DGIdb - EXEMESTANE Drug Record

EXEMESTANE chembl:CHEMBL1200374 ApprovedAntineoplastic

Alternate Names:

AROMASIN
EXEMESTANE
FCE-24304
PNU-155971
EXEMESTANUM
6-METHYLENEANDROSTA-1,4-DIENE-3,17-DIONE
AROMASIN®
EXEMESTANO
chemidplus:107868-30-4
pubchem.compound:60198
rxcui:258494
drugbank:00990
chembl:CHEMBL1200374

Drug Info:

Drug Class	antineoplastic agents
Year of Approval	1999
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antineoplastic agent

(7 More Sources)

Publications:

Oesterreich S et al., 2015, Associations between genetic variants and the effect of letrozole and exemestane on bone mass and bone turnover., Breast Cancer Res Treat
Fontein DB et al., 2014, Germline variants in the CYP19A1 gene are related to specific adverse events in aromatase inhibitor users: a substudy of Dutch patients in the TEAM trial., Breast Cancer Res Treat
Wang L et al., 2010, Functional genetic polymorphisms in the aromatase gene CYP19 vary the response of breast cancer patients to neoadjuvant therapy with aromatase inhibitors., Cancer Res
Abrial et al., 2009, Role of neo-adjuvant hormonal therapy in the treatment of breast cancer: a review of clinical trials., Int J Gen Med
Nabholtz, 2008, Long-term safety of aromatase inhibitors in the treatment of breast cancer., Ther Clin Risk Manag
Barnadas et al., 2009, Exemestane as primary treatment of oestrogen receptor-positive breast cancer in postmenopausal women: a phase II trial., Br. J. Cancer
Untch et al., 2008, Exemestane in early breast cancer: a review., Ther Clin Risk Manag
Koutras et al., 2009, Antiproliferative effect of exemestane in lung cancer cells., Mol. Cancer
Brueggemeier et al., 2005, Aromatase inhibitors in the treatment of breast cancer., Endocr. Rev.
Robinson, 2009, A review of the use of exemestane in early breast cancer., Ther Clin Risk Manag
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Brueggemeier, 2006, Update on the use of aromatase inhibitors in breast cancer., Expert Opin Pharmacother
Platt A et al., 2016, Impact of nonsynonymous single nucleotide polymorphisms on in-vitro metabolism of exemestane by hepatic cytosolic reductases., Pharmacogenet Genomics
Liu M et al., 2014, Aromatase inhibitor-associated bone fractures: a case-cohort GWAS and functional genomics., Mol Endocrinol
Love et al., 2005, Endocrine effects of tamoxifen plus exemestane in postmenopausal women with breast cancer., Clin. Cancer Res.
Rahman et al., 2008, CYP1B1 is not a major determinant of the disposition of aromatase inhibitors in epithelial cells of invasive ductal carcinoma., Drug Metab. Dispos.
Gala K et al., 2018, KMT2C mediates the estrogen dependence of breast cancer through regulation of ERα enhancer function., Oncogene

EXEMESTANE AKR1C4

Interaction Score: 4.42

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27111237

Sources:
PharmGKB
EXEMESTANE KMT2C

Interaction Score: 2.94

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
29755131

Sources:
CIViC
EXEMESTANE CYP19A1

Interaction Score: 2.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name exemestane ,Aromasin

Novel drug target Established target

Mechanism of Interaction Cytochrome P450 19A1 inhibitor

PMIDs:
26536870 24590773 20048079 20360896 18728707 19156139 19337436 19930708 15814851 19436613 11752352 17020418

Sources:
TdgClinicalTrial ChemblInteractions TEND PharmGKB TTD
EXEMESTANE AKR1C3

Interaction Score: 0.88

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27111237

Sources:
PharmGKB
EXEMESTANE BGLAP

Interaction Score: 0.38

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15746052

Sources:
NCI
EXEMESTANE CYP1B1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18256205

Sources:
NCI
EXEMESTANE PGR

Interaction Score: 0.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
EXEMESTANE TUBB1

Interaction Score: 0.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25148458

Sources:
PharmGKB
EXEMESTANE MAP4K4

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
EXEMESTANE ESR2

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
EXEMESTANE ESR1

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26536870

Sources:
PharmGKB FDA
EXEMESTANE ERBB2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Exemestane + Seribantumab

Indication/Tumor Type Her2-receptor negative breast cancer

Response Type predicted – sensitive

PMIDs:
None found

Sources:
JAX-CKB
EXEMESTANE NFE2L2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
EXEMESTANE AR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

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

EXEMESTANE Primary Drug Name

Drug Info:

Year of Approval 1999

Drug Class antineoplastic agents

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

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small Molecule

FDA Approval approved

Publications:

NCI: EXEMESTANE

Version: 14-September-2017

Alternate Names:

C1097 NCI drug code

Drug Info:

Publications:

Love et al., 2005, Endocrine effects of tamoxifen plus exemestane in postmenopausal women with breast cancer., Clin. Cancer Res.

