LETAIRIS (ambrisentan) · Gilead Sciences
Letairis is an endothelin receptor antagonist indicated for the treatment of WHO Group 1 pulmonary arterial hypertension (PAH) in adult patients to improve exercise ability and delay clinical worsening. It is also indicated in combination with tadalafil to reduce the risks of disease progression and hospitalization for worsening PAH. Clinical effectiveness was established predominantly in patients with WHO Functional Class II–III symptoms with etiologies of idiopathic or heritable PAH (60%) or PAH associated with connective tissue diseases (34%).
How LETAIRIS Works
Ambrisentan is a high-affinity, highly selective ( >4000-fold) endothelin receptor antagonist (ERA) targeting the endothelin type A (ET_A) receptor. In patients with PAH, concentrations of Endothelin-1 (ET-1)—a potent peptide that mediates vasoconstriction and cell proliferation—are significantly elevated. While ET_A receptors mediate vasoconstriction and cell proliferation, ET_B receptors are associated with vasodilation and ET-1 clearance. By selectively blocking the ET_A receptor, ambrisentan inhibits the pathogenic effects of ET-1 in the pulmonary vascular smooth muscle and endothelium.
Development Insights
Details
- Status
- Prescription
- First Approved
- 2007-06-15
- Patent Cliff
- 2031
- Routes
- ORAL
- Dosage Forms
- TABLET
LETAIRIS Approval History
What LETAIRIS Treats
1 indicationsLETAIRIS is approved for 1 conditions since its original approval in 2007. These indications span multiple therapeutic areas including oncology, immunology, and more.
LETAIRIS Boxed Warning
EMBRYO-FETAL TOXICITY Letairis is contraindicated for use during pregnancy because it may cause major birth defects if used by pregnant patients, based on studies in animals [see Contraindications (4.1) , Warnings and Precautions (5.1) , and Use in Specific Populations (8.1) ] . Therefore, for females of reproductive potential, exclude pregnancy before the initiation of treatment with Letairis. Advise use of effective contraception before initiation, during treatment, and for one month after tre...
WARNING: EMBRYO-FETAL TOXICITY Letairis is contraindicated for use during pregnancy because it may cause major birth defects if used by pregnant patients, based on studies in animals [see Contraindications (4.1) , Warnings and Precautions (5.1) , and Use in Specific Populations (8.1) ] . Therefore, for females of reproductive potential, exclude pregnancy before the initiation of treatment with Letairis. Advise use of effective contraception before initiation, during treatment, and for one month after treatment with Letairis [see Dosage and Administration (2.2) Contraindications (4.1) , Warnings and Precautions (5.1) , and Use in Specific Populations (8.1 , 8.3) ]. When pregnancy is detected, discontinue Letairis as soon as possible ( 5.1 ). WARNING: EMBRYO-FETAL TOXICITY See full prescribing information for complete boxed warning. Based on animal data Letairis may cause fetal harm if used during pregnancy ( 4.1 , 5.1 , 8.1 ). Females of reproductive potential: Exclude pregnancy before the start of treatment. Use effective contraception prior to initiation of treatment, during treatment, and for one month after treatment with Letairis ( 2.2 , 4.1 , 5.1 , 8.1 , 8.3 ) When pregnancy is detected, discontinue Letairis as soon as possible ( 5.1 ).
LETAIRIS 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.
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 LETAIRIS's indications
See all emerging drugs →Phase 3 candidates targeting molecules with no FDA-approved drug, in indications LETAIRIS treats. First-in-class if their pivotal trials read out positive.
Drugs Similar to LETAIRIS
3 of 18FDA-approved drugs for similar conditions. Compare mechanisms and indications to understand treatment alternatives.
Gilead Sciences's other novel FDA approvals
Other CDER-designated drugs from the same sponsor (2016–2025).
