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BEXAROTENE Drug Record

  • Summary
  • Interactions
  • Claims
  • BEXAROTENE chembl:CHEMBL1023 ApprovedAntineoplasticImmunotherapy

    Alternate Names:

    LGD1069
    LG100069
    TARGRETINE
    LGD-1069
    BEXAROTENE
    LG-100069
    TARGRETIN
    BEXAROTENUM
    P-[1-(5,6,7,8,-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTHYL)VINYL]BENZOIC ACID
    BEXAROTÈNE
    BEXAROTENO
    4-[1-(5,6,7,8,-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTALENYL)ETHENYL]BENZOIC ACID
    4-[1-(3,5,5,8,8-PENTAMETHYLTETRALIN-2-YL)ETHENYL]BENZOIC ACID
    TARGRETYN
    P-(1-(5,6,7,8-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTHYL)VINYL)BENZOIC ACID
    TARGREXIN
    TARGREXIN®
    BEXAROTEN
    pubchem.compound:82146
    rxcui:233272
    chembl:CHEMBL1023
    drugbank:00307
    chemidplus:153559-49-0

    Drug Info:

    FDA Approval approved
    Drug Class Small Molecule
    Drug Indications antineoplastic agent
    Drug Class antineoplastic agents
    Year of Approval 1999
    (5 More Sources)

    Publications:

    Yen et al., 2005, The selective retinoid X receptor agonist bexarotene (LGD1069, Targretin) prevents and overcomes multidrug resistance in advanced breast carcinoma., Mol. Cancer Ther.
    Lalloyer et al., 2006, The RXR agonist bexarotene improves cholesterol homeostasis and inhibits atherosclerosis progression in a mouse model of mixed dyslipidemia., Arterioscler. Thromb. Vasc. Biol.
    Yen et al., 2006, A selective retinoid X receptor agonist bexarotene (LGD1069, targretin) inhibits angiogenesis and metastasis in solid tumours., Br. J. Cancer
    Rigas et al., 2005, Emerging role of rexinoids in non-small cell lung cancer: focus on bexarotene., Oncologist
    Rizvi et al., 2001, Placebo-controlled trial of bexarotene, a retinoid x receptor agonist, as maintenance therapy for patients treated with chemotherapy for advanced non-small-cell lung cancer., Clin Lung Cancer
    Farol et al., 2004, Bexarotene: a clinical review., Expert Rev Anticancer Ther
    Tooker et al., 2007, Bexarotene (LGD1069, Targretin), a selective retinoid X receptor agonist, prevents and reverses gemcitabine resistance in NSCLC cells by modulating gene amplification., Cancer Res.
    Lowe et al., Bexarotene., Am J Clin Dermatol
    Tsai et al., 2008, A phase I study of bexarotene, a retinoic X receptor agonist, in non-M3 acute myeloid leukemia., Clin. Cancer Res.
    Wagner CE et al., 2009, Modeling, synthesis and biological evaluation of potential retinoid X receptor (RXR) selective agonists: novel analogues of 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene)., J Med Chem
    Ohsawa F et al., 2013, Mechanism of retinoid X receptor partial agonistic action of 1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)-1H-benzotriazole-5-carboxylic acid and structural development to increase potency., J Med Chem
    Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
    Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
    Fu et al., 2007, The retinoid X receptor-selective ligand, LGD1069, inhibits tumor-induced angiogenesis via suppression of VEGF in human non-small cell lung cancer., Cancer Lett.
  • BEXAROTENE   RXRB

    Interaction Score: 11.45

    Interaction Types & Directionality:
    activator (activating)
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Retinoid X receptor agonist
    Direct Interaction yes
    Notes

    PMIDs:
    15897247 17008586 16495926 15632250 14700480 15056048 17483357 11702369 17016423 17139284 18765556


    Sources:
    TALC TdgClinicalTrial ChemblInteractions TEND

  • BEXAROTENE   RXRG

    Interaction Score: 11.16

    Interaction Types & Directionality:
    activator (activating)
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Retinoid X receptor agonist
    Direct Interaction yes
    Trial Name bexarotene,Targretin

    PMIDs:
    15897247 17008586 16495926 15632250 14700480 15056048 17483357 11702369 18765556


    Sources:
    TALC TdgClinicalTrial ChemblInteractions TEND

  • BEXAROTENE   RXRA

    Interaction Score: 1.6

    Interaction Types & Directionality:
    activator (activating)
    agonist (activating)

    Interaction Info:
    Novel drug target Established target
    Trial Name bexarotene,Targretin
    Notes

    PMIDs:
    19791803 23391145 15897247 17008586 16495926 15632250 14700480 15056048 17483357 11702369 18765556


    Sources:
    TALC DTC TdgClinicalTrial ChemblInteractions TEND TTD

  • BEXAROTENE   NR1H3

    Interaction Score: 0.4

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • BEXAROTENE   MAPK8

    Interaction Score: 0.34

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17027148


    Sources:
    NCI

  • BEXAROTENE   BLM

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • BEXAROTENE   NR1I2

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • BEXAROTENE   KAT2A

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • BEXAROTENE   USP1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TEND: BEXAROTENE

    • Version: 01-August-2011

    Alternate Names:
    BEXAROTENE Primary Drug Name

    Drug Info:
    Year of Approval 1999
    Drug Class antineoplastic agents

    Publications:

  • TdgClinicalTrial: BEXAROTENE

    • Version: January-2014

    Alternate Names:

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

    Publications:

  • NCI: LGD1069

    • Version: 14-September-2017

    Alternate Names:
    C1635 NCI drug code

    Drug Info:

    Publications:
    Fu et al., 2007, The retinoid X receptor-selective ligand, LGD1069, inhibits tumor-induced angiogenesis via suppression of VEGF in human non-small cell lung cancer., Cancer Lett.

  • DTC: BEXAROTENE

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL1023 ChEMBL Drug ID

    Drug Info:

    Publications:
    Wagner CE et al., 2009, Modeling, synthesis and biological evaluation of potential retinoid X receptor (RXR) selective agonists: novel analogues of 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene)., J Med Chem
    Ohsawa F et al., 2013, Mechanism of retinoid X receptor partial agonistic action of 1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)-1H-benzotriazole-5-carboxylic acid and structural development to increase potency., J Med Chem

  • TALC: BEXAROTENE

    • Version: 12-May-2016

    Alternate Names:
    BEXAROTENE Primary Drug Name
    BEXAROTENE Drug Generic Name
    TARGRETIN Drug Trade Name

    Drug Info:

    Publications:

  • TTD: Bexarotene

    • Version: 2020.06.01

    Alternate Names:
    D0N0RU TTD Drug ID

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL1023

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL1023

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • PharmGKB: bexarotene

    • Version: 18-August-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