TRACLEER (bosentan)
TRACLEER is indicated for the treatment of Pulmonary Arterial Hypertension; Congenital Heart Disease.
How TRACLEER Works
Bosentan is a specific and competitive antagonist of endothelin-1 (ET-1) at both $ET_A$ and $ET_B$ receptor types, located in the endothelium and vascular smooth muscle. ET-1 is a neurohormone that is typically elevated in the plasma and lung tissue of patients with PAH, contributing to the disease's pathogenesis. By preventing ET-1 from binding to its receptors, bosentan reduces pulmonary vascular resistance and improves exercise capacity.
Development Insights
Details
- Status
- Prescription
- First Approved
- 2001-11-20
- Patent Cliff
- 2027
- Routes
- ORAL
- Dosage Forms
- TABLET, FOR SUSPENSION, TABLET
TRACLEER Approval History
What TRACLEER Treats
2 indicationsTRACLEER is approved for 2 conditions since its original approval in 2001. These indications span multiple therapeutic areas including oncology, immunology, and more.
- Pulmonary Arterial Hypertension
- Congenital Heart Disease
TRACLEER Boxed Warning
RISKS OF HEPATOTOXICITY and EMBRYO-FETAL TOXICITY Because of the risk of hepatotoxicity, TRACLEER is available only through a restricted program called the Bosentan Risk Evaluation and Mitigation Strategy (REMS). Under the Bosentan REMS, prescribers, patients, and pharmacies must enroll in the program [see Warnings and Precautions (5.2) ] . WARNING: RISKS OF HEPATOTOXICITY and EMBRYO-FETAL TOXICITY See full prescribing information for complete boxed warning. TRACLEER is available only through a ...
WARNING: RISKS OF HEPATOTOXICITY and EMBRYO-FETAL TOXICITY Because of the risk of hepatotoxicity, TRACLEER is available only through a restricted program called the Bosentan Risk Evaluation and Mitigation Strategy (REMS). Under the Bosentan REMS, prescribers, patients, and pharmacies must enroll in the program [see Warnings and Precautions (5.2) ] . WARNING: RISKS OF HEPATOTOXICITY and EMBRYO-FETAL TOXICITY See full prescribing information for complete boxed warning. TRACLEER is available only through a restricted distribution program called the Bosentan Risk Evaluation and Mitigation Strategy (REMS) because of the risk of hepatotoxicity ( 5.2 ): Elevations of liver aminotransferases (ALT, AST) and liver failure have been reported with TRACLEER ( 5.1 ). Measure liver aminotransferases prior to initiation of treatment and then monthly ( 2.1 , 5.1 ). Discontinue TRACLEER if aminotransferase elevations are accompanied by signs or symptoms of liver dysfunction or injury or increases in bilirubin ≥2×ULN ( 2.4 , 5.1 ). Based on animal data, TRACLEER may cause fetal harm if used during pregnancy ( 4.1 , 5.3 , 8.1 ). Females of reproductive potential: Exclude pregnancy before initiating treatment. Use effective contraception prior to initiation of treatment, during treatment and for one month after stopping TRACLEER ( 2.1 , 4.1 , 5.3 , 8.1 , 8.3 ). When pregnancy is detected, discontinue TRACLEER as soon as possible ( 5.3 ). Hepatotoxicity In clinical studies, TRACLEER caused at least 3-fold upper limit of normal (ULN) elevation of liver aminotransferases (ALT and AST) in about 11% of patients, accompanied by elevated bilirubin in a small number of cases. Because these changes are a marker for potential serious hepatotoxicity, serum aminotransferase levels must be measured prior to initiation of treatment and then monthly [see Dosage and Administration (2.4) , Warnings and Precautions (5.1) ] . In the postmarketing period, in the setting of close monitoring, rare cases of u
TRACLEER Competitive Set
ProThree rings of competition based on shared molecular targets and treated indications.
Direct competitors
Same target(s) AND same indication — head-to-head.
MoA expansion candidates
Same target(s), different indications — where else is this mechanism being explored?
Indication competitors
Same indication, different mechanism — what else might this patient receive?
Filters applied: drops same-active-ingredient (505(b)(2) reformulations), route-mismatch (topical vs systemic), and cross-therapeutic-area matches in same-indication rings.
