Details of the Drug

General Information of Drug (ID: DMIOGBU)

Drug Name
Bosentan
Synonyms
Actelion; Bosentanum; Tracleer; Bosentan (INN); KS-5062; Ro 47-0203; Tracleer (TN); Bosentan [USAN:INN:BAN]; Ro 47-0203/039; Ro-47-0203; Ro-47-0203/029; Ro-47-0203/039; P-tert-Butyl-N-[6-(2-hydroxyethoxy); P-tert-Butyl-N-(6-(2-hydroxyethoxy)-5-(o-methoxyphenoxy)-2-(2-pyrimidinyl)-4-pyrimidinyl)benzenesulfonamide; 4-(1,1-Dimethylethyl)-N-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-(2,2'-bipyrimidin)-4-yl) benzenesulfornamide; 4-(1,1-Dimethylethyl)-N-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-(2,2'-bipyrimidin)-4-yl)benzenesulfornamide; 4-t-butyl-N-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2,2'-bipyrimidin-4-yl)benzenesulfonamide; 4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2,2'-bipyrimidin-4-yl]benzenesulfonamide; 4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-pyrimidin-2-ylpyrimidin-4-yl]benzenesulfonamide
Indication
Disease Entry ICD 11 Status REF
Pulmonary arterial hypertension BB01.0 Approved [1]
Pulmonary hypertension BB01 Approved [2]
Scleroderma 4A42 Investigative [2]
Therapeutic Class
Antihypertensive Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 3 Molecular Weight (mw) 551.6
Logarithm of the Partition Coefficient (xlogp) 3.8
Rotatable Bond Count (rotbonds) 11
Hydrogen Bond Donor Count (hbonddonor) 2
Hydrogen Bond Acceptor Count (hbondacc) 11
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [3]
Bioavailability
The bioavailability of drug is 50% []
Clearance
The drug present in the plasma can be removed from the body at the rate of 2.1 mL/min/kg [4]
Elimination
2% of drug is excreted from urine in the unchanged form [3]
Half-life
The concentration or amount of drug in body reduced by one-half in 5 hours [4]
Metabolism
The drug is metabolized via the liver []
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 6.474 micromolar/kg/day [5]
Unbound Fraction
The unbound fraction of drug in plasma is 0.037% [4]
Vd
The volume of distribution (Vd) of drug is 18 L []
Water Solubility
The ability of drug to dissolve in water is measured as 0.001 mg/mL [3]
Adverse Drug Reaction (ADR)
ADR Term Variation Related DOT DOT ID REF
Liver disorder Not Available NOS3 OTLDT7NR [6]
Chemical Identifiers
Formula
C27H29N5O6S
IUPAC Name
4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-pyrimidin-2-ylpyrimidin-4-yl]benzenesulfonamide
Canonical SMILES
CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)NC2=C(C(=NC(=N2)C3=NC=CC=N3)OCCO)OC4=CC=CC=C4OC
InChI
InChI=1S/C27H29N5O6S/c1-27(2,3)18-10-12-19(13-11-18)39(34,35)32-23-22(38-21-9-6-5-8-20(21)36-4)26(37-17-16-33)31-25(30-23)24-28-14-7-15-29-24/h5-15,33H,16-17H2,1-4H3,(H,30,31,32)
InChIKey
GJPICJJJRGTNOD-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
104865
ChEBI ID
CHEBI:51450
CAS Number
147536-97-8
DrugBank ID
DB00559
TTD ID
D0U4CE
VARIDT ID
DR00288
INTEDE ID
DR0222
ACDINA ID
D00074
Combinatorial Drugs (CBD) Click to Jump to the Detailed CBD Information of This Drug
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Endothelin A receptor (EDNRA) TTKRD0G EDNRA_HUMAN Modulator [7]
Endothelin B receptor (EDNRB) TT3ZTGU EDNRB_HUMAN Modulator [7]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTPFTEQ SO2B1_HUMAN Substrate [8]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [8]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Substrate [8]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME 		DE4LYSA CP3A4_HUMAN Substrate [9]
Cytochrome P450 2C9 (CYP2C9)
Main DME 		DE5IED8 CP2C9_HUMAN Substrate [10]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
2-aminomuconic semialdehyde dehydrogenase (ALDH8A1) OTINY3MW AL8A1_HUMAN Gene/Protein Processing [11]
3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1 (HSD3B1) OTNAZVKB 3BHS1_HUMAN Gene/Protein Processing [11]
Achaete-scute homolog 1 (ASCL1) OTI4X44G ASCL1_HUMAN Gene/Protein Processing [11]
Alcohol dehydrogenase 1A (ADH1A) OTTS983E ADH1A_HUMAN Gene/Protein Processing [11]
Alcohol dehydrogenase 1C (ADH1C) OTO1DV7F ADH1G_HUMAN Gene/Protein Processing [11]
All-trans-retinol dehydrogenase ADH1B (ADH1B) OTV3TB81 ADH1B_HUMAN Gene/Protein Processing [11]
All-trans-retinol dehydrogenase ADH4 (ADH4) OTKDKKNG ADH4_HUMAN Gene/Protein Processing [11]
Amino acid transporter heavy chain SLC3A2 (SLC3A2) OTBR33M9 4F2_HUMAN Gene/Protein Processing [11]
ATP-binding cassette sub-family C member 2 (ABCC2) OTJSIGV5 MRP2_HUMAN Gene/Protein Processing [12]
ATP-binding cassette sub-family C member 3 (ABCC3) OTC3IJV4 MRP3_HUMAN Gene/Protein Processing [12]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Pulmonary arterial hypertension
ICD Disease Classification BB01.0
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Endothelin A receptor (EDNRA) DTT EDNRA 3.19E-05 -2.69 -1.71
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTP OATP2B1 2.89E-11 -1.11E+00 -2.81E+00
Organic anion transporting polypeptide 1B3 (SLCO1B3) DTP OATP1B3 2.08E-04 3.94E-02 1.17E-01
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 7.59E-01 -3.08E-02 -1.64E-01
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 4.97E-04 -1.04E+00 -1.67E+00
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 1.10E-01 -1.23E-01 -2.88E-01
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Bosentan
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Riociguat DMXBLMP Moderate Increased metabolism of Bosentan caused by Riociguat mediated induction of CYP450 enzyme. Pulmonary hypertension [BB01] [13]
Coadministration of a Drug Treating the Disease Different from Bosentan (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Remdesivir DMBFZ6L Moderate Increased risk of hepatotoxicity by the combination of Bosentan and Remdesivir. 1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019] [14]
Tretinoin DM49DUI Moderate Increased metabolism of Bosentan caused by Tretinoin mediated induction of CYP450 enzyme. Acne vulgaris [ED80] [15]
Repaglinide DM5SXUV Moderate Increased metabolism of Bosentan caused by Repaglinide mediated induction of CYP450 enzyme. Acute diabete complication [5A2Y] [16]
Tolazamide DMIHRNA Moderate Increased metabolism of Bosentan caused by Tolazamide mediated induction of CYP450 enzyme. Acute diabete complication [5A2Y] [15]
Pioglitazone DMKJ485 Moderate Increased metabolism of Bosentan caused by Pioglitazone mediated induction of CYP450 enzyme. Acute diabete complication [5A2Y] [15]
Glipizide DMZA5PQ Moderate Increased metabolism of Bosentan caused by Glipizide mediated induction of CYP450 enzyme. Acute diabete complication [5A2Y] [15]
Midostaurin DMI6E0R Moderate Increased metabolism of Bosentan caused by Midostaurin mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [17]
Arn-509 DMT81LZ Moderate Accelerated clearance of Bosentan due to the transporter induction by Arn-509. Acute myeloid leukaemia [2A60] [18]
Gilteritinib DMTI0ZO Moderate Increased metabolism of Bosentan caused by Gilteritinib mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [19]
Oliceridine DM6MDCF Major Increased metabolism of Bosentan caused by Oliceridine mediated induction of CYP450 enzyme. Acute pain [MG31] [20]
Donepezil DMIYG7Z Moderate Increased metabolism of Bosentan caused by Donepezil mediated induction of CYP450 enzyme. Alzheimer disease [8A20] [15]
