TheraRadar
Data updated: May 26, 2026

OPSYNVI (macitentan)

Endothelin Receptor Antagonists
Cardiovascular Approved 2024-03-22

Opsynvi is a combination medication used for the long-term management of pulmonary arterial hypertension in adults with WHO functional class II or III symptoms. It helps patients by reducing the likelihood of hospitalization and clinical worsening while also improving their physical exercise capacity. This therapy combines two different types of medicine into a single treatment to address the underlying issues of the disease.

Source: FDA Label • ACTELION • Endothelin Receptor Antagonist

How OPSYNVI Works

This medication works by blocking endothelin receptors to prevent blood vessel narrowing and inflammation while simultaneously inhibiting the PDE5 enzyme to increase levels of cyclic guanosine monophosphate (cGMP). These combined actions promote the relaxation of pulmonary vascular smooth muscle cells and encourage vasodilation. By targeting these two pathways, the drug helps improve blood flow through the pulmonary vascular bed.

1
Indication
--
Phase 3 Trials
2
Years on Market

Details

Status
Prescription
First Approved
2024-03-22
Patent Cliff
2029

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Routes
ORAL
Dosage Forms
TABLET

Companies

Active Ingredient: MACITENTAN , TADALAFIL

OPSYNVI Approval History

2025
2026
Original
New Indication
New Form
Label Update
6 FDA actions from 2024 to 2025
Apr 2025 SUPPL
Update · REMS
Dec 2024 SUPPL
Update · REMS
Mar 2024 ORIGINAL
New Combo · Type 4 - New Combination

What OPSYNVI Treats

1 indications

OPSYNVI is approved for 1 conditions since its original approval in 2024. These indications span multiple therapeutic areas including oncology, immunology, and more.

  • Pulmonary Arterial Hypertension
Source: FDA Label

OPSYNVI Boxed Warning

EMBRYO-FETAL TOXICITY OPSYNVI is contraindicated for use during pregnancy because it may cause fetal harm based on animal data [see Contraindications (4.1) , Warnings and Precautions (5.1) , Use in Specific Populations (8.1) ]. Therefore, for females of reproductive potential, exclude pregnancy before the start of treatment with OPSYNVI. Advise use of effective contraception before the initiation of treatment, during treatment, and for one month after stopping treatment with OPSYNVI [see Dosage ...

OPSYNVI Competitive Set

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Filters applied: drops same-active-ingredient (505(b)(2) reformulations), route-mismatch (topical vs systemic), and cross-therapeutic-area matches in same-indication rings.

