Macitentan — uses, dosing, side effects & the brands that sell it · pharmaranks
Macitentan: uses, dosing, side effects & brands
Macitentan 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.
By the pharmaranks editorial team·Reviewed against the FDA (openFDA label, NDC Directory & Enforcement) sources·How we research
From the FDA label for Macitentan (application ANDA211107). Other macitentan products — different forms, different strengths — are dosed differently. Follow the label for the one you were prescribed.
10 mg once daily. Doses higher than 10 mg once daily have not been studied in patients with PAH and are not recommended ( 2.1 ). 2.1 Recommended Dosage The recommended dosage of macitentan tablets is 10 mg once daily for oral administration. Doses higher than 10 mg once daily have not been studied in patients with PAH and are not recommended. 2.2 Pregnancy Testing in Females of Reproductive Potential Exclude pregnancy before initiating treatment with macitentan tablets in females of reproductive potential [see Boxed Warning, Contraindications (4.1), Warnings and Precautions (5.1), and Use in Specific Populations (8.3)] .
Macitentan side effects
Clinically significant adverse reactions that appear in other sections of the labeling include: Embryo-fetal Toxicity [see Warnings and Precautions (5.1)] Hepatotoxicity [see Warnings and Precautions (5.2)] Fluid Retention [see Warnings and Precautions (5.3)] Decrease in Hemoglobin [see Warnings and Precautions (5.4)] Most common adverse reactions (more frequent than placebo by ≥3%) are anemia, nasopharyngitis/pharyngitis, bronchitis, headache, influenza, and urinary tract infection ( 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact Torrent Pharma Inc. at 1-800-912-9561 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trial Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in 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 clinical practice. Safety data for macitentan tablets were obtained primarily from one placebo-controlled clinical study in 742 patients with PAH (SERAPHIN study) [see Clinical Studies (14.1)] . The exposure to macitentan tablets in this trial was up to 3.6 years with a median exposure of about 2 years (N=542 for 1 year; N=429 for 2 years; and N=98 for more than 3 years). The overall incidence of treatment discontinuations because of adverse events was similar across macitentan…
Who shouldn’t take macitentan
Pregnancy ( 4.1 ) Hypersensitivity ( 4.2 ) 4.1 Pregnancy Macitentan tablets may cause fetal harm when administered to a pregnant woman. Macitentan tablets are contraindicated in females who are pregnant. Macitentan tablets were consistently shown to have teratogenic effects when administered to animals. If macitentan tablets are used during pregnancy, advise the patient of the potential risk to a fetus [see Warnings and Precautions (5.1) and Use in Specific Populations (8.1)] . 4.2 Hypersensitivity Macitentan tablets is contraindicated in patients with a history of a hypersensitivity reaction to macitentan or any component of the product [see Adverse Reactions (6.2)] .
Every macitentan product we track (2)
Same active ingredient — different manufacturer, form, price and FDA recall record. That last one is what our independent score measures.
Macitentan is an endothelin receptor antagonist. The chemical name of macitentan is N-[5-(4-Bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide. It has a molecular formula of C 19 H 20 Br 2 N 6 O 4 S and a molecular weight of 588.27. Macitentan is achiral and has the following structural formula: Macitentan is a crystalline powder that is insoluble in water. In the solid state macitentan is very stable, is not hygroscopic, and is not light sensitive. Macitentan tablets are available as a 10 mg film-coated tablet for once daily oral administration. The tablets include the following inactive ingredients: cellulose microcrystalline, magnesium stearate, mannitol 25, polysorbate 80, povidone K- 30, silicified microcrystalline cellulose, and sodium starch glycolate (Type-A). The tablets are film-coated with a coating material containing lecithin (soya), polyvinyl alcohol-part, hydrolyzed, talc, titanium dioxide, and xanthan gum. structure
What kind of drug is macitentan?
The FDA classifies macitentan 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 macitentan 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 macitentan 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 macitentan sold under?
We track 2 macitentan-containing products in the U.S.: Macitentan and Opsumit. They are the same active ingredient; they differ in form, manufacturer, price and FDA recall record.
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.
Macitentan drug interactions
Strong CYP3A4 inducers (rifampin) reduce exposure to macitentan: avoid co-administration with macitentan tablets ( 7.1 , 12.3 ). Strong CYP3A4 inhibitors (ketoconazole, ritonavir) increase exposure to macitentan: avoid co-administration with macitentan tablets ( 7.2 , 12.3 ). 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 macitentan tablets ( 7.3 , 12.3 ). 7.1 Strong CYP3A4 Inducers Strong inducers of CYP3A4 such as rifampin significantly reduce macitentan exposure. Concomitant use of macitentan tablets with strong CYP3A4 inducers should be avoided [see Clinical Pharmacology (12.3)] . 7.2 Strong CYP3A4 Inhibitors Concomitant use of strong CYP3A4 inhibitors like ketoconazole approximately double macitentan exposure. Many HIV drugs like ritonavir are strong inhibitors of CYP3A4. Avoid concomitant use of macitentan tablets with strong CYP3A4 inhibitors [see Clinical Pharmacology (12.3)] . Use other PAH treatment options when strong CYP3A4 inhibitors are needed as part of HIV treatment [see Clinical Pharmacology (12.3)] . 7.3 Moderate Dual or Combined CYP3A4 and CYP2C9 Inhibitors Concomitant use of moderate dual inhibitors of CYP3A4 and CYP2C9 such as fluconazole is predicted to increase macitentan exposure approximately 4-fold based on…
Across the brands we track, macitentan 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 macitentan?
Yes. Our catalog lists 1 generic macitentan 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.