Metronidazole DMTIVEN Moderate Decreased metabolism of Bosentan caused by Metronidazole mediated inhibition of CYP450 enzyme. Amoebiasis [1A36] [15]
Ivabradine DM0L594 Moderate Increased metabolism of Bosentan caused by Ivabradine mediated induction of CYP450 enzyme. Angina pectoris [BA40] [18]
Bepridil DM0RKS4 Moderate Increased metabolism of Bosentan caused by Bepridil mediated induction of CYP450 enzyme. Angina pectoris [BA40] [15]
Dronedarone DMA8FS5 Moderate Increased metabolism of Bosentan caused by Dronedarone mediated induction of CYP450 enzyme. Angina pectoris [BA40] [21]
Nifedipine DMSVOZT Moderate Increased metabolism of Bosentan caused by Nifedipine mediated induction of CYP450 enzyme. Angina pectoris [BA40] [15]
Bedaquiline DM3906J Major Increased metabolism of Bosentan caused by Bedaquiline mediated induction of CYP450 enzyme. Antimicrobial drug resistance [MG50-MG52] [18]
Cilostazol DMZMSCT Moderate Increased metabolism of Bosentan caused by Cilostazol mediated induction of CYP450 enzyme. Arterial occlusive disease [BD40] [15]
Voriconazole DMAOL2S Moderate Increased metabolism of Bosentan caused by Voriconazole mediated induction of CYP450 enzyme. Aspergillosis [1F20] [14]
Posaconazole DMUL5EW Moderate Decreased metabolism of Bosentan caused by Posaconazole mediated inhibition of CYP450 enzyme. Aspergillosis [1F20] [15]
Zileuton DMVRIC2 Moderate Increased metabolism of Bosentan caused by Zileuton mediated induction of CYP450 enzyme. Asthma [CA23] [15]
Dalfopristin DM4LTKV Moderate Decreased metabolism of Bosentan caused by Dalfopristin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [15]
Clarithromycin DM4M1SG Moderate Increased metabolism of Bosentan caused by Clarithromycin mediated induction of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [15]
Troleandomycin DMUZNIG Moderate Decreased metabolism of Bosentan caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [15]
Telithromycin DMZ4P3A Moderate Increased metabolism of Bosentan caused by Telithromycin mediated induction of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [22]
Ag-221 DMS0ZBI Moderate Decreased clearance of Bosentan due to the transporter inhibition by Ag-221. BCR-ABL1-negative chronic myeloid leukaemia [2A41] [14]
Cariprazine DMJYDVK Moderate Increased metabolism of Bosentan caused by Cariprazine mediated induction of CYP450 enzyme. Bipolar disorder [6A60] [23]
Erdafitinib DMI782S Major Increased metabolism of Bosentan caused by Erdafitinib mediated induction of CYP450 enzyme. Bladder cancer [2C94] [24]
Pexidartinib DMS2J0Z Major Increased risk of hepatotoxicity by the combination of Bosentan and Pexidartinib. Bone/articular cartilage neoplasm [2F7B] [25]
Ixabepilone DM2OZ3G Moderate Increased metabolism of Bosentan caused by Ixabepilone mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [26]
Lapatinib DM3BH1Y Moderate Increased metabolism of Bosentan caused by Lapatinib mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [14]
HKI-272 DM6QOVN Major Increased metabolism of Bosentan caused by HKI-272 mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [14]
LY2835219 DM93VBZ Moderate Increased metabolism of Bosentan caused by LY2835219 mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [27]
Exemestane DM9HPW3 Moderate Increased metabolism of Bosentan caused by Exemestane mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [28]
Esterified estrogens DM9KZDO Moderate Increased metabolism of Bosentan caused by Esterified estrogens mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [29]
Tucatinib DMBESUA Moderate Increased metabolism of Bosentan caused by Tucatinib mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [30]
Alpelisib DMEXMYK Moderate Increased metabolism of Bosentan caused by Alpelisib mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [31]
Letrozole DMH07Y3 Moderate Increased metabolism of Bosentan caused by Letrozole mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [15]
Quinestrol DMJ6H1Z Moderate Increased metabolism of Bosentan caused by Quinestrol mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [29]
Tamoxifen DMLB0EZ Moderate Increased metabolism of Bosentan caused by Tamoxifen mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [32]
Cabazitaxel DMPAZHC Moderate Increased metabolism of Bosentan caused by Cabazitaxel mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [33]
Bosutinib DMTI8YE Major Increased metabolism of Bosentan caused by Bosutinib mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [34]
Estradiol DMUNTE3 Moderate Increased metabolism of Bosentan caused by Estradiol mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [29]
Atorvastatin DMF28YC Moderate Increased metabolism of Bosentan caused by Atorvastatin mediated induction of CYP450 enzyme. Cardiovascular disease [BA00-BE2Z] [15]
Macitentan DMP79A1 Moderate Increased metabolism of Bosentan caused by Macitentan mediated induction of CYP450 enzyme. Cardiovascular disease [BA00-BE2Z] [35]
PF-04449913 DMSB068 Major Increased metabolism of Bosentan caused by PF-04449913 mediated induction of CYP450 enzyme. Chronic myelomonocytic leukaemia [2A40] [36]
Phenylbutazone DMAYL0T Moderate Decreased metabolism of Bosentan caused by Phenylbutazone mediated inhibition of CYP450 enzyme. Chronic pain [MG30] [15]
Dihydrocodeine DMB0FWL Moderate Increased metabolism of Bosentan caused by Dihydrocodeine mediated induction of CYP450 enzyme. Chronic pain [MG30] [37]
Anisindione DM2C48U Moderate Increased metabolism of Bosentan caused by Anisindione mediated induction of CYP450 enzyme. Coagulation defect [3B10] [38]
Irinotecan DMP6SC2 Moderate Increased metabolism of Bosentan caused by Irinotecan mediated induction of CYP450 enzyme. Colorectal cancer [2B91] [39]
Drospirenone DM1A9W3 Major Increased metabolism of Bosentan caused by Drospirenone mediated induction of CYP450 enzyme. Contraceptive management [QA21] [40]
Levonorgestrel DM1DP7T Major Increased metabolism of Bosentan caused by Levonorgestrel mediated induction of CYP450 enzyme. Contraceptive management [QA21] [40]
Ulipristal DMBNI20 Moderate Increased metabolism of Bosentan caused by Ulipristal mediated induction of CYP450 enzyme. Contraceptive management [QA21] [18]
Mestranol DMG3F94 Major Increased metabolism of Bosentan caused by Mestranol mediated induction of CYP450 enzyme. Contraceptive management [QA21] [41]
Norgestimate DMYP4XC Major Increased metabolism of Bosentan caused by Norgestimate mediated induction of CYP450 enzyme. Contraceptive management [QA21] [41]
Levobupivacaine DM783CH Minor Increased metabolism of Bosentan caused by Levobupivacaine mediated induction of CYP450 enzyme. Corneal disease [9A76-9A78] [42]
Halothane DM80OZ5 Moderate Increased metabolism of Bosentan caused by Halothane mediated induction of CYP450 enzyme. Corneal disease [9A76-9A78] [15]
Cocaine DMSOX7I Moderate Increased metabolism of Bosentan caused by Cocaine mediated induction of CYP450 enzyme. Corneal disease [9A76-9A78] [43]
Alfentanil DMVO0UB Moderate Increased metabolism of Bosentan caused by Alfentanil mediated induction of CYP450 enzyme. Corneal disease [9A76-9A78] [44]
Mifepristone DMGZQEF Moderate Decreased metabolism of Bosentan caused by Mifepristone mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [45]
Osilodrostat DMIJC9X Moderate Increased metabolism of Bosentan caused by Osilodrostat mediated induction of CYP450 enzyme. Cushing syndrome [5A70] [46]