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Clinical Trial Registry

29 trials
Trial Sponsor ID Phase Status Title
NCT05179876 PLATYPUS CR109121 NOPRODPAPUH3001, 2021-002297-11 Ph 3 recruiting A Study Providing Treatment Access in Participants With Pulmonary Hypertension Completing a Parent Study and Having no Other Option
NCT05167825 results posted CR109128 67896062PAH3001, 2023-000984-30 Ph 3 completed A Study of Macitentan in Japanese Pediatric Participants With Pulmonary Arterial Hypertension
NCT02932410 TOMORROW results posted AC-055-312 Ph 3 completed A Study to Assess Whether Macitentan Delays Disease Progression in Children With Pulmonary Arterial Hypertension (PAH)
NCT04271475 MACiTEPH results posted CR108742 67896062CTP3001, 2019-004131-24 Ph 3 terminated A Study to Evaluate Efficacy and Safety of Macitentan 75 mg in Inoperable or Persistent/Recurrent Chronic Thromboembolic Pulmonary Hypertension
NCT03359291 AC-055-122 Ph 1 completed Clinical Study to Investigate the Effect of Macitentan on the Concentrations of Rosuvastatin in the Blood of Healthy Male Subjects
NCT01346930 MUSIC OL AC-055B202 Ph 2 withdrawn Safety and Tolerability Study of Macitentan in Patients With Idiopathic Pulmonary Fibrosis
NCT03422328 UMBRELLA AC-055-314 2017-003934-10 Ph 3 completed A Clinical Study to Investigate the Long-term Safety of the Drug Macitentan in Patients With Pulmonary Hypertension Who Were Previously Treated With Macitentan in Clinical Studies.
NCT05731492 CR109286 2022-002754-74, 67896062PAH1013 Ph 1 withdrawn A Study of Macitentan in Children Below 2 Years of Age
NCT04235270 CR108735 67896062PAH1006 Ph 1 completed A Study of Macitentan and Tadalafil as a Fixed Dose Combination and the Free Combination in Healthy Adult Participants
NCT05392530 CR109202 2022-000275-39, 67896062PAH1012 Ph 1 completed A Study of Two Different Test Formulations Compared to the Reference Formulation of Macitentan in Healthy Adult Participants
NCT05433675 CR109185 67896062PAH1010, 2022-000262-17 Ph 1 completed A Study of Two Macitentan Formulations in Healthy Adult Participants
NCT02310672 REPAIR results posted AC-055-403 Ph 4 completed REPAIR: Right vEntricular Remodeling in Pulmonary ArterIal hypeRtension
NCT02558231 TRITON results posted AC-065A308 Ph 3 completed The Efficacy and Safety of Initial Triple Versus Initial Dual Oral Combination Therapy in Patients With Newly Diagnosed Pulmonary Arterial Hypertension
NCT00667823 SERAPHIN OL results posted AC-055-303 Ph 3 completed Clinical Study to Assess the Long-term Safety and Tolerability of ACT 064992 in Patients With Symptomatic Pulmonary Arterial Hypertension
NCT02112487 AC-055-311 Ph 3 completed Extension of the Psychometric Validation Study ORCHESTRA in Patients With PAH
NCT02060721 MERIT-2 results posted AC-055E202 2013-003457-25 Ph 2 completed Clinical Study to Assess the Safety, Tolerability and Efficacy of Macitentan in Subjects With Inoperable Chronic Thromboembolic Pulmonary Hypertension
NCT02382016 PORTICO results posted AC-055-404 Ph 4 completed PORtopulmonary Hypertension Treatment wIth maCitentan - a randOmized Clinical Trial
NCT04211272 CR108727 2019-004001-27, 67896062PAH1003 Ph 1 completed A 2-part Study to Investigate the Effect of Macitentan in Healthy Male Participants
NCT04963439 CR109027 2021-001258-67, 67896062PAH1008 Ph 1 completed A Study of Two Macitentan Pediatric Formulations in Healthy Adult Participants
NCT02021292 MERIT-1 results posted AC-055E201 Ph 2 completed Clinical Study to Assess the Efficacy, Safety and Tolerability of Macitentan in Subjects With Inoperable Chronic Thromboembolic Pulmonary Hypertension
NCT03153111 SERENADE results posted AC-055G202 2016-003653-15 Ph 2 completed A Study to Evaluate Whether Macitentan is an Effective and Safe Treatment for Patients With Heart Failure With Preserved Ejection Fraction and Pulmonary Vascular Disease
NCT05373108 results posted 18-001544 Ph 4 completed Endothelin-1 and Cardiac Allograft Vasculopathy (CAV)
NCT02893176 14-001710 Ph 4 withdrawn Macitentan in the Treatment of Organ Rejection After Lung Transplantation
NCT02651272 MENSCH results posted H-33165 Ph 2 terminated Macitentan in Pulmonary Hypertension of Sickle Cell Disease
NCT02968901 OPTIMA AC-055-405 Ph 4 terminated Clinical Study Evaluating the Effects of First-line Oral cOmbination theraPy of maciTentan and tadalafIl in Patients With Newly Diagnosed pulMonary Arterial Hypertension (OPTIMA)
NCT02070991 MELODY-1 results posted AC-055G201 Ph 2 completed Clinical Study to Evaluate the Safety and Tolerability of Macitentan in Subjects With Combined Pre- and Post-capillary Pulmonary Hypertension (CpcPH) Due to Left Ventricular Dysfunction
NCT01841762 results posted AC-055-401 Ph 3 completed Clinical Study of Macitentan in Patients With Pulmonary Arterial Hypertension to Psychometrically Validate the PAH-SYMPACT Instrument
NCT01847014 SYMPHONYext results posted AC-055-402 Ph 3 terminated Clinical Study of Macitentan in Patients With PAH to Psychometrically Validate PAH-SYMPACT Instrument
NCT02081690 ORCHESTRA results posted AC-055-310 Ph 3 terminated A Pulmonary Arterial Hypertension Study With Macitentan to Validate the PAH-SYMPACT™ in France, Italy and Spain
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Active Pipeline

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Ongoing clinical trials by development phase

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Key Completed Trials

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Completed studies with published results, ranked by significance

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Trial Timeline

Full development history with FDA approval milestones

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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.

OPSYNVI FDA Label Details

Indications & Usage

FDA Label (PDF)

OPSYNVI is indicated for the treatment of Pulmonary Arterial Hypertension.

⚠️ BOXED WARNING

WARNING: EMBRYO-FETAL TOXICITY OPSYNVI is contraindicated for use during pregnancy because it may cause fetal harm based on animal data [see Contraindications (4.1) , Warnings and Precautions (5.1) , Use in Specific Populations (8.1) ]. Therefore, for females of reproductive potential, exclude pregn...

View full patent landscape →
6 OB patents · 3 families · 158 international docs across 37 countries

OPSYNVI Patents & Exclusivity

Latest Patent: Oct 2029
Exclusivity: Sep 2031

Patents (6 active)

US8268847*PED Expires Oct 18, 2029
US8268847 Expires Apr 18, 2029
US10946015*PED Expires Mar 11, 2027
US10946015 Expires Sep 11, 2026
US7094781*PED Expires Jun 5, 2026
US7094781 Expires Dec 5, 2025

Exclusivity

NP Until Mar 2027
ODE-475 Until Mar 2031
NP Until Mar 2027
ODE-475 Until Mar 2031
PED Until Sep 2027
PED Until Sep 2027
PED Until Sep 2031
PED Until Sep 2031
NP Until Mar 2027
ODE-475 Until Mar 2031
NP Until Mar 2027
ODE-475 Until Mar 2031
PED Until Sep 2027
PED Until Sep 2027
PED Until Sep 2031
PED Until Sep 2031
Source: FDA Orange Book

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Revenue Insights

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  • Historical trend analysis

Patent Timeline

  • Cliff: 2029
  • 24 active patents

Trial Analysis

  • Clinical trial tracking
  • Development stage analysis

Competitive Landscape

  • 18 similar drugs
  • Same target/indication analysis
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Data Sources

Data sourced from official FDA and NIH databases. Click links to verify on original sources.