DGIdb - BOSENTAN Drug Record

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

(3 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: 17.54

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 GuideToPharmacology TTD
BOSENTAN EDNRA

Interaction Score: 8.86

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: 0.6

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:
GuideToPharmacology: 178100482
- Version: 29-September-2020
Alternate Names:

BOSENTAN GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL957
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL957
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Novel drug target	Established target
Trial Name	Tracleer
Direct Interaction	yes

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

BOSENTAN Drug Record

BOSENTAN chembl:CHEMBL957 Approved

Alternate Names:

Drug Info:

Publications:

BOSENTAN EDNRB

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 GuideToPharmacology TTD

BOSENTAN EDNRA

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 Types & Directionality: n/a

Interaction Info:

PMIDs: 17496208

Sources: PharmGKB

BOSENTAN NR1I2

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

TEND: BOSENTAN

Alternate Names: BOSENTAN Primary Drug Name

Drug Info: Year of Approval 2001 Drug Class antihypertensive agents

Publications:

TdgClinicalTrial: BOSENTAN

Alternate Names:

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

Publications:

PharmGKB: bosentan

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

Alternate Names: D0U4CE TTD Drug ID

Drug Info:

Publications:

GuideToPharmacology: 178100482

Alternate Names: BOSENTAN GuideToPharmacology Ligand Name

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL957

Alternate Names:

Drug Info:

Publications:

ChemblInteractions: CHEMBL957

Alternate Names:

Drug Info:

Publications:

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 GuideToPharmacology TTD

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

Interaction Types & Directionality:

n/a

PMIDs:
17496208

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Alternate Names:

BOSENTAN Primary Drug Name

Drug Info:

Year of Approval 2001

Drug Class antihypertensive agents

Drug Info:

Drug Indications for treatment of pulmonary arterial hypertension

Drug Class Small Molecule

FDA Approval approved

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.

Alternate Names:

D0U4CE TTD Drug ID

Alternate Names:

BOSENTAN GuideToPharmacology Ligand Name