MK-8228 DMOB58Q Moderate Decreased metabolism of Bosentan caused by MK-8228 mediated inhibition of CYP450 enzyme. Cytomegaloviral disease [1D82] [14]
Rivaroxaban DMQMBZ1 Moderate Increased metabolism of Bosentan caused by Rivaroxaban mediated induction of CYP450 enzyme. Deep vein thrombosis [BD71] [47]
Aprepitant DM053KT Moderate Increased metabolism of Bosentan caused by Aprepitant mediated induction of CYP450 enzyme. Depression [6A70-6A7Z] [48]
Vilazodone DM4LECQ Moderate Increased metabolism of Bosentan caused by Vilazodone mediated induction of CYP450 enzyme. Depression [6A70-6A7Z] [49]
Vortioxetine DM6F1PU Moderate Increased metabolism of Bosentan caused by Vortioxetine mediated induction of CYP450 enzyme. Depression [6A70-6A7Z] [50]
Trazodone DMK1GBJ Moderate Increased metabolism of Bosentan caused by Trazodone mediated induction of CYP450 enzyme. Depression [6A70-6A7Z] [15]
[3H]estrone-3-sulphate DMGPF0N Moderate Increased metabolism of Bosentan caused by [3H]estrone-3-sulphate mediated induction of CYP450 enzyme. Discovery agent [N.A.] [51]
Oxybutynine DMJPBAX Moderate Increased metabolism of Bosentan caused by Oxybutynine mediated induction of CYP450 enzyme. Discovery agent [N.A.] [15]
Ospemifene DMC4GEI Moderate Increased metabolism of Bosentan caused by Ospemifene mediated induction of CYP450 enzyme. Dyspareunia [GA12] [52]
Oestradiol valerate and dienogest DMZK0FQ Major Increased metabolism of Bosentan caused by Oestradiol valerate and dienogest mediated induction of CYP450 enzyme. Endometriosis [GA10] [41]
Zonisamide DM0DTF7 Moderate Increased metabolism of Bosentan caused by Zonisamide mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [15]
Ethosuximide DMDZ9LT Moderate Increased metabolism of Bosentan caused by Ethosuximide mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [15]
Tiagabine DMKSQG0 Moderate Increased metabolism of Bosentan caused by Tiagabine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [15]
Fosphenytoin DMOX3LB Moderate Increased metabolism of Bosentan caused by Fosphenytoin mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [14]
Clonazepam DMTO13J Moderate Increased metabolism of Bosentan caused by Clonazepam mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [15]
Rufinamide DMWE60C Moderate Increased metabolism of Bosentan caused by Rufinamide mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [18]
Carbamazepine DMZOLBI Moderate Increased metabolism of Bosentan caused by Carbamazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [14]
Cannabidiol DM0659E Moderate Increased risk of hepatotoxicity by the combination of Bosentan and Cannabidiol. Epileptic encephalopathy [8A62] [18]
Nicardipine DMCDYW7 Moderate Increased metabolism of Bosentan caused by Nicardipine mediated induction of CYP450 enzyme. Essential hypertension [BA00] [15]
Mefenamic acid DMK7HFI Moderate Increased metabolism of Bosentan caused by Mefenamic acid mediated induction of CYP450 enzyme. Female pelvic pain [GA34] [15]
Praziquantel DMOU1PK Moderate Increased metabolism of Bosentan caused by Praziquantel mediated induction of CYP450 enzyme. Flatworm infection [1F70-1F86] [53]
Bay 80-6946 DMLOS5R Moderate Increased metabolism of Bosentan caused by Bay 80-6946 mediated induction of CYP450 enzyme. Follicular lymphoma [2A80] [54]
Tazemetostat DMWP1BH Major Increased metabolism of Bosentan caused by Tazemetostat mediated induction of CYP450 enzyme. Follicular lymphoma [2A80] [55]
Solifenacin DMG592Q Moderate Increased metabolism of Bosentan caused by Solifenacin mediated induction of CYP450 enzyme. Functional bladder disorder [GC50] [56]
Mirabegron DMS1GYT Minor Increased metabolism of Bosentan caused by Mirabegron mediated induction of CYP450 enzyme. Functional bladder disorder [GC50] [57]
Itraconazole DMCR1MV Moderate Decreased metabolism of Bosentan caused by Itraconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [15]
Miconazole DMPMYE8 Moderate Decreased metabolism of Bosentan caused by Miconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [14]
Ketoconazole DMPZI3Q Moderate Increased metabolism of Bosentan caused by Ketoconazole mediated induction of CYP450 enzyme. Fungal infection [1F29-1F2F] [15]
Cisapride DMY7PED Moderate Increased metabolism of Bosentan caused by Cisapride mediated induction of CYP450 enzyme. Gastro-oesophageal reflux disease [DA22] [15]
Ripretinib DM958QB Moderate Increased metabolism of Bosentan caused by Ripretinib mediated induction of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [14]
Sunitinib DMCBJSR Moderate Increased metabolism of Bosentan caused by Sunitinib mediated induction of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [14]
Avapritinib DMK2GZX Major Increased metabolism of Bosentan caused by Avapritinib mediated induction of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [18]
Ergotamine DMKR3C5 Moderate Increased metabolism of Bosentan caused by Ergotamine mediated induction of CYP450 enzyme. Headache [8A80-8A84] [14]
Boceprevir DMBSHMF Moderate Decreased metabolism of Bosentan caused by Boceprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [58]
Telaprevir DMMRV29 Moderate Decreased metabolism of Bosentan caused by Telaprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [58]
Daclatasvir DMSFK9V Major Increased metabolism of Bosentan caused by Daclatasvir mediated induction of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [18]
Isoniazid DM5JVS3 Moderate Decreased metabolism of Bosentan caused by Isoniazid mediated inhibition of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [15]
Rifapentine DMCHV4I Moderate Increased metabolism of Bosentan caused by Rifapentine mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [59]
Pretomanid DMDYA31 Major Increased metabolism of Bosentan caused by Pretomanid mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [60]
Brentuximab vedotin DMWLC57 Moderate Increased risk of hepatotoxicity by the combination of Bosentan and Brentuximab vedotin. Hodgkin lymphoma [2B30] [61]
MK-1439 DM215WE Major Increased metabolism of Bosentan caused by MK-1439 mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [18]
Delavirdine DM3NF5G Moderate Increased metabolism of Bosentan caused by Delavirdine mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [62]
Fosamprenavir DM4W9B3 Moderate Increased metabolism of Bosentan caused by Fosamprenavir mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [14]
Fostemsavir DM50ILT Moderate Decreased clearance of Bosentan due to the transporter inhibition by Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [63]
Efavirenz DMC0GSJ Moderate Increased metabolism of Bosentan caused by Efavirenz mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [64]
Dolutegravir DMCZGRE Minor Increased metabolism of Bosentan caused by Dolutegravir mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [65]
Saquinavir DMG814N Moderate Decreased metabolism of Bosentan caused by Saquinavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [14]
Elvitegravir DMG9B1U Moderate Increased metabolism of Bosentan caused by Elvitegravir mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [14]
Rilpivirine DMJ0QOW Moderate Increased metabolism of Bosentan caused by Rilpivirine mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [14]
