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EXEMESTANE Drug Record

  • Summary
  • Interactions
  • Claims
  • 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:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21