What's emerging in TRACLEER's indications
See all emerging drugs →Phase 3 candidates targeting molecules with no FDA-approved drug, in indications TRACLEER treats. First-in-class if their pivotal trials read out positive.
Drugs Similar to TRACLEER
3 of 19FDA-approved drugs for similar conditions. Compare mechanisms and indications to understand treatment alternatives.
Clinical Trial Registry
32 trials| Trial | Sponsor ID | Phase | Status | Title |
|---|---|---|---|---|
| NCT06957002 BOSICART | P200041 2024-517030-17 | Ph 2 | not yet recruiting | Bosentan in the Treatment of Giant Cell Arteritis |
| NCT01241383 ScS-REINBO | P081217 | Ph 2 | completed | Effect of Bosentan in Scleroderma Renal Crisis |
| NCT04158635 | 21314 NCI-2021-06609, 19312 | Ph 1 | recruiting | Gemcitabine, Nab-Paclitaxel, and Bosentan for the Treatment of Unresectable Pancreatic Cancer |
| NCT05723874 results posted | 1346-0056 2021-006676-17 | Ph 1 | completed | A Study in Healthy Men to Test Whether Bosentan Influences the Amount of BI 425809 in the Blood |
| NCT04388124 ENDOTHELIN-2 | 2018/0350/HP | Ph 2 | recruiting | Endothelin-1 Receptor Blockade in Resistant Hypertension |
| NCT07081932 | 1305-0113 2025-521104-21-00, U1111-1321-0860 | Ph 1 | completed | A Study in Healthy Men to Test How Bosentan Influences the Amount of Nerandomilast in the Blood |
| NCT05072106 results posted | PM1183-A-019-20 | Ph 1 | completed | Study to Evaluate the Effect of Bosentan on the Pharmacokinetics of Lurbinectedin in Patients With Advanced Solid Tumors |
| NCT01338415 FUTURE 3 Ext results posted | AC-052-374 2010-021793-12 | Ph 3 | completed | FUTURE 3 Study Extension |
| NCT01223352 FUTURE 3 results posted | AC-052-373 | Ph 3 | completed | Effects of Two Dosing Regimens of Bosentan in Children With Pulmonary Arterial Hypertension |
| NCT00631475 BUILD OL results posted | AC-052-322 | Ph 3 | completed | Open Label Extension Study in Patients With Idiopathic Pulmonary Fibrosis Who Completed Protocol AC-052-321/ BUILD 3 / NCT00391443 |
| NCT01389856 FUTURE 4 results posted | AC-052-391 | Ph 3 | terminated | Persistent Pulmonary Hypertension of the Newborn |
| NCT01395732 HOME | AC-052-427 | Ph 4 | completed | Bosentan in Systemic Sclerosis |
| NCT04068272 BOSRET | IOBA-02-2016 | Ph 1 | completed | Safety of Bosentan in Type II Diabetic Patients |
| NCT04991207 | BIA-51058-107 2015-004350-17 | Ph 1 | completed | Effect of BIA 5-1058 400 mg on the Steady State Pharmacokinetics of Bosentan |
| NCT01392469 results posted | CQTI571A2102 2010-021344-17 | Ph 3 | completed | Pharmacokinetic Effects of QTI571 on Sildenafil and Bosentan in Pulmonary Arterial Hypertension Participants |
| NCT00638131 | BOS-ND-2007 | Ph 3 | terminated | Bosentan Use in Patients With Diabetic Nephropathy |
| NCT02480335 CEASESTIFF | NL49919.042.14 | Ph 4 | completed | The Clinical And Subclinical Effects on Arterial Stiffness of Bosentan in Patients With Systemic Sclerosis |
| NCT02317679 | 13-PP-10 | Ph 2 | completed | Treatment of Resistant Port-wine Stains With Bosentan and Pulsed Dye Laser: a Pilot Study |
| NCT02667704 results posted | 1199.239 2015-003819-38 | Ph 1 | completed | Influence of Bosentan on the Pharmacokinetics of Nintedanib |
| NCT00825266 results posted | SU-09052008-1295 IRB#7432 | Ph 2 | terminated | Insulin Resistance in Pulmonary Arterial Hypertension |
| NCT01518595 | 1-Fuhrmann | Ph 2 | terminated | Bosentan for Treatment of Hepatopulmonary Syndrome in Patients With Liver Cirrhosis |
| NCT00926627 BOPSAC | EudraCT - 2007-005117-18 | Ph 2 | terminated | Safety and Efficacy Study of Bosentan in Progressive Pulmonary Sarcoidosis |
