Based on 1 source · Recall-safety score from FDA recall history — this product's own recalls and its manufacturer's record. Not an efficacy or quality rating. methodology →
Key facts
- Active ingredient
- Macitentan
- Drug class
- Endothelin Receptor Antagonist
- Form
- Tablet
- Strength
- Macitentan 10MG
- Type
- Prescription (Rx)
- Brand or generic
- Generic
- May treat
- pulmonary hypertension
- Manufacturer
- Torrent
- Half-life
- about 16 hours (apparent elimination half-life) (how long it stays in your system)
- FDA application
- ANDA211107
- FDA boxed warning
- Yes — see the boxed warning
What is Macitentan?
From the FDA label: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
How to use
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)] .
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…
FDA Boxed Warning (the FDA’s most serious warning)
Boxed (black-box) warning — from the FDA label
See full prescribing information for complete boxed warning. Based on animal data, macitentan tablets may cause fetal harm if used during pregnancy (4.1, 5.1, 8.1). Females of reproductive potential: exclude pregnancy before start of treatment. Prevent pregnancy prior to initiation of treatment, during treatment and for one month after treatment by using effective methods of contraception (2.2, 8.3). When pregnancy is detected, discontinue macitentan tablets as soon as possible (5.1). WARNING: EMBRYO-FETAL TOXICITY Macitentan tablets are 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 macitentan tablets. Advise use of effective contraception before the initiation of treatment, during treatment, and for one month after stopping treatment with macitentan tablets [see Dosage and Administration (2.2), Use in Specific Populations (8.3)] . When pregnancy is detected, discontinue macitentan tablets as soon as possible [see Warnings and Precautions (5.1)] .
Warnings
Important safety information
ERAs cause hepatotoxicity and liver failure. Obtain baseline liver enzymes and monitor as clinically indicated ( 5.2 ). Fluid retention may require intervention ( 5.3 ). Decreases in hemoglobin ( 5.4 ). Pulmonary edema in patients with pulmonary veno-occlusive disease. If confirmed, discontinue treatment ( 5.5 ). Decreases in sperm count have been observed in patients taking ERAs ( 5.6 ). 5.1 Embryo-fetal Toxicity Based on data from animal reproduction studies, macitentan tablets may cause fetal harm when administered to a pregnant patient and is contraindicated during pregnancy. The available human data for ERAs do not establish the presence or absence of major birth defects related to the use of macitentan tablets. Advise patients who can become pregnant of the potential risk to a fetus. Obtain a pregnancy test prior to initiation of therapy with macitentan tablets. Advise patients who can become pregnant to use effective contraceptive methods prior to initiation of treatment, during treatment, and for one month after discontinuation of treatment with macitentan tablets. When pregnancy is detected, discontinue use as soon as possible [see Dosage and Administration (2.2), Contraindications (4.1), and Use in Specific Populations (8.1, 8.3)] . 5.2 Hepatotoxicity ERAs have caused elevations of aminotransferases, hepatotoxicity, and liver failure. The incidence of elevated aminotransferases in the study of macitentan tablets in PAH is shown in Table 1. Table 1: Incidence of Elevated Aminotransferases in the SERAPHIN Study Macitentan tablets 10 mg ( N=242 ) Placebo (N=249) >3 x ULN 3.4% 4.5% >8 x ULN 2.1% 0.4% In the placebo-controlled study of macitentan tablets, discontinuations for hepatic adverse events were 3.3% in the macitentan tablets 10 mg group vs. 1.6% for placebo. Obtain liver enzyme tests prior to initiation of macitentan tablets and repeat during treatment as clinically indicated [see Adverse Reactions (6.2)] . Advise patients to report symptoms suggesting hepatic injury (nausea, vomiting, right upper quadrant pain, fatigue, anorexia, jaundice, dark urine, fever, or itching). If clinically relevant aminotransferase elevations occur, or if elevations are accompanied by an increase in bilirubin >2 x ULN, or by clinical symptoms of hepatotoxicity, discontinue macitentan tablets. Consider re-initiation of macitentan tablets when hepatic enzyme levels normalize in patients who have not experienced clinical symptoms of hepatotoxicity. 