

FULVESTRANT chembl:CHEMBL1358 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23448346

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 30807234

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23684894

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17029634

Sources: NCI

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name fulvestrant,Faslodex Mechanism of Interaction Estrogen receptor antagonist

PMIDs: 20621492 17337183 19133777 25879485 19845386 26407012 17275315 24185512 24185510 12113237 12080538 11398912 11922402 15018596 15865850 12542403 11752352 20151846

Sources: TALC DTC TdgClinicalTrial ChemblInteractions TEND CIViC PharmGKB TTD FDA OncoKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27252418

Sources: CIViC

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Notes Mechanism of Interaction Estrogen receptor antagonist Direct Interaction yes

PMIDs: 19845386

Sources: TALC DTC ChemblInteractions PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24448819

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB FDA

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Fulvestrant + GDC-0941 Indication/Tumor Type estrogen-receptor positive breast cancer Response Type no benefit

PMIDs: 27174596 31091374

Sources: JAX-CKB CIViC OncoKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Fulvestrant + GDC-0941 Indication/Tumor Type estrogen-receptor positive breast cancer Response Type sensitive

PMIDs: 26733612

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB FDA

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12130719

Sources: NCI

TEND: FULVESTRANT

Alternate Names: FULVESTRANT Primary Drug Name

Drug Info: Year of Approval 2002 Drug Class antineoplastic agents, hormonal

Publications:

TdgClinicalTrial: FULVESTRANT

Alternate Names:

Drug Info: Drug Indications antineoplastic agent Drug Class Small Molecule FDA Approval approved

Publications:

NCI: FULVESTRANT

Alternate Names: C1379 NCI drug code

Drug Info:

DTC: FULVESTRANT

Alternate Names: CHEMBL1358 ChEMBL Drug ID

Drug Info:

JAX-CKB: Fulvestrant

Alternate Names:

Drug Info:

PharmGKB: fulvestrant

Alternate Names:

Drug Info:

Publications: 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.

CIViC: FULVESTRANT

Alternate Names:

Interaction Types & Directionality:

n/a

PMIDs:
23448346

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
30807234

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
23684894

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
17029634

Sources:
NCI

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name fulvestrant,Faslodex

Mechanism of Interaction Estrogen receptor antagonist

PMIDs:
20621492 17337183 19133777 25879485 19845386 26407012 17275315 24185512 24185510 12113237 12080538 11398912 11922402 15018596 15865850 12542403 11752352 20151846

Sources:
TALC DTC TdgClinicalTrial ChemblInteractions TEND CIViC PharmGKB TTD FDA OncoKB

Interaction Types & Directionality:

n/a

PMIDs:
27252418

Sources:
CIViC

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Notes

Mechanism of Interaction Estrogen receptor antagonist

Direct Interaction yes

PMIDs:
19845386

Sources:
TALC DTC ChemblInteractions PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
24448819

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB FDA

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Fulvestrant + GDC-0941

Indication/Tumor Type estrogen-receptor positive breast cancer

Response Type no benefit

PMIDs:
27174596 31091374

Sources:
JAX-CKB CIViC OncoKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Fulvestrant + GDC-0941

Indication/Tumor Type estrogen-receptor positive breast cancer

Response Type sensitive

PMIDs:
26733612

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB FDA

Interaction Types & Directionality:

n/a

PMIDs:
12130719

Sources:
NCI

Alternate Names:

FULVESTRANT Primary Drug Name

Drug Info:

Year of Approval 2002

Drug Class antineoplastic agents, hormonal

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small Molecule

FDA Approval approved

Alternate Names:

C1379 NCI drug code

Alternate Names:

CHEMBL1358 ChEMBL Drug ID

Publications:

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.

Alternate Names:

D0JO7Y TTD Drug ID

Alternate Names:

FULVESTRANT Primary Drug Name

FULVESTRANT Drug Generic Name

FASLODEX Drug Trade Name