bosentan / Generic mfg. - LARVOL DELTA

A Clinical Trial to Evaluate MK-4208/TERN-701 in Healthy Adult Participants (MK-4208-001/TERN701-1014) (clinicaltrials.gov) - P1 | N=196 | Completed | Sponsor: Terns, Inc., a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)

New P1 trial

Eisenmenger Syndrome After Delayed Atrial Septal Defect Closure at High Altitude: A Case Report. (PubMed, Am J Case Rep) - "Multidisciplinary management included bosentan 125 mg twice daily, tadalafil 10 mg once daily, nocturnal oxygen, diuretics, and anticoagulation, resulting in symptomatic stabilization and discharge on day 4. CONCLUSIONS Delayed atrial septal defect repair at high altitude can lead to irreversible Eisenmenger syndrome, for which current therapy is palliative. Early defect recognition and closure, congenital heart screening, and access to pulmonary vasodilators and transplant programs are imperative in resource-constrained mountainous regions."

Journal • Cardiovascular • Congestive Heart Failure • Heart Failure • Hematological Disorders • Hypertension • Palliative care • Pulmonary Arterial Hypertension • Pulmonary Disease • Respiratory Diseases • Transplantation

A Study in Healthy Men to Test How Bosentan Influences the Amount of Zongertinib in the Blood (clinicaltrials.gov) - P1 | N=16 | Completed | Sponsor: Boehringer Ingelheim | Active, not recruiting ➔ Completed

Trial completion

Impact of CYP3A inducers on nerandomilast pharmacokinetics (ERS 2026) - "Two open-label, two-treatment, two-period, fixed-sequence crossover trials were conducted to evaluate the effect of strong (carbamazepine) and moderate (bosentan) CYP3A inducers on nerandomilast PK in healthy male subjects (n=16 per study). Strong and moderate CYP3A inducers reduced nerandomilast exposure, decreasing AUC by 51% and 41% and Cmax by 31% and 15%, respectively."

PK/PD data • Idiopathic Pulmonary Fibrosis • Immunology • Interstitial Lung Disease • Pulmonary Disease • Respiratory Diseases

Assessing drug-induced liver injury liabilities in human and animal hepatocytes under static and perfused spheroid culture conditions. (PubMed, Toxicol Sci) - "Cells were exposed to species-specific DILI compounds chlorpromazine (CPZ), bosentan (BOS), and fialuridine (FIAU). The microfluidics-based MPS exhibited modestly improved hepatocyte spheroid function relative to static models, although limited MPS throughput constrained our ability for testing drugs beyond FIAU. Overall, these results demonstrate that integrating multi-species hepatocyte spheroids across static and microfluidic platforms enables comparative DILI assessment and supports improved preclinical-to-clinical translation."

Journal • Hepatology • Liver Failure

Targeting Novel Pathways in Pulmonary Arterial Hypertension: A Systematic Review and Meta-Analysis of New Therapeutic Agents. (PubMed, Niger Med J) - "Udenafil and fasudil showed modest benefits, while anastrozole had mixed results with possible sex-specific effects. At the individual trial level, sotatercept (0.7 mg/kg), riociguat (2.5 mg), and metformin (500 mg with bosentan) showed the most favourable benefit profiles. Standardised trial designs and consistent outcome reporting are needed to confirm these potential disease-modifying effects."

Journal • Retrospective data • Cardiovascular • Heart Failure • Hypertension • Pulmonary Arterial Hypertension • Pulmonary Disease • Respiratory Diseases

Long-term management of a child with aortopulmonary septal defect and Eisenmenger syndrome: a 6-year follow-up case study. (PubMed, Folia Med (Plovdiv)) - "Despite the administration of medical therapy with sildenafil, bosentan, and antiplatelets, the patient's condition remained unfavorable due to fixed pulmonary vascular obstructive disease. This case underscores the importance of early diagnosis and the complexities of managing advanced pulmonary hypertension in congenital heart defects."