5.3 Fluid Retention Peripheral edema and fluid retention are known clinical consequences of PAH and known effects of ERAs. In the placebo-controlled study of macitentan tablets in PAH, the incidence of edema was 21.9% in the macitentan tablets 10 mg group and 20.5% in the placebo group. Patients with underlying left ventricular dysfunction may be at particular risk for developing significant fluid retention after initiation of ERA treatment. In a small study of macitentan tablets in patients with pulmonary hypertension because of left ventricular dysfunction, more patients in the macitentan tablets group developed significant fluid retention and had more hospitalizations because of worsening heart failure compared to those randomized to placebo. Postmarketing cases of edema and fluid retention occurring within weeks of starting macitentan tablets, some requiring intervention with a diuretic or hospitalization for decompensated heart failure, have been reported [see Adverse Reactions (6.2)] . Monitor for signs of fluid retention after macitentan tablets initiation. If clinically significant fluid retention develops, evaluate the patient to determine the cause, such as macitentan tablets or underlying heart failure, and the possible need to discontinue macitentan tablets. 5.4 Hemoglobin Decrease Decreases in hemoglobin concentration and hematocrit have occurred following administration of other ERAs and were observed in clinical studies with macitentan tablets. These decreases occurred early and stabilized thereafter. In the placebo-controlled study of macitentan tablets in PAH, macitentan tablets 10 mg caused a mean decrease in hemoglobin from baseline to up to 18 months of about 1.0 g/dL compared to no change in the placebo group. A decrease in hemoglobin to below 10.0 g/dL was reported in 8.7% of the macitentan tablets 10 mg group and in 3.4% of the placebo group. Decreases in hemoglobin seldom require transfusion. Initiation of macitentan tablets is not recommended in patients with severe anemia. Measure hemoglobin prior to initiation of treatment and repeat during treatment as clinically indicated [see Adverse Reactions (6.1)] . 5.5 Pulmonary Edema with Pulmonary Veno-occlusive Disease (PVOD) Should signs of pulmonary edema occur, consider the possibility of associated PVOD. If confirmed, discontinue macitentan tablets. 5.6 Decreased Sperm Counts Macitentan tablets, like other ERAs, may have an adverse effect on spermatogenesis. Counsel men about potential effects on fertility [see Use in Specific Populations (8.3) and Nonclinical Toxicology (13.1)] .
Who should not 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)] .
Overdose — what happens if you take too much
Macitentan tablets has been administered as a single dose of up to and including 600 mg to healthy subjects (60 times the approved dosage). Adverse reactions of headache, nausea and vomiting were observed. In the event of an overdose, standard supportive measures should be taken, as required. Dialysis is unlikely to be effective because macitentan is highly protein-bound.
U.S. Poison Control: call or text 1-800-222-1222 (free, 24/7). In an emergency call 911. From the FDA label; not medical advice.
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 physiologically based pharmacokinetic (PBPK) modeling. Avoid concomitant use of macitentan with moderate dual inhibitors of CYP3A4 and CYP2C9 (such as fluconazole and amiodarone) [see Clinical Pharmacology (12.3)] . Concomitant treatment of both a moderate CYP3A4 inhibitor and moderate CYP2C9 inhibitor with macitentan should also be avoided [see Clinical Pharmacology (12.3)] .
How long does Macitentan stay in your body?
The elimination half-life of macitentan is about 16 hours (apparent elimination half-life) — the time it takes the body to clear about half of it. As a rule of thumb, a medicine is mostly gone after roughly 4 to 5 half-lives, though this varies from person to person with age and kidney or liver function. Macitentan has a longer-lasting ACTIVE metabolite that outlasts the parent: its apparent elimination half-life is approximately 48 hours (vs ~16 hours for macitentan itself). This metabolite matters clinically — at steady state in PAH patients its systemic exposure is about 3 times that of the parent and it contributes roughly 40% of total pharmacologic activity (it is about 20% as potent as the parent in vitro). Special populations: the label states no clinically relevant effect of age, sex, or race on the pharmacokinetics. Severe renal impairment (CrCl 15–29 mL/min) raises exposure to macitentan and its metabolite by ~30% and ~60% respectively; mild/moderate/severe hepatic impairment lowers exposure — in both cases the label deems the change not clinically relevant.