Rahman et al., 2008, CYP1B1 is not a major determinant of the disposition of aromatase inhibitors in epithelial cells of invasive ductal carcinoma., Drug Metab. Dispos.

PharmGKB: exemestane

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Platt A et al., 2016, Impact of nonsynonymous single nucleotide polymorphisms on in-vitro metabolism of exemestane by hepatic cytosolic reductases., Pharmacogenet Genomics

Oesterreich S et al., 2015, Associations between genetic variants and the effect of letrozole and exemestane on bone mass and bone turnover., Breast Cancer Res Treat

Fontein DB et al., 2014, Germline variants in the CYP19A1 gene are related to specific adverse events in aromatase inhibitor users: a substudy of Dutch patients in the TEAM trial., Breast Cancer Res Treat

CIViC: EXEMESTANE
- Version: 14-September-2020
Alternate Names:

Drug Info:

Publications:

Gala K et al., 2018, KMT2C mediates the estrogen dependence of breast cancer through regulation of ERα enhancer function., Oncogene
TTD: Exemestane
- Version: 2020.06.01
Alternate Names:

D0D2VS TTD Drug ID

Drug Info:

Publications:
DTC: EXEMESTANE
- Version: 02-September-2020
Alternate Names:

CHEMBL1200374 ChEMBL Drug ID

Drug Info:

Publications:
ChemblInteractions: CHEMBL1200374
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1200374
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
JAX-CKB: Exemestane
- Version: 27-September-2017
Alternate Names:

Drug Info:

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

Drug Info:

Publications:

Trial Name	exemestane ,Aromasin
Novel drug target	Established target
Mechanism of Interaction	Cytochrome P450 19A1 inhibitor

combination therapy	Exemestane + Seribantumab
Indication/Tumor Type	Her2-receptor negative breast cancer
Response Type	predicted – sensitive

EXEMESTANE Drug Record

EXEMESTANE chembl:CHEMBL1200374 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27111237

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 29755131

Sources: CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name exemestane ,Aromasin Novel drug target Established target Mechanism of Interaction Cytochrome P450 19A1 inhibitor

PMIDs: 26536870 24590773 20048079 20360896 18728707 19156139 19337436 19930708 15814851 19436613 11752352 17020418

Sources: TdgClinicalTrial ChemblInteractions TEND PharmGKB TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27111237

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15746052

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18256205

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB FDA

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25148458

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26536870

Sources: PharmGKB FDA

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Exemestane + Seribantumab Indication/Tumor Type Her2-receptor negative breast cancer Response Type predicted – sensitive

PMIDs: None found

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

TEND: EXEMESTANE

Alternate Names: EXEMESTANE Primary Drug Name

Drug Info: Year of Approval 1999 Drug Class antineoplastic agents

Publications:

TdgClinicalTrial: EXEMESTANE

Alternate Names:

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

Publications:

NCI: EXEMESTANE

Alternate Names: C1097 NCI drug code

Drug Info:

PharmGKB: exemestane

Alternate Names:

Drug Info:

CIViC: EXEMESTANE

Alternate Names:

Drug Info:

Publications: Gala K et al., 2018, KMT2C mediates the estrogen dependence of breast cancer through regulation of ERα enhancer function., Oncogene

TTD: Exemestane

Interaction Types & Directionality:

n/a

PMIDs:
27111237

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
29755131

Sources:
CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name exemestane ,Aromasin

Novel drug target Established target

Mechanism of Interaction Cytochrome P450 19A1 inhibitor

PMIDs:
26536870 24590773 20048079 20360896 18728707 19156139 19337436 19930708 15814851 19436613 11752352 17020418

Sources:
TdgClinicalTrial ChemblInteractions TEND PharmGKB TTD

Interaction Types & Directionality:

n/a

PMIDs:
27111237

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
15746052

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
18256205

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB FDA

Interaction Types & Directionality:

n/a

PMIDs:
25148458

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
26536870

Sources:
PharmGKB FDA

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Exemestane + Seribantumab

Indication/Tumor Type Her2-receptor negative breast cancer

Response Type predicted – sensitive

PMIDs:
None found

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Alternate Names:

EXEMESTANE Primary Drug Name

Drug Info:

Year of Approval 1999

Drug Class antineoplastic agents

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small Molecule

FDA Approval approved

Alternate Names:

C1097 NCI drug code

Publications:

Gala K et al., 2018, KMT2C mediates the estrogen dependence of breast cancer through regulation of ERα enhancer function., Oncogene

Alternate Names:

D0D2VS TTD Drug ID

Alternate Names:

CHEMBL1200374 ChEMBL Drug ID