Journal • Cardiovascular • Hypertension • Pulmonary Arterial Hypertension • Pulmonary Disease • Respiratory Diseases

Endothelin‑1 clearance by endothelin‑B receptor–expressing LYVE1⁺ macrophages limits cardiometabolic disease progression (ESC 2026) - "Substantiating the proatherogenic potential of ET-1, dual ETA/ETB receptor blockade with bosentan reduced lesion burden...(B). Weight difference of mice over the course of 18 weeks, p<0,05."

Atherosclerosis • Cardiovascular • EDN1 • EDNRB • LYVE1

POPS or POP02: Pharmacokinetics, Pharmacodynamics, and Safety Profile of Understudied Drugs Administered to Children Per Standard of Care (POPS) (clinicaltrials.gov) - P=N/A | N=5000 | Recruiting | Sponsor: Duke University | Trial completion date: Jul 2027 ➔ Dec 2026 | Trial primary completion date: Mar 2027 ➔ Nov 2026

Trial completion date • Trial primary completion date • ADHD (Impulsive Aggression) • Asthma • Attention Deficit Hyperactivity Disorder • Bronchopulmonary Dysplasia • Cardiovascular • CNS Disorders • Dermatology • Developmental Disorders • Endocrine Disorders • Genetic Disorders • Gynecology • Heart Failure • Hematological Disorders • Hemophilia • Hypertension • Immunology • Infectious Disease • Insomnia • Metabolic Disorders • Nephrology • Novel Coronavirus Disease • Pain • Pneumonia • Psychiatry • Pulmonary Arterial Hypertension • Pulmonary Disease • Rare Diseases • Renal Disease • Respiratory Diseases • Sleep Disorder

Outcomes of VSD closure in children > 2 years with severe PAH – interim analysis (ESC 2026) - "Thirty-seven children (mean age 6.5±3.7 years, range 2–18) deemed operable underwent surgical VSD closure and received dual pulmonary vasodilator therapy (sildenafil and bosentan) for 1 year. Near normalization of mPAP at 1 year in the majority is encouraging. A longer follow-up is needed to confirm sustained benefits."

Clinical • Cardiovascular • Congestive Heart Failure • Heart Failure

A Multimodal Right Ventricular Protective Strategy for Urgent Liver Retransplantation in Severe Portopulmonary Hypertension (ASA 2026) - "Despite an mPAP rebound to 48 mmHg, surgery proceeded using an aggressive RV-protective strategy including triple vasodilator therapy (sildenafil, bosentan, inhaled iloprost), PAC, and TEE (transesophageal Echochardiogram). mPAP was reduced to 30 mmHg pre-reperfusion, ensuring hemodynamic stability. Multimodal optimization and a "reperfusion-readiness" mindset enable successful urgent retransplantation in severe POPH, challenging traditional contraindications through dynamic monitoring and RV protection."

Cardiovascular • Hematological Disorders • Pulmonary Arterial Hypertension • Pulmonary Disease • Respiratory Diseases • Thrombosis • Transplantation

Improvement of Refractory Cutaneous Ulcers and Pulmonary Arterial Hypertension Following Rituximab and Mycophenolate Mofetil Therapy in Anti-melanoma Differentiation-Associated Gene 5 (Anti-MDA5) Antibody-Positive Dermatomyositis. (PubMed, Cureus) - "Despite the escalation of immunosuppressive therapy with glucocorticoids, tacrolimus, intravenous immunoglobulin, and cyclophosphamide, the cutaneous ulcers remained refractory. Bosentan was discontinued, and azathioprine was initiated to maintain remission, allowing for a successful pregnancy and delivery of a healthy infant. This case suggests a potential role for an MMF- and RTX-containing combination regimen in refractory cutaneous ulcers and PAH associated with anti-MDA5 DM."

