Bosentan 125mg tablets
Requires a prescription from a doctor or prescriber
Bosentan is a dual endothelin receptor antagonist marketed under the trade name Tracleer by Actelion Pharmaceuticals.
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Official medicine documents
Safety monitoring data
Yellow Card reports
The MHRA Yellow Card scheme collects reports of suspected side effects from healthcare professionals and patients. View the Drug Analysis Profile (iDAP) for real-world adverse reaction data.
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Suspected adverse reactions reported for Bosentan
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Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
EudraVigilance
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Suspected adverse reactions reported for Bosentan
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EudraVigilance data is published by the European Medicines Agency (EMA). A suspected adverse reaction is not necessarily caused by the medicine.
8 branded products available
MHRA licensed products
View all licensed products for Bosentan on the MHRA register
Bosentan 125mg tablets
Bosentan 125mg tablets
Bosentan 125mg tablets
Bosentan 125mg tablets
WHO defined daily dose (DDD)
250 mg
Not a recommended dose. The DDD is the assumed average maintenance dose per day for a drug used for its main indication in adults. It is a statistical measure used for research and comparison purposes only.
Source: WHO Collaborating Centre for Drug Statistics Methodology, distributed via the NHS dm+d supplementary BNF/ATC mapping files (NHSBSA). Contains public sector information licensed under the Open Government Licence v3.0.
Therapeutically similar medicines
Similarity is based on WHO Anatomical Therapeutic Chemical (ATC) classification and on a factual NHS dm+d therapeutic-grouping code prefix. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
NHS prescribing volume and spending trends
Guidelines from the National Institute for Health and Care Excellence
NICE clinical guidance(2)
Digital ulcers: sildenafil (ESUOM42)
Idiopathic pulmonary fibrosis in adults: diagnosis and management (CG163)
Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
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Codes for healthcare professionals and prescribing systems
These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
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SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF code shown is the factual mapping value distributed by NHS Business Services Authority (NHSBSA) in the dm+d supplementary file under OGL v3.0; it is not affiliated with, nor licensed from, the publishers of the British National Formulary. ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Academic studies and reviews for this medicine's active substance
Showing all 27 studies.
Reviews & meta-analyses: 7 · Randomised trials: 1 · 2016–2026
Showing all 27 studies, sorted by most relevant.
Noha Rami Ismail, Hamdy A. Makhlouf, Atef Hassan, et al.
American Heart Journal Plus, 2024
Chronic thromboembolic pulmonary hypertension (CTEPH) is a major risk for pulmonary hypertension with poor prognosis. Limited data is available on the optimal treatment of choice. We aimed to comprehensively assess the efficacy and safety of CTEPH targeted therapies and update the evidence. We searched PubMed, Scopus, and the Cochrane library up to December 2023 to include randomized controlled trials comparing different therapies in patients with CTEPH. Primary outcomes were 6-minute walk distance (6 MWD), pulmonary vascular resistance (PVR), and mean pulmonary artery pressure (mPAP). While secondary outcomes were the mean right atrial pressure (mRAP), Borg dyspnea score, cardiac output (CO), cardiac index, adverse events, and all-cause mortality. Fourteen RCTs comprising 1047 patients were included in this network meta-analysis. Regarding 6 MWD, PADN (MD=113.59, 95% CI: 53.80; 173.39), BPA (MD=48.84, 95% CI: 27.99; 69.69), riociguat (MD=42.59, 95% CI: 22.01; 63.18), treprostinil (MD=41.60, 95% CI: 17.07; 66.13), and macitentan (MD=34.00, 95% CI: 3.50; 64.50) were favored compared to placebo. In terms of PVR, BPA (MD=-392.19, 95% CI: -571.77; -212.62), treprostinil (MD=-287.20, 95% CI: -475.63; -98.77), PADN (MD=-280.61, 95% CI: -506.69; -54.52), bosentan (MD=-176.00, 95% CI: -340.91; -11.09), and riociguat (MD=-171.61, 95% CI: -298.40; -44.81) displayed statistically significant results. Current therapeutic modalities are effective in terms of improving exercise capacity, pulmonary hemodynamics, and reducing adverse events and all-cause mortality. Overall, BPA and PADN were superior to all other targeted medications in the studied outcomes. • The optimal treatment modality for CTEPH is still controversial, with conflicting data in the literature. • Our meta-analysis of 14 RCTs showed that BPA and PADN were superior to all other treatment modalities to reduce the odds of mortality. • SUCRA values and treatment ranking list confirm the current findings. • This study can be a guide of recommending BPA and PADN as the approaches of choice in treating CTEPH. • These findings should be validated with large-volume RCTs with long-term outcomes.