Amprenavir DMLMXE0 Moderate Decreased metabolism of Bosentan caused by Amprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [14]
Atazanavir DMSYRBX Moderate Increased metabolism of Bosentan caused by Atazanavir mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [14]
Maraviroc DMTL94F Moderate Increased metabolism of Bosentan caused by Maraviroc mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [14]
Bempedoic acid DM1CI9R Moderate Decreased clearance of Bosentan due to the transporter inhibition by Bempedoic acid. Hyper-lipoproteinaemia [5C80] [66]
Simvastatin DM30SGU Moderate Increased metabolism of Bosentan caused by Simvastatin mediated induction of CYP450 enzyme. Hyper-lipoproteinaemia [5C80] [15]
Fluvastatin DM4MDJY Moderate Decreased metabolism of Bosentan caused by Fluvastatin mediated inhibition of CYP450 enzyme. Hyper-lipoproteinaemia [5C80] [15]
Fenofibrate DMFKXDY Moderate Decreased metabolism of Bosentan caused by Fenofibrate mediated inhibition of CYP450 enzyme. Hyper-lipoproteinaemia [5C80] [14]
Mipomersen DMGSRN1 Major Increased risk of hepatotoxicity by the combination of Bosentan and Mipomersen. Hyper-lipoproteinaemia [5C80] [67]
Teriflunomide DMQ2FKJ Major Increased risk of hepatotoxicity by the combination of Bosentan and Teriflunomide. Hyper-lipoproteinaemia [5C80] [20]
BMS-201038 DMQTAGO Major Increased risk of hepatotoxicity by the combination of Bosentan and BMS-201038. Hyper-lipoproteinaemia [5C80] [68]
Losartan DM72JXH Moderate Increased metabolism of Bosentan caused by Losartan mediated induction of CYP450 enzyme. Hypertension [BA00-BA04] [15]
Levamlodipine DM92S6N Moderate Increased metabolism of Bosentan caused by Levamlodipine mediated induction of CYP450 enzyme. Hypertension [BA00-BA04] [15]
Verapamil DMA7PEW Moderate Increased metabolism of Bosentan caused by Verapamil mediated induction of CYP450 enzyme. Hypertension [BA00-BA04] [15]
Irbesartan DMTP1DC Moderate Increased metabolism of Bosentan caused by Irbesartan mediated induction of CYP450 enzyme. Hypertension [BA00-BA04] [15]
Conivaptan DM1V329 Moderate Decreased metabolism of Bosentan caused by Conivaptan mediated inhibition of CYP450 enzyme. Hypo-osmolality/hyponatraemia [5C72] [15]
Tolvaptan DMIWFRL Moderate Increased metabolism of Bosentan caused by Tolvaptan mediated induction of CYP450 enzyme. Hypo-osmolality/hyponatraemia [5C72] [18]
Fludrocortisone DMUDIR8 Moderate Increased metabolism of Bosentan caused by Fludrocortisone mediated induction of CYP450 enzyme. Hypo-osmolality/hyponatraemia [5C72] [15]
Lesinurad DMUR64T Moderate Increased metabolism of Bosentan caused by Lesinurad mediated induction of CYP450 enzyme. Inborn purine/pyrimidine/nucleotide metabolism error [5C55] [69]
Berotralstat DMWA2DZ Moderate Decreased metabolism of Bosentan caused by Berotralstat mediated inhibition of CYP450 enzyme. Innate/adaptive immunodeficiency [4A00] [15]
Suvorexant DM0E6S3 Moderate Increased metabolism of Bosentan caused by Suvorexant mediated induction of CYP450 enzyme. Insomnia [7A00-7A0Z] [70]
Ramelteon DM7IW9J Moderate Increased metabolism of Bosentan caused by Ramelteon mediated induction of CYP450 enzyme. Insomnia [7A00-7A0Z] [71]
Zaleplon DMGFWSM Moderate Increased metabolism of Bosentan caused by Zaleplon mediated induction of CYP450 enzyme. Insomnia [7A00-7A0Z] [15]
ITI-007 DMUQ1DO Major Increased metabolism of Bosentan caused by ITI-007 mediated induction of CYP450 enzyme. Insomnia [7A00-7A0Z] [72]
Quazepam DMY4D87 Moderate Increased metabolism of Bosentan caused by Quazepam mediated induction of CYP450 enzyme. Insomnia [7A00-7A0Z] [15]
Estazolam DMZGXUM Moderate Increased metabolism of Bosentan caused by Estazolam mediated induction of CYP450 enzyme. Insomnia [7A00-7A0Z] [15]
Naloxegol DML0B41 Moderate Increased metabolism of Bosentan caused by Naloxegol mediated induction of CYP450 enzyme. Large intestine motility disorder [DB32] [73]
Methotrexate DM2TEOL Moderate Increased risk of hepatotoxicity by the combination of Bosentan and Methotrexate. Leukaemia [2A60-2B33] [18]
Pemigatinib DM819JF Major Increased metabolism of Bosentan caused by Pemigatinib mediated induction of CYP450 enzyme. Liver cancer [2C12] [18]
Testosterone DM7HUNW Moderate Increased metabolism of Bosentan caused by Testosterone mediated induction of CYP450 enzyme. Low bone mass disorder [FB83] [15]
Crizotinib DM4F29C Moderate Increased metabolism of Bosentan caused by Crizotinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [74]
Brigatinib DM7W94S Major Increased metabolism of Bosentan caused by Brigatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [14]
Ceritinib DMB920Z Moderate Increased metabolism of Bosentan caused by Ceritinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [15]
Lurbinectedin DMEFRTZ Major Decreased metabolism of Bosentan caused by Lurbinectedin mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [75]
PF-06463922 DMKM7EW Major Increased metabolism of Bosentan caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [76]
Osimertinib DMRJLAT Moderate Increased metabolism of Bosentan caused by Osimertinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [77]
Pralsetinib DMWU0I2 Moderate Increased metabolism of Bosentan caused by Pralsetinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [78]
Capmatinib DMYCXKL Major Increased metabolism of Bosentan caused by Capmatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [79]
Selpercatinib DMZR15V Major Increased metabolism of Bosentan caused by Selpercatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [18]
Artemether DM48QOT Moderate Increased metabolism of Bosentan caused by Artemether mediated induction of CYP450 enzyme. Malaria [1F40-1F45] [14]
Calaspargase pegol DMQZBXI Moderate Increased risk of hepatotoxicity by the combination of Bosentan and Calaspargase pegol. Malignant haematopoietic neoplasm [2B33] [80]
Idelalisib DM602WT Moderate Increased risk of hepatotoxicity by the combination of Bosentan and Idelalisib. Mature B-cell leukaemia [2A82] [81]
GDC-0199 DMH0QKA Major Increased metabolism of Bosentan caused by GDC-0199 mediated induction of CYP450 enzyme. Mature B-cell leukaemia [2A82] [82]
IPI-145 DMWA24P Moderate Decreased metabolism of Bosentan caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [15]
Acalabrutinib DM7GCVW Moderate Increased metabolism of Bosentan caused by Acalabrutinib mediated induction of CYP450 enzyme. Mature B-cell lymphoma [2A85] [83]
Clofarabine DMCVJ86 Moderate Increased risk of hepatotoxicity by the combination of Bosentan and Clofarabine. Mature B-cell lymphoma [2A85] [84]
Vemurafenib DM62UG5 Moderate Increased metabolism of Bosentan caused by Vemurafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [85]
Selumetinib DMC7W6R Major Increased metabolism of Bosentan caused by Selumetinib mediated induction of CYP450 enzyme. Melanoma [2C30] [86]
LGX818 DMNQXV8 Major Increased metabolism of Bosentan caused by LGX818 mediated induction of CYP450 enzyme. Melanoma [2C30] [87]
Dabrafenib DMX6OE3 Moderate Increased metabolism of Bosentan caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [18]
Estrone DM5T6US Moderate Increased metabolism of Bosentan caused by Estrone mediated induction of CYP450 enzyme. Menopausal disorder [GA30] [29]
Ethinyl estradiol DMODJ40 Major Increased metabolism of Bosentan caused by Ethinyl estradiol mediated induction of CYP450 enzyme. Menopausal disorder [GA30] [41]
