ArticleClinical pharmacology and therapeutics2013
Association of CYP2C9*2 with bosentan-induced liver injury.
Article in Clinical pharmacology and therapeutics, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers, 1 of them a synthesis that pooled it.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
24 citing papers in PubMed, 1 synthesis or guideline pooled it, 52 citations in OpenAlex.
- Efficacy and safety of switching from bosentan or ambrisentan to macitentan in pulmonary arterial hypertension: A systematic review and meta-analysis.Frontiers in cardiovascular medicine · 2022Pooled it
- Phase I study of PF‐04895162, a Kv7 channel opener, reveals unexpected hepatotoxicity in healthy subjects, but not rats or monkeys: clinical evidence of disrupted bile acid homeostasis.Pharmacology research & perspectives · 2019Trial
- Mechanistically resolved prediction of compound hepatotoxicity using primary human liver spheroids-Application to recent real-world cases.Drug metabolism and disposition: the biological fate of chemicals · 2026Article
- A newFrontiers in toxicology · 2026Article
- Pharmacogenetics in pediatric cardiology.Frontiers in pediatrics · 2026Article
- Predicting Systemic and Liver Bosentan Exposure Using Physiologically-Based Pharmacokinetic Modeling.CPT: pharmacometrics & systems pharmacology · 2025Article
- Drug-Induced Autoimmune Hepatitis by Varenicline and Infliximab as a Continuous Disease Spectrum with Two Different Flares: Acute Liver Injury Followed by Hepatic Autoimmunity.International journal of molecular sciences · 2025Review
- Drug metabolizing enzymes and transporters, and their roles for the development of drug-induced liver injury.Expert opinion on drug metabolism & toxicology · 2025Review
- Pharmacogenomics in the Management of Pulmonary Arterial Hypertension: Current Perspectives.Pharmacogenomics and personalized medicine · 2023Review
- Pharmacological counseling in hepatotoxicity induced by macitentan and selexipag: a case report.Journal of medical case reports · 2022Article
- Review
- High-Fidelity Drug-Induced Liver Injury Screen Using Human Pluripotent Stem Cell-Derived Organoids.Gastroenterology · 2021Article
- The Transition From Ambrisentan to Macitentan in Patients With Pulmonary Arterial Hypertension: A Real-word Prospective Study.Frontiers in pharmacology · 2021Article
- Human Three-Dimensional Hepatic Models: Cell Type Variety and Corresponding Applications.Frontiers in bioengineering and biotechnology · 2021Review
- Worldwide Use of RUCAM for Causality Assessment in 81,856 Idiosyncratic DILI and 14,029 HILI Cases Published 1993-Mid 2020: A Comprehensive Analysis.Medicines (Basel, Switzerland) · 2020Review
- A network meta-analysis for safety of endothelin receptor antagonists in pulmonary arterial hypertension.Cardiovascular diagnosis and therapy · 2019Article
- Biomarkers of drug-induced liver injury.Advances in pharmacology (San Diego, Calif.) · 2019Review
- Biomarkers of drug-induced liver injury: progress and utility in research, medicine, and regulation.Expert review of molecular diagnostics · 2018Review
- Pharmacogenomics of CYP2C9: Functional and Clinical Considerations.Journal of personalized medicine · 2017Review
- Drug-induced liver injury: Do we know everything?World journal of hepatology · 2017Review
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Authors and funding
17 authors at 2 institutions in 1 country.
Funding
Abstract
Bosentan (Tracleer) is an endothelin receptor antagonist prescribed for the treatment of pulmonary arterial hypertension (PAH). Its use is limited by drug-induced liver injury (DILI). To identify genetic markers of DILI, association analyses were performed on 56 Caucasian PAH patients receiving bosentan. Twelve functional polymorphisms in five genes (ABCB11, ABCC2, CYP2C9, SLCO1B1, and SLCO1B3) implicated in bosentan pharmacokinetics were tested for associations with alanine aminotransferase (ALT), aspartate aminotransferase (AST), and DILI. After adjusting for body mass index, CYP2C9*2 was the only polymorphism associated with ALT, AST, and DILI (β = 2.16, P = 0.024; β = 1.92, P = 0.016; odds ratio 95% CI = 2.29-∞, P = 0.003, respectively). Bosentan metabolism by CYP2C9*2 in vitro was significantly reduced compared with CYP2C9*1 and was comparable to that by CYP2C9*3. These results suggest that CYP2C9*2 is a potential genetic marker for prediction of bosentan-induced liver injury and warrants investigation for the optimization of bosentan treatment.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.