Macitentan is an endothelin receptor antagonist. It is available as tablets for oral use. MedsAcross supplies Macitentan for export from India to licensed hospitals, importers and physicians acting for named patients, with the documents each country requires.
Information from the US FDA prescribing information, retrieved 12 November 2026. Not yet medically reviewed.How we review
From the regulator-approved product information. Each section names its source.
OPSUMIT is an endothelin receptor antagonist (ERA) indicated for the treatment of pulmonary arterial hypertension (PAH, WHO Group I) in adults to reduce the risks of disease progression and hospitalization for PAH.
Source: US FDA prescribing information
Endothelin (ET)-1 and its receptors (ET A and ET B ) mediate a variety of deleterious effects, such as vasoconstriction, fibrosis, proliferation, hypertrophy, and inflammation. In disease conditions such as PAH, the local ET system is upregulated and is involved in vascular hypertrophy and in organ damage. Macitentan is an endothelin receptor antagonist that inhibits the binding of ET-1 to both ET A and ET B receptors. Macitentan displays high affinity and sustained occupancy of the ET receptors in human pulmonary arterial smooth muscle cells. One of the metabolites of macitentan is also pharmacologically active at the ET receptors and is estimated to be about 20% as potent as the parent drug in vitro. The clinical impact of dual endothelin blockage is unknown.
Source: US FDA prescribing information
10 mg once daily. Doses higher than 10 mg once daily have not been studied in patients with PAH and are not recommended. Recommended Dosage The recommended dosage of OPSUMIT is 10 mg once daily for oral administration. Pregnancy Testing in Females of Reproductive Potential Exclude pregnancy before initiating treatment with OPSUMIT in females of reproductive potential.
Source: US FDA prescribing information
Pregnancy. Hypersensitivity Pregnancy OPSUMIT may cause fetal harm when administered to a pregnant woman. OPSUMIT is contraindicated in females who are pregnant. OPSUMIT was consistently shown to have teratogenic effects when administered to animals. If OPSUMIT is used during pregnancy, advise the patient of the potential risk to a fetus.
Source: US FDA prescribing information
Boxed warning (embryo-fetal toxicity opsumit): is contraindicated for use during pregnancy because it may cause fetal harm based on animal data. Therefore, for females of reproductive potential, exclude pregnancy before the start of treatment with OPSUMIT. Advise use of effective contraception before the initiation of treatment, during treatment, and for one month after stopping treatment with OPSUMIT. ERAs cause hepatotoxicity and liver failure. Obtain baseline liver enzymes and monitor as clinically indicated. Fluid retention may require intervention. Decreases in hemoglobin. Pulmonary edema in patients with pulmonary veno-occlusive disease. If confirmed, discontinue treatment. Decreases in sperm count have been observed in patients taking ERAs.
Source: US FDA prescribing information
Clinically significant adverse reactions that appear in other sections of the labeling include: Embryo-fetal Toxicity Hepatotoxicity Fluid Retention Decrease in Hemoglobin Most common adverse reactions (more frequent than placebo by ≥3%) are anemia, nasopharyngitis/pharyngitis, bronchitis, headache, influenza, and urinary tract infection.
Source: US FDA prescribing information
Strong CYP3A4 inducers (rifampin) reduce exposure to macitentan: avoid co-administration with OPSUMIT. Strong CYP3A4 inhibitors (ketoconazole, ritonavir) increase exposure to macitentan: avoid co-administration with OPSUMIT. Moderate dual CYP3A4 and CYP2C9 inhibitors (fluconazole, amiodarone) or use of combined CYP3A4 and CYP2C9 inhibitors may increase exposure to macitentan: avoid co-administration with OPSUMIT.
Source: US FDA prescribing information
Store at 20 ºC to 25 ºC (68 ºF to 77 ºF). Excursions are permitted between 15 °C and 30 °C (59 °F and 86 °F).
Source: US FDA prescribing information
For healthcare professionals and buyers. This is not medical advice. Treatment decisions belong to the prescriber.
2 presentations of Macitentan, sorted by availability.
| Medicine | Manufacturer | Register | Availability |
|---|---|---|---|
| Macitentan 10 mg tabletOralGeneric name | — | US FDA | Available on request |
| Opsumit 10 mg tabletOral | Actelion Pharmaceuticals | US FDA | Available on request |
1 brand names across 1 markets.
United States
Approval facts from US FDA, EMA and CDSCO data, and registration status by country where we hold register data.
Conditions linked to Macitentan in public data. This is not a list of approved uses, see the clinical information.
Yes, on request. MedsAcross lists 2 presentations of Macitentan and sources them for licensed hospitals, importers and physicians against valid import documents.
The catalogue lists 1 brand names for Macitentan, including Opsumit.
Yes. The US FDA first approved Macitentan on 18 October 2013, according to Drugs@FDA.
Yes. Macitentan has a central EU marketing authorisation (status: authorised), according to European Medicines Agency data.
No listed presentation of Macitentan is recorded as needing a cold chain. Storage conditions are shown on each presentation page.
Macitentan is classified under ATC code C02KX04 (Macitentan).
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