Danazol DML8KTN Moderate Decreased metabolism of Bosentan caused by Danazol mediated inhibition of CYP450 enzyme. Menstrual cycle bleeding disorder [GA20] [15]
Ubrogepant DM749I3 Moderate Increased metabolism of Bosentan caused by Ubrogepant mediated induction of CYP450 enzyme. Migraine [8A80] [88]
Rimegepant DMHOAUG Major Increased metabolism of Bosentan caused by Rimegepant mediated induction of CYP450 enzyme. Migraine [8A80] [89]
Exjade DMHPRWG Moderate Decreased metabolism of Bosentan caused by Exjade mediated inhibition of CYP450 enzyme. Mineral absorption/transport disorder [5C64] [90]
Flibanserin DM70DTN Moderate Increased metabolism of Bosentan caused by Flibanserin mediated induction of CYP450 enzyme. Mood disorder [6A60-6E23] [91]
Midazolam DMXOELT Moderate Increased metabolism of Bosentan caused by Midazolam mediated induction of CYP450 enzyme. Mood/affect symptom [MB24] [15]
Siponimod DM2R86O Major Increased metabolism of Bosentan caused by Siponimod mediated induction of CYP450 enzyme. Multiple sclerosis [8A40] [14]
Deflazacort DMV0RNS Major Increased metabolism of Bosentan caused by Deflazacort mediated induction of CYP450 enzyme. Muscular dystrophy [8C70] [18]
Rifabutin DM1YBHK Moderate Increased metabolism of Bosentan caused by Rifabutin mediated induction of CYP450 enzyme. Mycobacterium infection [1B10-1B21] [14]
Fedratinib DM4ZBK6 Major Increased metabolism of Bosentan caused by Fedratinib mediated induction of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [18]
Ruxolitinib DM7Q98D Moderate Increased metabolism of Bosentan caused by Ruxolitinib mediated induction of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [92]
Imatinib DM7RJXL Moderate Increased metabolism of Bosentan caused by Imatinib mediated induction of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [15]
Dasatinib DMJV2EK Moderate Increased metabolism of Bosentan caused by Dasatinib mediated induction of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [14]
Busulfan DMXYJ9C Moderate Increased metabolism of Bosentan caused by Busulfan mediated induction of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [15]
Modafinil DMYILBE Moderate Increased metabolism of Bosentan caused by Modafinil mediated induction of CYP450 enzyme. Narcolepsy [7A20] [93]
Rolapitant DM8XP26 Moderate Increased metabolism of Bosentan caused by Rolapitant mediated induction of CYP450 enzyme. Nausea/vomiting [MD90] [18]
Netupitant DMEKAYI Moderate Increased metabolism of Bosentan caused by Netupitant mediated induction of CYP450 enzyme. Nausea/vomiting [MD90] [15]
Granisetron DMIUW25 Moderate Increased metabolism of Bosentan caused by Granisetron mediated induction of CYP450 enzyme. Nausea/vomiting [MD90] [15]
Ondansetron DMOTQ1I Moderate Increased metabolism of Bosentan caused by Ondansetron mediated induction of CYP450 enzyme. Nausea/vomiting [MD90] [15]
E-2007 DMJDYNQ Moderate Increased metabolism of Bosentan caused by E-2007 mediated induction of CYP450 enzyme. Neuropathy [8C0Z] [18]
Entrectinib DMMPTLH Major Increased metabolism of Bosentan caused by Entrectinib mediated induction of CYP450 enzyme. Non-small cell lung cancer [2C25] [94]
Sibutramine DMFJTDI Moderate Increased metabolism of Bosentan caused by Sibutramine mediated induction of CYP450 enzyme. Obesity [5B80-5B81] [15]
Levomethadyl Acetate DM06HG5 Major Increased metabolism of Bosentan caused by Levomethadyl Acetate mediated induction of CYP450 enzyme. Opioid use disorder [6C43] [95]
Valdecoxib DMAY7H4 Moderate Increased metabolism of Bosentan caused by Valdecoxib mediated induction of CYP450 enzyme. Osteoarthritis [FA00-FA05] [15]
Diclofenac DMPIHLS Moderate Increased metabolism of Bosentan caused by Diclofenac mediated induction of CYP450 enzyme. Osteoarthritis [FA00-FA05] [15]
Naproxen DMZ5RGV Moderate Increased metabolism of Bosentan caused by Naproxen mediated induction of CYP450 enzyme. Osteoarthritis [FA00-FA05] [15]
Olaparib DM8QB1D Major Increased metabolism of Bosentan caused by Olaparib mediated induction of CYP450 enzyme. Ovarian cancer [2C73] [14]
Rucaparib DM9PVX8 Moderate Decreased metabolism of Bosentan caused by Rucaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [15]
Butorphanol DM5KYPJ Major Increased metabolism of Bosentan caused by Butorphanol mediated induction of CYP450 enzyme. Pain [MG30-MG3Z] [20]
Ibuprofen DM8VCBE Moderate Increased metabolism of Bosentan caused by Ibuprofen mediated induction of CYP450 enzyme. Pain [MG30-MG3Z] [15]
Buprenorphine DMPRI8G Moderate Increased metabolism of Bosentan caused by Buprenorphine mediated induction of CYP450 enzyme. Pain [MG30-MG3Z] [96]
Hydrocodone DMQ2JO5 Major Increased metabolism of Bosentan caused by Hydrocodone mediated induction of CYP450 enzyme. Pain [MG30-MG3Z] [20]
Pimavanserin DMR7IVC Moderate Increased metabolism of Bosentan caused by Pimavanserin mediated induction of CYP450 enzyme. Parkinsonism [8A00] [97]
Bromocriptine DMVE3TK Moderate Increased metabolism of Bosentan caused by Bromocriptine mediated induction of CYP450 enzyme. Parkinsonism [8A00] [15]
Abametapir DM2RX0I Moderate Decreased metabolism of Bosentan caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [98]
Macimorelin DMQYJIR Moderate Increased metabolism of Bosentan caused by Macimorelin mediated induction of CYP450 enzyme. Pituitary gland disorder [5A60-5A61] [99]
Lefamulin DME6G97 Major Increased metabolism of Bosentan caused by Lefamulin mediated induction of CYP450 enzyme. Pneumonia [CA40] [100]
Prednisone DM2HG4X Moderate Increased metabolism of Bosentan caused by Prednisone mediated induction of CYP450 enzyme. Postoperative inflammation [1A00-CA43] [15]
Hydrocortisone DMGEMB7 Moderate Increased metabolism of Bosentan caused by Hydrocortisone mediated induction of CYP450 enzyme. Postoperative inflammation [1A00-CA43] [15]
Ergonovine DM0VEC1 Moderate Increased metabolism of Bosentan caused by Ergonovine mediated induction of CYP450 enzyme. Postpartum haemorrhage [JA43] [14]
Lonafarnib DMGM2Z6 Major Increased metabolism of Bosentan caused by Lonafarnib mediated induction of CYP450 enzyme. Premature ageing appearance [LD2B] [101]
Enzalutamide DMGL19D Moderate Increased metabolism of Bosentan caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [102]
Darolutamide DMV7YFT Moderate Increased metabolism of Bosentan caused by Darolutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [103]
Silodosin DMJSBT6 Moderate Increased metabolism of Bosentan caused by Silodosin mediated induction of CYP450 enzyme. Prostate hyperplasia [GA90] [14]
Apremilast DMTWS9E Moderate Increased metabolism of Bosentan caused by Apremilast mediated induction of CYP450 enzyme. Psoriasis [EA90] [104]
Everolimus DM8X2EH Moderate Increased metabolism of Bosentan caused by Everolimus mediated induction of CYP450 enzyme. Renal cell carcinoma [2C90] [14]
Axitinib DMGVH6N Major Increased metabolism of Bosentan caused by Axitinib mediated induction of CYP450 enzyme. Renal cell carcinoma [2C90] [105]
Temsirolimus DMS104F Moderate Increased metabolism of Bosentan caused by Temsirolimus mediated induction of CYP450 enzyme. Renal cell carcinoma [2C90] [14]
Tofacitinib DMBS370 Moderate Increased metabolism of Bosentan caused by Tofacitinib mediated induction of CYP450 enzyme. Rheumatoid arthritis [FA20] [14]