Journal • Cardiovascular • Dermatomyositis • Hypertension • Immunology • Melanoma • Myositis • Oncology • Pulmonary Arterial Hypertension • Pulmonary Disease • Respiratory Diseases • Rheumatology • Solid Tumor • IFIH1

A targeted lipidomics workflow for high-throughput phenotyping and mechanism-based in vitro hepatotoxicity studies. (PubMed, Toxicol In Vitro) - "We used primary hepatocytes from human, rat, monkey, and dog cultured in 96-well plates and exposed to chlorpromazine (1-30 μM), bosentan (1-200 μM), and fialuridine (1-100 μM) from culture day 4 to 8. The targeted lipidomics workflow provided mechanism-informed phenotyping of chemical-induced lipid responses in cultured hepatocytes. Moreover, it provided a framework for mechanistic evaluation, supported cross-species comparison, and complemented in vitro hepatotoxicity assessments."

Journal • Preclinical • Hepatology • Liver Failure

Comparative clinical evaluation of endothelin receptor antagonists in pulmonary arterial hypertension using a multi-criteria decision analysis framework. (PubMed, Int J Clin Pharm) - "Within the proposed MCDA framework, ambrisentan achieved the highest overall score across multiple clinical and practical dimensions. The framework provides a transparent tool for structured evaluation, although economic and accessibility findings should be interpreted within the Chinese healthcare context."

Journal • Cardiovascular • Hypertension • Pulmonary Arterial Hypertension • Pulmonary Disease • Respiratory Diseases

Next-generation therapeutics and renaissance of legacy drugs targeting the endothelin system. (PubMed, Can J Physiol Pharmacol) - "Endothelin-1 (ET-1) was discovered in 1988, followed by identification of ETA and ETB receptors in 1990, enabling rapid development of the first endothelin receptor antagonists (bosentan, ambrisentan, and macitentan) for pulmonary arterial hypertension, a condition marked by elevated ET-1. Nearly a decade later, a new therapeutic wave began with the ETB agonist sovateltide (2021) for cerebral ischemic stroke, demonstrating the benefits of ETB activation...Clazosentan (ETA) for cerebral vasospasm and aprocitentan (ETA/ETB) for resistant hypertension extended endothelin-targeted therapy into more common diseases. In kidney disease, sparsentan (AT1/ETA) and atrasentan (ETA) have both been approved for IgA nephropathy, with atrasentan succeeding after earlier failed trials...This review outlines approaches for identifying legacy endothelin compounds suitable for new indications, using zibotentan, now combined with dapagliflozin to reduce fluid retention as an example. Kidney..."

Journal • Review • Cardiovascular • Glomerulonephritis • Hypertension • IgA Nephropathy • Ischemic stroke • Nephrology • Pulmonary Arterial Hypertension • Pulmonary Disease • Renal Disease • Respiratory Diseases • EDN1

A Study in Healthy Men to Test How Bosentan Influences the Amount of Zongertinib in the Blood (clinicaltrials.gov) - P1 | N=16 | Active, not recruiting | Sponsor: Boehringer Ingelheim | Recruiting ➔ Active, not recruiting

Enrollment closed

L-carnosine as a biocompatible dipeptide carrier for oral delivery of amorphous bosentan: the ternary systems loaded with a new grade of poly(acrylic acid), hypromellose or copovidone. (PubMed, Int J Pharm) - No abstract available

Journal

Mechanistically resolved prediction of compound hepatotoxicity using primary human liver spheroids-Application to recent real-world cases. (PubMed, Drug Metab Dispos) - "Cholestatic liability was identified using bile acid coexposure with accurate classification of chlorpromazine and bosentan and confirmation of bile salt export pump downregulation. Importantly, the model also recapitulated hepatotoxicity signals observed in recent clinical development, including for Bruton's tyrosine kinase inhibitors (tolebrutinib and evobrutinib), oral glucagon-like peptide-1 receptor agonists (danuglipron vs orforglipron), synergistic toxicity on azelaprag-tirzepatide coexposure and enhanced sensitivity to the IL-17A inhibitor LY3509754 on coculture with nonparenchymal liver cells...The model maintains stable CYP expression and metabolic activity, captures the impact of nonparenchymal cells on hepatic clearance, and detects mitochondrial, cholestatic, and interaction-driven toxicity, including recent real-world clinical cases. These findings support 3-dimensional human liver spheroids as translational new approach methodologies for integrating..."