Abstract licence: CC BY-NC-ND
R. Steinhorn, J. Fineman, Andjela Kusic-Pajic, et al.
The Journal of pediatrics, 2016
- Bosentan
- Nitric Oxide
- Persistent Fetal Circulation Syndrome
Qinhua Zhao, N. Guo, Jun Chen, et al.
Journal of Clinical Pharmacy and Therapeutics, 2021
- Walk Test
- Network Meta-Analysis
- Bosentan
Hongyu Kuang, Yu-hao Wu, Qijian Yi, et al.
Medicine, 2018
- Bosentan
- Heart Defects, Congenital
- Sulfonamides
BACKGROUND: Oral bosentan has been widely applied in pulmonary arterial hypertension associated with congenital heart disease (PAH-CHD). A systemic review and meta-analysis was conducted for a therapeutic evaluation of oral bosentan in both adult and pediatric patients with PAH-CHD. The acute responses and a long-term effect were respectively assessed in a comparison with baseline characteristics, and the improvement of exercise tolerance was analyzed. METHODS: PubMed, Medline, Embase, and Cochrane Central Register of clinical controlled trails or observational studies have been searched for a recording of bosentan effects on the PAH-CHD participants. For mortality and rate of adverse events (AEs), it was described in detail. Randomized-effects model or fixed-effects model was used to calculate different effective values with a sensitivity analysis. RESULTS: Seventeen studies were pooled in this review, and 3 studies enrolled the pediatric patients. Among all studies, 456 patients were diagnosed with PAH-CHD, and 91.7% were treated with oral bosentan. With a term less than 6 months of bosentan therapy, there existed a significant improvement in 6-minute walk distance (6MWD) and the World Health Organization functional class (WHO-FC), but no such differences in Borg dyspnea index scores (BDIs) and the resting oxygen saturation (SpO2). Although with a prolonged treatment, not only 6MWD and FC, but also the resting SpO2 and heart rate were changed for a better exercise capability. Additionally, compared with the basic cardiopulmonary hemodynamics, it showed a statistically significant difference in mean pulmonary arterial pressure (mPAP) and pulmonary vascular resistance index (PVRi). Although a limitation of pooled studies with comparative outcomes of different terms, outcomes presented a lower WHO-FC which contributes to a success in a prolonged treatment. CONCLUSIONS: Bosentan in PAH-CHD is well established and still requires clinical trials for an identification of its efficiency on CHD patients for an optimized period lessening a serious complication and the common AEs.
Abstract licence: CC BY-ND
M. Packer, J. McMurray, H. Krum, et al.
JACC. Heart failure, 2017
- Cause of Death
- Bosentan
- Australia
O. Araz
The Eurasian journal of medicine, 2020
Acute respiratory distress syndrome is characterized by dyspnea at presentation, tachypnea on physical examination, findings of bilateral infiltration in chest radiography, refractory hypoxia, and high mortality. Although the main treatment approach is to address the underlying disease, there are also pharmacological and nonpharmacological options for supportive treatment. There is currently no pharmacological agent with proven efficacy in this syndrome, and many drugs are being studied for this purpose. One of these is the endothelin receptor antagonist bosentan. Cite this article as: Araz O. Current Pharmacological Approach to ARDS: The Place of Bosentan. Eurasian J Med 2020; 52(1): 81-85.
Abstract licence: CC BY
Xinwang Chen, Z. Zhai, Ke Huang, et al.