| NCT01779609 | ET-EX-TRAINING | Ph 4 | completed | ET-blockade and Exercise-induced Vascular Adaptations in T2DM |
| NCT01779596 | ET-EX-ACUTE | Ph 4 | completed | ET-blockade and Exercise Induced Blood Flow in T2DM |
| NCT00679068 | 525FSM | Ph 4 | terminated | Effects of Bosentan on Respiratory Mechanics |
| NCT00820352 BADDHY | BO-001 EUDRACT Number: 2008-005514-40 | Ph 3 | completed | Safety and Efficacy of Bosentan in Patients With Diastolic Heart Failure and Secondary Pulmonary Hypertension |
| NCT01218607 BOMPA | UZL-S52480 | Ph 3 | completed | Bosentan for Mild Pulmonary Vascular Disease in Asd Patients. |
| NCT01352065 ERAATH | CHS-ERA-2011 | Ph 2, Ph 3 | completed | Characterization and Detection of Prolonged Endothelin Receptors Antagonists Administration |
| NCT01292551 TEMPO | TEMPO study 2010-022389-28 | Ph 2 | completed | Study of Placebo or Bosentan to Treat Patients With Single Ventricle Physiology. |
| NCT00581607 BOSAPAH | BOSAPAH-1 7-3-22-1 | Ph 2, Ph 3 | completed | Double Blind, Randomized Trial of Bosentan for Sarcoidosis Associated Pulmonary Hypertension |
| NCT00815347 results posted | 08-287-1 001 | Ph 2 | terminated | Bosentan for Poorly Controlled Asthma |
| NCT01662037 | SJTUMS-20120314 | Ph 2 | completed | Bosentan Therapy in Children With Functional Single Ventricle |
Active Pipeline
Ongoing clinical trials by development phase
Key Completed Trials
Completed studies with published results, ranked by significance
Trial Timeline
Full development history with FDA approval milestones
Understanding FDA Approval Types
| Count | Type | What it means |
|---|---|---|
| - | ORIG | Original approval - drug first enters market |
| - | SUPPL - Efficacy | New indication (new disease/condition approved) |
| - | SUPPL - Labeling | Label text changes (warnings, dosing updates) |
| - | SUPPL - Manufacturing | Production changes (new facility) |
| - | SUPPL - Chemistry | Formulation changes (new dosage strength) |
Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.
TRACLEER FDA Label Details
Indications & Usage
FDA Label (PDF)TRACLEER is indicated for the treatment of Pulmonary Arterial Hypertension; Congenital Heart Disease.
WARNING: RISKS OF HEPATOTOXICITY and EMBRYO-FETAL TOXICITY Because of the risk of hepatotoxicity, TRACLEER is available only through a restricted program called the Bosentan Risk Evaluation and Mitigation Strategy (REMS). Under the Bosentan REMS, prescribers, patients, and pharmacies must enroll in ...
Pro Intelligence Preview
Deep insights for TRACLEER
Revenue Insights
- • Quarterly revenue tracking
- • Historical trend analysis
Patent Timeline
- • Cliff: 2027
- • 2 active patents
Trial Analysis
- • 33 total trials
- • Stage: Declining
Competitive Landscape
- • 19 similar drugs
- • Same target/indication analysis
Full approval history • All patents • Revenue trends • Competitor analysis
Data Sources
Data sourced from official FDA and NIH databases. Click links to verify on original sources.
How We Calculate These Metrics
Trial Activity Stage
Measures the current development activity pattern based on trial phases, status, and trends. Important: This measures R&D activity, not commercial lifecycle.
Trial statuses: "Active" means recruiting or ongoing. "Completed" means reached planned endpoint. "Terminated" means stopped early—often due to safety, efficacy, or business reasons.
- Growth: High proportion of early-phase trials (Phase 1/2), active development
- Expansion: Significant Phase 3 activity, approaching or pursuing approvals
- Mature: Substantial Phase 4 post-marketing studies
- Stable: Mixed phase distribution, steady development
- Declining: Low active trial ratio, reduced R&D investment