Flurbiprofen DMGN4BY Moderate Increased metabolism of Bosentan caused by Flurbiprofen mediated induction of CYP450 enzyme. Rheumatoid arthritis [FA20] [15]
Dexamethasone DMMWZET Moderate Increased metabolism of Bosentan caused by Dexamethasone mediated induction of CYP450 enzyme. Rheumatoid arthritis [FA20] [15]
Leflunomide DMR8ONJ Major Increased risk of hepatotoxicity by the combination of Bosentan and Leflunomide. Rheumatoid arthritis [FA20] [20]
Quetiapine DM1N62C Moderate Increased metabolism of Bosentan caused by Quetiapine mediated induction of CYP450 enzyme. Schizophrenia [6A20] [14]
Aripiprazole DM3NUMH Moderate Increased metabolism of Bosentan caused by Aripiprazole mediated induction of CYP450 enzyme. Schizophrenia [6A20] [106]
Pimozide DMW83TP Moderate Increased metabolism of Bosentan caused by Pimozide mediated induction of CYP450 enzyme. Schizophrenia [6A20] [15]
Fentanyl DM8WAHT Major Increased metabolism of Bosentan caused by Fentanyl mediated induction of CYP450 enzyme. Sensation disturbance [MB40] [20]
Avanafil DM75CXN Moderate Increased metabolism of Bosentan caused by Avanafil mediated induction of CYP450 enzyme. Sexual dysfunction [HA00-HA01] [107]
Tadalafil DMJZHT1 Moderate Increased metabolism of Bosentan caused by Tadalafil mediated induction of CYP450 enzyme. Sexual dysfunction [HA00-HA01] [18]
Voxelotor DMCS6M5 Major Increased metabolism of Bosentan caused by Voxelotor mediated induction of CYP450 enzyme. Sickle-cell disorder [3A51] [108]
LDE225 DMM9F25 Major Increased metabolism of Bosentan caused by LDE225 mediated induction of CYP450 enzyme. Skin cancer [2C30-2C37] [109]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Bosentan caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [18]
Larotrectinib DM26CQR Moderate Increased metabolism of Bosentan caused by Larotrectinib mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [14]
Methylprednisolone DM4BDON Moderate Increased metabolism of Bosentan caused by Methylprednisolone mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [15]
Vinblastine DM5TVS3 Moderate Increased metabolism of Bosentan caused by Vinblastine mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [15]
Ifosfamide DMCT3I8 Moderate Increased metabolism of Bosentan caused by Ifosfamide mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [15]
Docetaxel DMDI269 Moderate Increased metabolism of Bosentan caused by Docetaxel mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [110]
Trabectedin DMG3Y89 Moderate Increased risk of hepatotoxicity by the combination of Bosentan and Trabectedin. Solid tumour/cancer [2A00-2F9Z] [18]
Armodafinil DMGB035 Moderate Increased metabolism of Bosentan caused by Armodafinil mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [93]
LEE011 DMMX75K Moderate Increased metabolism of Bosentan caused by LEE011 mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [15]
Etoposide DMNH3PG Moderate Increased metabolism of Bosentan caused by Etoposide mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [15]
Prednisolone DMQ8FR2 Moderate Increased metabolism of Bosentan caused by Prednisolone mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [15]
Norethindrone DMTY169 Major Increased metabolism of Bosentan caused by Norethindrone mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [41]
Taxol DMUOT9V Moderate Increased metabolism of Bosentan caused by Taxol mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [111]
Doxorubicin DMVP5YE Moderate Increased metabolism of Bosentan caused by Doxorubicin mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [18]
Ivermectin DMDBX5F Moderate Increased metabolism of Bosentan caused by Ivermectin mediated induction of CYP450 enzyme. Strongyloidiasis [1F6B] [15]
Disulfiram DMCL2OK Moderate Decreased metabolism of Bosentan caused by Disulfiram mediated inhibition of CYP450 enzyme. Substance abuse [6C40] [15]
Naltrexone DMUL45H Moderate Increased risk of hepatotoxicity by the combination of Bosentan and Naltrexone. Substance abuse [6C40] [112]
Warfarin DMJYCVW Moderate Increased metabolism of Bosentan caused by Warfarin mediated induction of CYP450 enzyme. Supraventricular tachyarrhythmia [BC81] [38]
Fostamatinib DM6AUHV Moderate Increased metabolism of Bosentan caused by Fostamatinib mediated induction of CYP450 enzyme. Thrombocytopenia [3B64] [15]
Eltrombopag DMOGFIX Moderate Decreased clearance of Bosentan due to the transporter inhibition by Eltrombopag. Thrombocytopenia [3B64] [113]
Apixaban DM89JLN Moderate Increased metabolism of Bosentan caused by Apixaban mediated induction of CYP450 enzyme. Thrombosis [DB61-GB90] [114]
Brilinta DMBR01X Moderate Increased metabolism of Bosentan caused by Brilinta mediated induction of CYP450 enzyme. Thrombosis [DB61-GB90] [20]
Clopidogrel DMOL54H Moderate Decreased metabolism of Bosentan caused by Clopidogrel mediated inhibition of CYP450 enzyme. Thrombosis [DB61-GB90] [15]
Sirolimus DMGW1ID Moderate Increased metabolism of Bosentan caused by Sirolimus mediated induction of CYP450 enzyme. Transplant rejection [NE84] [14]
Tacrolimus DMZ7XNQ Moderate Increased metabolism of Bosentan caused by Tacrolimus mediated induction of CYP450 enzyme. Transplant rejection [NE84] [14]
Tolbutamide DM02AWV Moderate Increased metabolism of Bosentan caused by Tolbutamide mediated induction of CYP450 enzyme. Type 2 diabetes mellitus [5A11] [15]
Saxagliptin DMGXENV Moderate Increased metabolism of Bosentan caused by Saxagliptin mediated induction of CYP450 enzyme. Type 2 diabetes mellitus [5A11] [115]
Chlorpropamide DMPHZQE Moderate Increased metabolism of Bosentan caused by Chlorpropamide mediated induction of CYP450 enzyme. Type 2 diabetes mellitus [5A11] [15]
Linagliptin DMWFJTR Moderate Increased metabolism of Bosentan caused by Linagliptin mediated induction of CYP450 enzyme. Type 2 diabetes mellitus [5A11] [116]
Elagolix DMB2C0E Moderate Increased metabolism of Bosentan caused by Elagolix mediated induction of CYP450 enzyme. Uterine fibroid [2E86] [117]
Astemizole DM2HN6Q Moderate Increased metabolism of Bosentan caused by Astemizole mediated induction of CYP450 enzyme. Vasomotor/allergic rhinitis [CA08] [15]
Triamcinolone DM98IXF Moderate Increased metabolism of Bosentan caused by Triamcinolone mediated induction of CYP450 enzyme. Vasomotor/allergic rhinitis [CA08] [15]
⏷ Show the Full List of 253 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Acesulfame E00341 36573 Flavoring agent
Aspartame E00402 134601 Flavoring agent
Phenylalanine E00100 6140 Solubilizing agent
Calcium hydrogenphosphate E00294 24441 Diluent
Carmellose sodium E00625 Not Available Disintegrant
Eisenoxyd E00585 56841934 Colorant
Ferric hydroxide oxide yellow E00539 23320441 Colorant
Glyceryl dibehenate E00537 22477175 Binding agent; Coating agent; Flavoring agent; Modified-release agent; Viscosity-controlling agent; lubricant
Magnesium stearate E00208 11177 lubricant
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Tartaric acid E00029 875 Acidulant; Complexing agent; Flavoring agent
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Triacetin E00080 5541 Humectant; Plasticizing agent; Solvent
⏷ Show the Full List of 14 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Bosentan 32 mg tablet 32 mg Tablet for Oral Suspension Oral
Bosentan 125 mg tablet 125 mg Oral Tablet Oral
Bosentan 62.5 mg tablet 62.5 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3494).
