Bosentan: uses, dosing, side effects & brands
Bosentan is an endothelin receptor antagonist sold in the U.S. under 2 brand and generic names, for pulmonary hypertension. Below: what the FDA label says, every product that contains it, what the pills look like, and its recall record.
Key facts
- Drug class
- Endothelin Receptor Antagonist
- Treats
- Pulmonary Hypertension
- Available as
- Tablet
- Sold as
- 2 products — Bosentan and Tracleer
- Prescription?
- Prescription only
- Generic available?
- Yes
- Boxed warning
- Boxed warning
How bosentan is dosed
From the FDA label for Bosentan (application ANDA213981). Other bosentan products — different forms, different strengths — are dosed differently. Follow the label for the one you were prescribed.
Patients older than 12 years of age: initiate at 62.5 mg orally twice daily; for patients weighing greater than 40 kg, increase to 125 mg orally twice daily after 4 weeks (2.2). Patients 12 years of age and younger: dosage is based on weight, see Table 1 ( 2.2 ). Reduce the dose and closely monitor patients developing aminotransferase elevations more than 3 X Upper Limit of Normal (ULN) ( 2.1 ). 2.1 Required Monitoring Healthcare professionals who prescribe bosentan must enroll in the Bosentan REMS and must comply with the required monitoring to minimize the risks associated with bosentan [see Warnings and Precautions ( 5.2 )] . Measure liver aminotransferase levels prior to initiation of treatment and then monthly [see Boxed Warning, Warnings and Precautions ( 5.1 , 5.2 )]. Exclude pregnancy before initiating treatment with bosentan in females of reproductive potential [see Boxed Warning, Contraindications ( 4.1 ), Warnings and Precautions ( 5.3 ), Use in Specific Populations ( 8.1 , 8.3 )] . 2.2 Recommended Dosage Administer bosentan orally following the dosing recommendations in Table 1. Doses above 125 mg twice daily did not appear to confer additional benefit sufficient to offset the increased risk of hepatotoxicity. Table 1 Dosing Recommendations Initial 4 weeks Maintenance (after 4 weeks) Patients > 12 years of age and > 40 kg 62.5 mg twice daily 125 mg twice daily…
Bosentan side effects
The following important adverse reactions are described elsewhere in the labeling: Hepatotoxicity [see Boxed Warning, Warnings and Precautions ( 5.1 )] Embryo-fetal Toxicity [see Boxed Warning, Warnings and Precautions ( 5.3 )] Fluid Retention [see Warnings and Precautions ( 5.4 )] Common adverse reactions (≥ 3% more than placebo) for the film- coated tablet are respiratory tract infection and anemia (6.1). Common adverse reactions (≥ 15%) for the dispersible tablet are upper respiratory tract infections and pyrexia ( 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact Zydus Pharmaceuticals (USA) Inc. at 1-877-993-8779 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Safety data on bosentan were obtained from 13 clinical studies (9 placebo-controlled and 4 open-label) in 870 adult patients with PAH and other diseases. Doses up to 8 times the currently recommended clinical dose (125 mg twice daily) were administered for a variety of durations. The exposure to bosentan in these trials ranged from 1 day to 4.1 years (n=94 for 1 year; n=61 for 1.5 years; and n=39 for more than 2 years).…
Who shouldn’t take bosentan
Pregnancy ( 4.1 ) Use with Cyclosporine A ( 4.2 ) Use with Glyburide ( 4.3 ) Hypersensitivity ( 4.4 ) 4.1 Pregnancy Use of bosentan is contraindicated in females who are pregnant [see Boxed Warning, Dosage and Administration ( 2.1 ), Warnings and Precautions ( 5.3 ), Use in Specific Populations ( 8.1 )] . 4.2 Use with Cyclosporine A Co-administration of cyclosporine A and bosentan resulted in markedly increased plasma concentrations of bosentan. Therefore, concomitant use of bosentan and cyclosporine A is contraindicated [see Drug Interactions ( 7.1 )] . 4.3 Use with Glyburide An increased risk of liver enzyme elevations was observed in patients receiving glyburide concomitantly with bosentan. Therefore co-administration of glyburide and bosentan is contraindicated [see Drug Interactions ( 7.1 )] . 4.4 Hypersensitivity Bosentan is contraindicated in patients who are hypersensitive to bosentan or any component of the product. Observed reactions include Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS), anaphylaxis, rash and angioedema [see Adverse Reactions ( 6.2 ), Description ( 11 )].
Bosentan drug interactions
Cytochrome P450: Coadministration of bosentan with drugs metabolized by CYP2C9 and CYP3A can increase exposure to bosentan and/or the coadministered drug ( 4.2 , 4.3 , 7.1 ). Hormonal contraceptives: bosentan use decreases contraceptive exposure and reduces effectiveness ( 7.2 ). 7.1 Cytochrome P450 Drug Interactions Bosentan is metabolized by CYP2C9 and CYP3A. Inhibition of these enzymes may increase the plasma concentration of bosentan [see Clinical Pharmacology ( 12.3 )] . Concomitant administration of both a CYP2C9 inhibitor (such as fluconazole or amiodarone) and a strong CYP3A inhibitor (e.g., ketoconazole, itraconazole) or a moderate CYP3A inhibitor (e.g., amprenavir, erythromycin, fluconazole, diltiazem) with bosentan will likely lead to large increases in plasma concentrations of bosentan. Co-administration of such combinations of a CYP2C9 inhibitor plus a strong or moderate CYP3A inhibitor with bosentan is not recommended. Bosentan is an inducer of CYP3A and CYP2C9. Consequently plasma concentrations of drugs metabolized by these two isozymes will be decreased when bosentan is co-administered. Bosentan had no relevant inhibitory effect on any CYP isozyme in vitro (CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP3A). Consequently, bosentan is not expected to increase the plasma concentrations of drugs metabolized by these enzymes. Figure 1 CYP3A induction-mediated effect of bosentan on other drugs F igure 2 Effect of other drugs on bosentan 7.2 Hormonal Contraceptives Hormonal contraceptives, including oral, injectable, transdermal and implantable forms, may not be reliable when bosentan is co-administered. Females should practice additional methods of contraception and not rely on hormonal contraception alone when taking bosentan [see Use in Specific Populations ( 8.3 )] . An interaction study demonstrated that co-administration of bosentan and a combination oral hormonal contraceptive produced average decreases of norethindrone and ethinyl estradiol levels of 14% and 31%, respectively. However, decreases in exposure were as much as 56% and 66%, respectively, in individual subjects. Image Image
Every bosentan product we track (2)
Same active ingredient — different manufacturer, form, price and FDA recall record. That last one is what our independent score measures.
