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BOSENTAN Drug Record

  • Summary
  • Interactions
  • Claims
  • BOSENTAN chembl:CHEMBL957 Approved

    Alternate Names:

    RO-470203029
    TRACLEER
    BOSENTAN MONOHYDRATE
    RO-47-0203-029
    BOSENTAN HYDRATE
    BOSENTAN
    BOSENTÁN
    TRACLEER®
    4-(1,1-DIMETHYLETHYL)-N-(6-(2-HYDROXYETHOXY)-5-(2-METHOXYPHENOXY)-(2,2'-BIPYRIMIDIN)-4-YL) BENZENESULFORNAMIDE
    BOSENTANUM
    BOSENTAN ANHYDROUS
    RO 47-0203
    P-TERT-BUTYL-N-(6-(2-HYDROXYETHOXY)-5-(O-METHOXYPHENOXY)-2-(2-PYRIMIDINYL)-4-PYRIMIDINYL)BENZENESULFONAMIDE
    pubchem.compound:104865
    drugbank:00559
    chemidplus:147536-97-8
    chembl:CHEMBL957
    rxcui:1468845

    Drug Info:

    Drug Class antihypertensive agents
    Year of Approval 2001
    FDA Approval approved
    Drug Class Small Molecule
    Drug Indications for treatment of pulmonary arterial hypertension
    (2 More Sources)

    Publications:

    Sihvola et al., 2002, Crosstalk of endothelin-1 and platelet-derived growth factor in cardiac allograft arteriosclerosis., J. Am. Coll. Cardiol.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Kiowski et al., 2001, Hemodynamic effects of bosentan in patients with chronic heart failure., Heart Fail Rev
    Martin et al., 2000, Differential effects of the mixed ET(A)/ET(B)-receptor antagonist bosentan on endothelin-induced bronchoconstriction, vasoconstriction and prostacyclin release., Naunyn Schmiedebergs Arch. Pharmacol.
    Albertini et al., 2001, Endothelin involvement in respiratory centre activity., Prostaglandins Leukot. Essent. Fatty Acids
    Kramp et al., 2001, Endothelin resets renal blood flow autoregulatory efficiency during acute blockade of NO in the rat., Am. J. Physiol. Renal Physiol.
    Gupta et al., 2005, Bosentan, the mixed ETA-ETB endothelin receptor antagonist, attenuated oxidative stress after experimental myocardial ischemia and reperfusion., Mol. Cell. Biochem.
    Gardiner et al., 1994, Effects of bosentan (Ro 47-0203), an ETA-, ETB-receptor antagonist, on regional haemodynamic responses to endothelins in conscious rats., Br. J. Pharmacol.
    Richard et al., 1994, Role of endogenous endothelin in myocardial and coronary endothelial injury after ischaemia and reperfusion in rats: studies with bosentan, a mixed ETA-ETB antagonist., Br. J. Pharmacol.
    Said et al., 2005, Effect of bosentan (ETA/ETB receptor antagonist) on metabolic changes during stress and diabetes., Pharmacol. Res.
    Marano et al., 1998, ET(A)/ET(B) receptor antagonist bosentan inhibits neointimal development in collared carotid arteries of rabbits., Life Sci.
    Treiber et al., 2007, Bosentan is a substrate of human OATP1B1 and OATP1B3: inhibition of hepatic uptake as the common mechanism of its interactions with cyclosporin A, rifampicin, and sildenafil., Drug Metab. Dispos.
  • BOSENTAN   EDNRB

    Interaction Score: 19.32

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name Tracleer
    Direct Interaction yes

    PMIDs:
    16335785 7921608 7858879 15629255 11752352 9806221


    Sources:
    TdgClinicalTrial ChemblInteractions TEND TTD

  • BOSENTAN   EDNRA

    Interaction Score: 9.66

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Endothelin receptor, ET-A/ET-B antagonist
    Direct Interaction yes
    Trial Name Tracleer

    PMIDs:
    11849873 11752352 11447307 10961375 11728166 11704565


    Sources:
    TdgClinicalTrial ChemblInteractions TEND TTD

  • BOSENTAN   SLCO1B1

    Interaction Score: 0.59

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17496208


    Sources:
    PharmGKB

  • BOSENTAN   NR1I2

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • TEND: BOSENTAN

    • Version: 01-August-2011

    Alternate Names:
    BOSENTAN Primary Drug Name

    Drug Info:
    Year of Approval 2001
    Drug Class antihypertensive agents

    Publications:

  • TdgClinicalTrial: BOSENTAN

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications for treatment of pulmonary arterial hypertension
    Drug Class Small Molecule
    FDA Approval approved

    Publications:

  • PharmGKB: bosentan

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Treiber et al., 2007, Bosentan is a substrate of human OATP1B1 and OATP1B3: inhibition of hepatic uptake as the common mechanism of its interactions with cyclosporin A, rifampicin, and sildenafil., Drug Metab. Dispos.

  • TTD: Bosentan

    • Version: 2020.06.01

    Alternate Names:
    D0U4CE TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL957

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL957

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

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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