2 Bosentan FDA Label
3 BDDCS applied to over 900 drugs
4 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
5 Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
6 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
7 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
8 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. 2007 Aug;35(8):1400-7.
9 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. 2007 Aug;35(8):1400-7.
10 Investigation of the mutual pharmacokinetic interactions between bosentan, a dual endothelin receptor antagonist, and simvastatin. Clin Pharmacokinet. 2003;42(3):293-301.
11 Omics-based responses induced by bosentan in human hepatoma HepaRG cell cultures. Arch Toxicol. 2018 Jun;92(6):1939-1952.
12 From the Cover: MechanisticInsights in Cytotoxic and Cholestatic Potential of the Endothelial Receptor Antagonists Using HepaRG Cells. Toxicol Sci. 2017 Jun 1;157(2):451-464. doi: 10.1093/toxsci/kfx062.
13 Product Information. Adempas (riociguat). Bayer Pharmaceutical Inc, West Haven, CT.
14 Cerner Multum, Inc. "Australian Product Information.".
15 Product Information. Tracleer (bosentan). Acetelion Pharmaceuticals US, Inc, South San Francisco, CA.
16 Bidstrup TB, Bjornsdottir I, Sidelmann UG, Thomsen MS, Hansen KT "CYP2C8 and CYP3A4 are the principal enzymes involved in the human in vitro biotransformation of the insulin secretagogue repaglinide." Br J Clin Pharmacol 56 (2003): 305-14. [PMID: 12919179]
17 Dutreix C, Munarini F, Lorenzo S, Roesel J, Wang Y "Investigation into CYP3A4-mediated drug-drug interactions on midostaurin in healthy volunteers." Cancer Chemother Pharmacol 72 (2013): 1223-34. [PMID: 24085261]
18 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
19 Product Information. Xospata (gilteritinib). Astellas Pharma US, Inc, Deerfield, IL.
20 Canadian Pharmacists Association.
21 Product Information. Multaq (dronedarone). sanofi-aventis , Bridgewater, NJ.
22 Product Information. Ketek (telithromycin). Aventis Pharmaceuticals, Bridgewater, NJ.
23 Product Information. Vraylar (cariprazine). Actavis Pharma, Inc., Parsippany, NJ.
24 Product Information. Balversa (erdafitinib). Janssen Products, LP, Horsham, PA.
25 Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
26 Product Information. Ixempra (ixabepilone). Bristol-Myers Squibb, Princeton, NJ.
27 Product Information. Verzenio (abemaciclib). Lilly, Eli and Company, Indianapolis, IN.
28 Product Information. Aromasin (exemestane) Pharmacia & Upjohn, Kalamazoo, MI.
29 Baciewicz AM "Oral contraceptive drug interactions." Ther Drug Monit 7 (1985): 26-35. [PMID: 2859674]
30 Product Information. Tukysa (tucatinib). Seattle Genetics Inc, Bothell, WA.
31 Product Information. Piqray (alpelisib). Novartis Pharmaceuticals, East Hanover, NJ.
32 Biochem Pharmacol "Variable contribution of cytochromes P450 2D6, 2C9, and 3A4 to the 4-hydroxylation of tamoxifen by human liver microsomes." Biochem Pharmacol 53 (1997): 171-8. [PMID: 9037249]
33 Product Information. Jevtana (cabazitaxel). sanofi-aventis , Bridgewater, NJ.
34 Product Information. Bosulif (bosutinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
35 Bruderer S, Aanismaa P, Homery MC, et al. "Effect of cyclosporine and rifampin on the pharmacokinetics of macitentan, a tissue-targeting dual endothelin receptor antagonist." AAPS J 14 (2012): 68-78. [PMID: 22189899]
36 Product Information. Daurismo (glasdegib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
37 Caraco Y, Sheller J, Wood AJ "Pharmacogenetic determinants of codeine induction by rifampin: the impact on codeine's respiratory, psychomotor and miotic effects." J Pharmacol Exp Ther 281 (1997): 330-6. [PMID: 9103514]
38 Murphey LM, Hood EH "Bosentan and warfarin interaction." Ann Pharmacother 37 (2003): 1028-31. [PMID: 12841813]
39 Crews KR, Stewart CF, Jones-Wallace D, et al "Altered irinotecan pharmacokinetics in pediatric high-grade glioma patients receiving enzyme-inducing anticonvulsant therapy." Clin Cancer Res 8 (2002): 2202-9. [PMID: 12114421]
40 Faculty of Sexual & Reproductive Healthcare "FSRH Clinical Guidance: Drug Interactions with Hormonal Contraception.".
41 Faculty of Sexual & Reproductive Healthcare "FSRH Clinical Guidance: Drug Interactions with Hormonal Contraception.".
42 Product Information. Chirocaine (levobupivacaine) Organon, West Orange, NJ.
43 Gilman AG, Rall TW, Nies AS, Taylor P, eds. "Goodman and Gilman's the Pharmacological Basis of Therapeutics. 8th ed." New York, NY: Pergamon Press Inc. (1990):.