The Clinical Respiratory Journal, 2018
- Bosentan
- Antihypertensive Agents
- Chronic Disease
Yuchen Wang, Selena Y. Chen, Junbao Du
Frontiers in Pediatrics, 2019
Idiopathic pulmonary arterial hypertension (IPAH) is a complex disease associated with progressive deterioration. Targeted therapy for IPAH has improved in the last several decades. However, there remain many challenges to current treatment of children with IPAH, including poor prognosis and a median survival of 0.8 years. Endothelin-1 (ET-1) appears to be a key mediator in the pathogenesis of IPAH, with elevated concentrations in the plasma. Bosentan, an endothelin receptor antagonist, has been confirmed in Food and Drug Administration (FDA) to effectively treat IPAH when administered in recent studies. This review focuses on related studies and advance of bosentan in the treatment of IPAH in children.
Abstract licence: CC BY
W. Shihoya, T. Nishizawa, K. Yamashita, et al.
Nature Structural &Molecular Biology, 2017
- Bosentan
- Models, Molecular
- Protein Binding
A. Trombetta, C. Pizzorni, B. Ruaro, et al.
The Journal of Rheumatology, 2016
- Bosentan
- Antihypertensive Agents
- Capillaries
Sources: aggregated from Europe PMC (EMBL-EBI), OpenAlex, Crossref, PubMed and other open scholarly databases. Retracted articles are excluded. Study information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
5 found
Half-life
5 hours
Mechanism
Endothelin-1 (ET-1) is a neurohormone, the effects of which are mediated by bind…
Food interactions
1 warning
Human targets
2 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
50%
Half-life
5 hours
Protein binding
98%
Volume of distribution
18 L
Metabolism
10 to 20%
Elimination
Clearance
4 L/h
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Known interactions with other medications. Always consult a healthcare professional.
Showing 50 of 1262 interactions
Mild decreases in blood pressure and increases in heart rate were observed. There is no specific experience of overdosage with bosentan beyond the doses described above. Massive overdosage may result in pronounced hypotension requiring active cardiovascular support.
How the body processes this drug — absorption, distribution, metabolism, and elimination
Proteins and enzymes this drug interacts with in the body
Enzymes involved in drug metabolism — important for understanding drug interactions
Proteins that transport this drug across cell membranes
PMID:15791618 PMID:16332456 PMID:18985798 PMID:19228692 PMID:20010382 PMID:20398791 PMID:22262466 PMID:24711118 PMID:29507376 PMID:32203132
Transports taurine-conjugated bile salts more rapidly than glycine-conjugated bile salts .
PMID:16332456
Also transports non-bile acid compounds, such as pravastatin and fexofenadine in an ATP-dependent manner and may be involved in their biliary excretion PMID:15901796 PMID:18245269
ATC G01AE10
ATC C02KX01
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
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Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Bosentan
Additional database identifiers
Drugs Product Database (DPD)
12538
ChemSpider
94651
BindingDB
50061101
PDB
K86
ZINC
ZINC000001538857
HUGO Gene Nomenclature Committee (HGNC)
HGNC:3180
GenAtlas
EDNRB
GeneCards
EDNRB
GenBank Gene Database
M74921
GenBank Protein Database
182276
Guide to Pharmacology
220
UniProt Accession
EDNRB_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:3179
GenAtlas
EDNRA
GeneCards
EDNRA
GenBank Gene Database
S63938
GenBank Protein Database
238636
Guide to Pharmacology
219
UniProt Accession
EDNRA_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2637
GenAtlas
CYP3A4
GeneCards
CYP3A4
GenBank Gene Database
M18907
Guide to Pharmacology
1337
UniProt Accession
CP3A4_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2623
GenAtlas
CYP2C9
GeneCards
CYP2C9
GenBank Gene Database
AY341248
Guide to Pharmacology
1326
UniProt Accession
CP2C9_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:42
GenAtlas
ABCB11
GeneCards
ABCB11
GenBank Gene Database
AF091582
GenBank Protein Database
3873243
Guide to Pharmacology
778
UniProt Accession
ABCBB_HUMAN
DrugBank citations
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Structured knowledge from the free knowledge base
ATC classifications (Wikidata)
Linked open data from Wikidata (Q27114267), a free and open knowledge base operated by the Wikimedia Foundation. Data is available under the Creative Commons CC0 1.0 Public Domain Dedication.