Clinical Trial Registry
27 trials| Trial | Sponsor ID | Phase | Status | Title |
|---|---|---|---|---|
| NCT07245680 COMMODITIES | APHP230847 2023-509891-40-00 | Ph 3 | recruiting | COMMODITIES Trial: Initial Dual Oral Therapy vs Monotherapy in PAH With Cardiovascular Comorbidities |
| NCT06256432 | N-003-CRD005 | Ph 2 | active not recruiting | Endothelin Receptor Antagonism With Ambrisentan to Treat Hepatorenal Syndrome |
| NCT04393246 | TACTIC-E | Ph 2, Ph 3 | completed | mulTi-Arm Therapeutic Study in Pre-ICu Patients Admitted With Covid-19 - Experimental Drugs and Mechanisms |
| NCT04771000 | N-003-CRD008 | Ph 2 | terminated | A Study of Micro Dose Ambrisentan in Hospitalized Patients With Respiratory Insufficiency Due to COVID-19 |
| NCT01342952 results posted | 114588 2010-021572-29 | Ph 2 | completed | Long-term Ambrisentan Extension Study for Pediatric Patients Who Participated in AMB112529 |
| NCT05437224 AMBLE | AMBEL | Ph 3 | completed | Efficacy and Safety Study of Ambrisentan in Chinese Patients With Pulmonary Arterial Hypertension |
| NCT01338636 EiPAH results posted | 2008P000687 | Ph 4 | completed | An Open-Label Uncontrolled Study of the Safety and Efficacy of Ambrisentan in Participants With Exercise-Induced Pulmonary Arterial Hypertension (PAH) |
| NCT03827200 | N-003-CRD003 2018-002088-25 | Ph 2 | terminated | A Study Evaluating the Utility of Ambrisentan in Lowering Portal Pressure in Patients With Liver Cirrhosis |
| NCT01224210 Portopulm results posted | Ambrisentan Portopulm Study | Ph 3 | completed | Ambrisentan in Patients With Porto-pulmonary Hypertension A Multicenter Open Label Trial |
| NCT01051960 results posted | 10-000567 | Ph 4 | completed | Exercise Induced Pulmonary Hypertension in Systemic Sclerosis and Treatment With Ambrisentan |
| NCT00777920 ABS-LT results posted | GS-US-300-0124 | Ph 3 | completed | Study of Ambrisentan in Participants With Pulmonary Hypertension |
| NCT00840463 results posted | IN-US-300-0126 | Ph 4 | terminated | Safety and Efficacy Trial to Treat Diastolic Heart Failure Using Ambrisentan |
| NCT02290613 EDITA results posted | 2014-05ED | Ph 2 | completed | Early Treatment of Borderline Pulmonary Arterial Hypertension Associated With Systemic Sclerosis (SSc-APAH) |
| NCT02712346 | Endothelin 5U01HL117684 | Ph 1 | completed | The Role of Endothelin-1 in Sickle Cell Disease |
| NCT02080637 results posted | Pro00050118 | Ph 2 | completed | Ambrisentan in Single Ventricle |
| NCT02885012 Letairis results posted | 00046009 | Ph 4 | terminated | Crossover Study From Macitentan or Bosentan Over to Ambrisentan |
| NCT00851929 | 17747 | Ph 2, Ph 3 | completed | Ambrisentan (Letairis) for Sarcoidosis Associated Pulmonary Hypertension |
| NCT01971580 results posted | IN-US-300-D076 | Ph 4 | completed | The Effects of Ambrisentan on Exercise Capacity in Fontan Patients |
| NCT01178073 AMBITION results posted | 112565 | Ph 3 | completed | A Study of First-Line Ambrisentan and Tadalafil Combination Therapy in Subjects With Pulmonary Arterial Hypertension (PAH) |
| NCT01808313 results posted | 115812 | Ph 3 | completed | Efficacy Study of Ambrisentan in Chinese Patients With Pulmonary Arterial Hypertension (PAH) |
| NCT01733095 | PoPH-GRZ ambrisentan | Ph 1, Ph 2 | withdrawn | Ambrisentan for Treatment of Portopulmonary Hypertension |
| NCT01330108 SCOBA-PH results posted | SCOBA-PH | Ph 4 | completed | Safely Change From Bosentan to Ambrisentan in Pulmonary Hypertension |
| NCT00879229 ARTEMIS-PH results posted | GS-US-300-0128 | Ph 3 | terminated | ARTEMIS-PH - Study of Ambrisentan in Subjects With Pulmonary Hypertension Associated With Idiopathic Pulmonary Fibrosis |
| NCT00768300 ARTEMIS-IPF results posted | GS-US-231-0101 | Ph 3 | terminated | (ARTEMIS-IPF) Randomized, Placebo-Controlled Study to Evaluate Safety and Effectiveness of Ambrisentan in IPF |
| NCT01530464 GQ01 results posted | Pro00028417 | Ph 1 | completed | The Safety Evaluation of Aminophylline and Ambrisentan When Administered Orally Alone and in Combination to Healthy Volunteers |
| NCT01352065 ERAATH | CHS-ERA-2011 | Ph 2, Ph 3 | completed | Characterization and Detection of Prolonged Endothelin Receptors Antagonists Administration |
| NCT00617305 ATHENA-1 results posted | GS-US-300-0117 | Ph 4 | completed | Study of Add-on Ambrisentan Therapy to Background Phosphodiesterase Type-5 Inhibitor (PDE5i) Therapy in Pulmonary Arterial Hypertension (ATHENA-1) |
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.
LETAIRIS FDA Label Details
Indications & Usage
FDA Label (PDF)Letairis is indicated for the treatment of pulmonary arterial hypertension (PAH) (WHO Group 1) in adult patients: To improve exercise ability and delay clinical worsening. In combination with tadalafil to reduce the risks of disease progression and hospitalization for worsening PAH, and to improve exercise ability [see Clinical Studies ]. Studies establishing effectiveness included predominantly patients with WHO Functional Class II–III symptoms and etiologies of idiopathic or heritable PAH (60%) or PAH associated with connective tissue diseases (34%). Letairis is an endothelin receptor antago...
WARNING: EMBRYO-FETAL TOXICITY Letairis is contraindicated for use during pregnancy because it may cause major birth defects if used by pregnant patients, based on studies in animals [see Contraindications (4.1) , Warnings and Precautions (5.1) , and Use in Specific Populations (8.1) ] . Therefore, ...
Pro Intelligence Preview
Deep insights for LETAIRIS
Revenue Insights
- • Quarterly revenue tracking
- • Historical trend analysis
Patent Timeline
- • Cliff: 2031
- • 12 active patents
Trial Analysis
- • 27 total trials
- • Stage: Declining
Competitive Landscape
- • 18 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