44 Kharasch ED, Thummel KE "Human alfentanil metabolism by cytochrome P450 3A3/4. An explanation for the interindividual variability in alfentanil clearance?" Anesth Analg 76 (1993): 1033-9. [PMID: 8484504]
45 He K, Woolf TF, Hollenberg PF "Mechanism-based inactivation of cytochrome P-450-3A4 by mifepristone (RU486)." J Pharmacol Exp Ther 288 (1999): 791-7. [PMID: 9918590]
46 Product Information. Isturisa (osilodrostat). Recordati Rare Diseases Inc, Lebanon, NJ.
47 Product Information. Xarelto (rivaroxaban). Bayer Inc, Toronto, IA.
48 Product Information. Emend (aprepitant). Merck & Company Inc, West Point, PA.
49 Product Information. Viibryd (vilazodone). Trovis Pharmaceuticals LLC, New Haven, CT.
50 Product Information. Brintellix (vortioxetine). Takeda Pharmaceuticals America, Lincolnshire, IL.
51 Back DJ, Breckenridge AM, Crawford FE, MacIver M, Orne ML, Rowe PH "Interindividual variation and drug interactions with hormonal steroid contraceptives." Drugs 21 (1981): 46-61. [PMID: 7009137]
52 Product Information. Osphena (ospemifene). Shionogi USA Inc, Florham Park, NJ.
53 Bittencourt PR, Gracia CM, Martins R, et al "Phenytoin and carbamazepine decrease oral bioavailability of praziquantel." Neurology 42 (1992): 492-6. [PMID: 1549207]
54 Product Information. Aliqopa (copanlisib). Bayer Pharmaceutical Inc, West Haven, CT.
55 Product Information. Tazverik (tazemetostat). Epizyme, Inc, Cambridge, MA.
56 Product Information. VESIcare (solifenacin). GlaxoSmithKline, Research Triangle Park, NC.
57 Product Information. Myrbetriq (mirabegron). Astellas Pharma US, Inc, Deerfield, IL.
58 Product Information. Incivek (telaprevir). Vertex Pharmaceuticals, Cambridge, MA.
59 Product Information. Priftin (rifapentine). Hoechst Marion-Roussel Inc, Kansas City, MO.
60 Product Information. Pretomanid (pretomanid). The Global Alliance for TB Drug Development, New York, NY.
61 Product Information. Adcetris (brentuximab vedotin). Seattle Genetics Inc, Bothell, WA.
62 Borin MT, Chambers JH, Carel BJ, Gagnon S, Freimuth WW "Pharmacokinetic study of the interaction between rifampin and delavirdine mesylate." Clin Pharmacol Ther 61 (1997): 544-53. [PMID: 9164416]
63 Product Information. Rukobia (fostemsavir). ViiV Healthcare, Research Triangle Park, NC.
64 Product Information. Sustiva (efavirenz). DuPont Pharmaceuticals, Wilmington, DE.
65 Product Information. Tivicay (dolutegravir). ViiV Healthcare, Research Triangle Park, NC.
66 Product Information. Nexletol (bempedoic acid). Esperion Therapeutics, Ann Arbor, MI.
67 Product Information. Kynamro (mipomersen). Genzyme Corporation, Cambridge, MA.
68 Product Information. Juxtapid (lomitapide). Aegerion Pharmaceuticals Inc, Cambridge, MA.
69 Product Information. Zurampic (lesinurad). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
70 Product Information. Belsomra (suvorexant). Merck & Company Inc, Whitehouse Station, NJ.
71 Product Information. Rozerem (ramelteon). Takeda Pharmaceuticals America, Lincolnshire, IL.
72 Product Information. Caplyta (lumateperone). Intra-Cellular Therapies, Inc., New York, NY.
73 Product Information. Movantik (naloxegol). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
74 Cerner Multum, Inc. "Canadian Product Information.".
75 Product Information. Zepzelca (lurbinectedin). Jazz Pharmaceuticals, Palo Alto, CA.
76 Product Information. Lorbrena (lorlatinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
77 Product Information. Tagrisso (osimertinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
78 Product Information. Gavreto (pralsetinib). Blueprint Medicines Corporation, Cambridge, MA.
79 Product Information. Tabrecta (capmatinib). Novartis Pharmaceuticals, East Hanover, NJ.
80 Al-Nawakil C, Willems L, Mauprivez C, et.al "Successful treatment of l-asparaginase-induced severe acute hepatotoxicity using mitochondrial cofactors." Leuk Lymphoma 55 (2014): 1670-4. [PMID: 24090500]
81 Product Information. Zydelig (idelalisib). Gilead Sciences, Foster City, CA.
82 Product Information. Venclexta (venetoclax). AbbVie US LLC, North Chicago, IL.
83 Product Information. Calquence (acalabrutinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
84 Product Information. Clolar (clofarabine). sanofi-aventis, Bridgewater, NJ.
85 Product Information. Zelboraf (vemurafenib). Genentech, South San Francisco, CA.
86 Product Information. Koselugo (selumetinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
87 Product Information. Braftovi (encorafenib). Array BioPharma Inc., Boulder, CO.
88 Product Information. Ubrelvy (ubrogepant). Allergan Inc, Irvine, CA.
89 Product Information. Nurtec ODT (rimegepant). Biohaven Pharmaceuticals, New Haven, CT.
90 Product Information. Exjade (deferasirox). Novartis Pharmaceuticals, East Hanover, NJ.
91 Product Information. Addyi (flibanserin). Sprout Pharmaceuticals, Raleigh, NC.
92 Product Information. Jakafi (ruxolitinib). Incyte Corporation, Wilmington, DE.
93 Product Information. Nuvigil (armodafinil). Cephalon Inc, West Chester, PA.
94 Product Information. Rozlytrek (entrectinib). Genentech, South San Francisco, CA.
95 Patel S, Robinson R, Burk M "Hypertensive crisis associated with St. John's Wort." Am J Med 112 (2002): 507-8. [PMID: 11959071]
96 Product Information. Buprenex (buprenorphine). Reckitt and Colman Pharmaceutical, Richmond, VA.
97 Product Information. Nuplazid (pimavanserin). Accelis Pharma, East Windsor, NJ.
98 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
99 Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC.
100 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
101 Product Information. Zokinvy (lonafarnib). Eiger BioPharmaceuticals, Palo Alto, CA.
102 Product Information. Xtandi (enzalutamide). Astellas Pharma US, Inc, Deerfield, IL.
103 Product Information. Nubeqa (darolutamide). Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ.
104 Product Information. Otezla (apremilast). Celgene Corporation, Summit, NJ.
105 Pithavala YK, Tortorici M, Toh M, et al "Effect of rifampin on the pharmacokinetics of axitinib (AG-013736) in Japanese and Caucasian healthy volunteers." Cancer Chemother Pharmacol 65 (2010): 563-70. [PMID: 19603168]
106 Product Information. Abilify (aripiprazole). Bristol-Myers Squibb, Princeton, NJ.
107 Product Information. Stendra (avanafil). Vivus Inc, Mountain View, CA.
108 Product Information. Oxbryta (voxelotor). Global Blood Therapeutics, Inc., South San Francisco, CA.
109 Product Information. Odomzo (sonidegib). Novartis Pharmaceuticals, East Hanover, NJ.
110 Aronson JK, Grahame-Smith DG "Clinical pharmacology: adverse drug interactions." Br Med J 282 (1981): 288-91. [PMID: 6779990]
111 Jamis-Dow CA, Klecker RW, Katki AG, Collins JM "Metabolism of Taxol by human liver microsomes and effect of inhibitors (Meeting abstract)." Proc Annu Meet Am Assoc Cancer Res 34 (1993): a21981993.
112 Product Information. ReVia (naltrexone). DuPont Pharmaceuticals, Wilmington, DE.
113 Allred AJ, Bowen CJ, Park JW, et al. "Eltrombopag increases plasma rosuvastatin exposure in healthy volunteers." Br J Clin Pharmacol 72 (2011): 321-9. [PMID: 21434975]
114 Product Information. Eliquis (apixaban). Bristol-Myers Squibb Canada Inc, Montreal, IN.
115 Product Information. Onglyza (saxagliptin). Bristol-Myers Squibb, Princeton, NJ.
116 Product Information. Tradjenta (linagliptin). Boehringer Ingelheim, Ridgefield, CT.
117 Product Information. Orilissa (elagolix). AbbVie US LLC, North Chicago, IL.