| # | Drug | Rating | Type | Form | Generic? | Pharmacy pays | |
|---|---|---|---|---|---|---|---|
| 1 | 66/100 | Prescription | Tablet | No data | — | View → | |
| 2 | Not yet rated | Prescription | Tablet | No data | — | View → |
What bosentan pills look like
Imprint codes, colour and shape from the FDA’s labelling data. Match the imprint on your pill — or search any imprint.
Can you crush or split bosentan?
At least one bosentanproduct is labelled to be swallowed whole — crushing an extended-release tablet releases the whole day’s dose at once. Which applies depends on the form you were given.
What each bosentan label says about crushing, splitting and chewingHow long bosentan keeps
The date on a sealed pack is not the only one: some bosentan labels start a second clock once the product is opened or mixed, as short as 7 days.
Does bosentan expire? The in-use limits and storage rules from its labelsBosentan and breastfeeding
From LactMed, the US National Library of Medicine’s Drugs and Lactation Database — quoted, not rewritten.
Full LactMed record for bosentan: levels in milk, effects in breastfed infants, and the drugs it would consider insteadA study in one patient taking bosentan during breastfeeding found very low levels in milk. Another woman breastfed her preterm newborn while taking bosentan and sildenafil with no adverse effects reported. Amounts ingested by the infant are far below doses given to treat infants and would not be expected to cause any adverse effects in breastfed infants.
National Institute of Child Health and Human Development, record revised August 15, 2025. LactMed states its information is not a substitute for professional judgement.
What people report to the FDA about bosentan
The FDA Adverse Event Reporting System (FAERS) collects reports from patients and clinicians. It holds 14,328 reports naming bosentan, and the FDA flagged 68% of those reports as serious. The effects reported most often — leaving out reports about overdose, misuse or the condition being treated, which dominate the raw list for common medicines:
- dyspnoea1,347 reports
- fatigue728 reports
- headache624 reports
- diarrhoea543 reports
- pneumonia487 reports
- malaise480 reports
- nausea472 reports
- dizziness444 reports
Read these as a signal, not a rate. A report does not mean bosentan caused the effect — anyone can file one, and many describe people taking several medicines for several conditions. Crucially there is no denominator: FAERS does not record how many people took the drug, so these counts cannot be turned into “X% of patients” — a bigger number often just means a more widely used or more talked-about drug. Duplicates exist, and publicity drives reporting. For what is actually established, read the FDA label section above.
Source: openFDA drug/event (FAERS), retrieved July 25, 2026.
Related calculators
Frequently asked questions
What is bosentan?
Bosentan is an endothelin receptor antagonist used to treat Pulmonary Hypertension.
What kind of drug is bosentan?
The FDA classifies bosentan as an endothelin receptor antagonist. Endothelin receptor antagonists block endothelin-1, a natural substance that powerfully tightens blood vessels. By stopping it from acting on its receptors, these drugs let vessels relax and widen, lowering pressure in the lung arteries in conditions like pulmonary arterial hypertension. If you are checking whether it is safe to combine with something else, the class is what matters — two drugs from the same class usually should not be stacked.
Can you take bosentan with other medicines?
It depends on the medicine. We check it against the FDA labels rather than guessing: our interaction checker searches each drug's own label for the other and quotes what it says, naming the section it came from. Run bosentan against whatever else you take — and remember that a label not naming a drug is not the same as that combination being safe.
What brand names is bosentan sold under?
We track 2 bosentan-containing products in the U.S.: Bosentan and Tracleer. They are the same active ingredient; they differ in form, manufacturer, price and FDA recall record.
What forms does bosentan come in?
Across the brands we track, bosentan is currently marketed as tablet, per the FDA's National Drug Code Directory. Each form is dosed differently — follow the label for the exact product you were prescribed.
Is there a generic bosentan?
Yes. Our catalog lists 1 generic bosentan product alongside the brand versions. A generic has the same active ingredient and must meet the FDA's bioequivalence standard; it usually costs less. Ask your pharmacist which one your plan covers.
Cite this page
- APA
- pharmaranks. (2026, July 24). Bosentan: uses, dosing, side effects & brands. https://pharmaranks.com/drugs/bosentan
- MLA
- “Bosentan: uses, dosing, side effects & brands.” pharmaranks, 24 July 2026, https://pharmaranks.com/drugs/bosentan.
We summarise public FDA and NIH sources — for a clinical claim, cite the primary source we link to as well.
Sources: FDA openFDA drug label, National Drug Code Directory, and Enforcement (recall) database. This page reproduces public FDA data and is not medical advice. Dosing is set by your prescriber.
Read the full FDA label for bosentan on DailyMed (NIH) ↗ — including its boxed warning in full.