This is general information, not medical advice. It doesn’t tell you when a drug test would read negative (tests detect substances for different, often longer, windows) or when it’s safe to take another dose — ask your pharmacist or prescriber. Source: OPSUMIT (macitentan) FDA label — DailyMed.
Drug class
How this class works, per Bosentan - StatPearls - NCBI Bookshelf.
May treat (source: NIH RxClass)
See how Macitentan ranks — best-rated endothelin receptor antagonist for:
Dosage forms
Tablet
The forms currently marketed in the U.S., per the FDA National Drug Code Directory.
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Frequently asked questions
- What does Macitentan treat?
- Macitentan (Macitentan) may be used to treat pulmonary hypertension, based on NIH RxClass drug-classification data (conditions a drug may treat — not a verbatim copy of the FDA-approved label). This is general reference, not medical advice.
- How does Macitentan work?
- Macitentan is a 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.
- How is Macitentan rated?
- pharmaranks gives Macitentan a composite score of 3.3 out of 5, currently based on 1 weighted source (FDA regulatory recall-safety data weighted highest). See our methodology at /how-we-rate.
- Is there a coupon or discount for Macitentan?
- pharmaranks is an independent ratings site, not a pharmacy — we don't issue coupons or sell Macitentan. To pay less, Macitentan is already a generic — usually the lowest-cost version — so the main levers are comparing cash prices between pharmacies and using a pharmacy discount-card service. Prices vary by pharmacy, insurance, and location, so always confirm at the counter. This is general reference, not medical or financial advice.
- Who makes Macitentan?
- Macitentan is marketed by Torrent. You can see Torrent's full profile, rating, and other products on pharmaranks.
- Is Macitentan a brand-name or generic drug?
- Macitentan is a generic medication; its active ingredient is Macitentan. Generics contain the same active ingredient as the brand-name original and are usually lower cost.
- Is Macitentan available over the counter?
- No. Macitentan is a prescription (Rx) medication in the US — you need a prescription from a licensed clinician (in person or via telehealth); it isn't sold over the counter. For some conditions there are OTC alternatives — ask your pharmacist.
- What forms does Macitentan come in?
- Macitentan is currently marketed as tablet, per the FDA's National Drug Code Directory.
- What class of drug is Macitentan?
- Macitentan is classified as endothelin receptor antagonist, per the FDA's Established Pharmacologic Class.
- Is Macitentan FDA-registered?
- Macitentan is on record with the U.S. FDA under application number ANDA211107. You can verify this on its official FDA label.
- Has Macitentan been recalled by the FDA?
- Macitentan has no FDA recalls recorded under its own application in the openFDA enforcement database. Its recall-safety score reflects its manufacturer's overall recall record. This is general reference, not medical advice — check the FDA recall database for the latest alerts.
- Is Macitentan safe?
- There's no single safe-or-not verdict. pharmaranks gives Macitentan a recall-safety score of 66/100, based on its FDA recall history (no recalls under its own FDA application) — not an efficacy or side-effect rating. Review its FDA-label side effects and warnings before use, and always consult a licensed professional.
- What are the side effects of Macitentan?
- Macitentan's side effects are taken directly from its FDA label. From the label: 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… Both common and serious reactions are documented in full on this page. This is general reference from the FDA, not medical advice — always consult a professional.
Clinical content sourced from the FDA label via openFDA (U.S. FDA). View the FDA label on DailyMed → Provided for general reference only — not medical advice. Always consult a licensed professional and the current prescribing information.
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macitentan
66/100