Journal • Real-world evidence • Hepatology • Liver Failure • Metabolic Disorders • IL17A

A Study in Healthy Men to Test How Bosentan Influences the Amount of Zongertinib in the Blood (clinicaltrials.gov) - P1 | N=16 | Recruiting | Sponsor: Boehringer Ingelheim | Not yet recruiting ➔ Recruiting

Enrollment open

The interplay of bosentan and finerenone in amelioration of cardiac dysfunction within benign prostatic hyperplasia in rats. (PubMed, Mol Biol Rep) - "BOS and/or FIN showed a significant ameliorative effect in BPH."

Journal • Preclinical • Benign Prostatic Hyperplasia • CASP3 • PCNA

Development of a population pharmacokinetic model using combined paediatric and adult data for four pulmonary arterial hypertension drugs. (PubMed, Br J Clin Pharmacol) - "This study clarified the pharmacokinetic parameters and their variability for sildenafil, tadalafil, bosentan and ambrisentan using combined data from Japanese paediatric and adult patients with PAH. The results of Bayesian estimation suggest that at current clinical dosages, plasma concentrations of these drugs may be lower in paediatric than adult patients."

Journal • PK/PD data • Cardiovascular • Hypertension • Pediatrics • Pulmonary Arterial Hypertension • Pulmonary Disease • Respiratory Diseases

ACTION: The Impact of ERA Switching on Risk Stratification in Pulmonary Arterial Hypertension (clinicaltrials.gov) - P=N/A | N=183 | Recruiting | Sponsor: University of Sao Paulo General Hospital | N=121 ➔ 183

Enrollment change • Cardiovascular • Congestive Heart Failure • Hypertension • Pulmonary Arterial Hypertension • Pulmonary Disease • Respiratory Diseases

Combined mechanical and chemical sympathectomy for refractory complicated Raynaud's phenomenon: an international multicenter case-based review. (PubMed, Rheumatol Int) - "This patient suffered a relapse with three new distal ulcers immediately following an administrative gap in Bosentan therapy. These hypothesis-generating findings suggest that multimodal sympathectomy is a feasible adjunctive strategy for limb salvage in refractory complicated secondary RP. Current literature enforces these findings supporting the notion for standardized dosing and stepwise approach for future research to support these hypothesis generating views."

Journal • Retrospective data • Review • Cardiovascular • Hematological Disorders • Immunology • Pain • Rheumatology • Scleroderma • Systemic Sclerosis • Thrombosis

Efficacy and safety of bosentan-related therapy in neonates with persistent pulmonary hypertension of the newborn: a systematic review and meta-analysis. (PubMed, Front Pediatr) - "https://www.crd.york.ac.uk/prospero/display_record.php?ID=CRD420261338730. PROSPERO: CRD420261338730."

Journal • Retrospective data • Review • Cardiovascular • Hematological Disorders • Hypertension • Hypotension • Pulmonary Arterial Hypertension • Pulmonary Disease • Respiratory Diseases

Study of the Benefit of Early Treatment With an Endothelin Inhibitor (Bosentan) in Patients With Sudden Blindness Due to Giant Cell Arteritis: CECIBO (clinicaltrials.gov) - P3 | N=8 | Completed | Sponsor: Centre Hospitalier Universitaire de Nice | Unknown status ➔ Completed

Trial completion • Giant Cell Arteritis • Immunology • Ophthalmology