Macitentan Olpha: Uses, Dosage & Side Effects
A dual endothelin receptor antagonist for the long-term treatment of pulmonary arterial hypertension (PAH) in adults – WHO functional class II to III
Macitentan Olpha is a prescription medication containing macitentan 10 mg, a dual endothelin receptor antagonist (ERA) used for the long-term treatment of pulmonary arterial hypertension (PAH) in adults classified as WHO functional class II to III. Macitentan works by blocking the action of endothelin-1, a potent vasoconstrictor and pro-proliferative peptide that plays a central role in the pathogenesis of PAH. By antagonizing both endothelin A (ETA) and endothelin B (ETB) receptors, macitentan reduces pulmonary vascular resistance, improves exercise capacity, and has been shown in the landmark SERAPHIN trial to significantly reduce the composite endpoint of disease progression, hospitalization for worsening PAH, and all-cause mortality. It is taken once daily as an oral film-coated tablet and can be used as monotherapy or in combination with other PAH-specific therapies, including phosphodiesterase-5 inhibitors.
Quick Facts: Macitentan Olpha
Key Takeaways
- Macitentan Olpha contains macitentan 10 mg, a dual endothelin receptor antagonist (ERA) that targets both ETA and ETB receptors to reduce pulmonary vascular resistance and improve hemodynamics in pulmonary arterial hypertension.
- The SERAPHIN trial (N=742) demonstrated that macitentan 10 mg significantly reduced the risk of disease progression, PAH-related hospitalization, and mortality by 45% compared to placebo, establishing it as a cornerstone therapy in PAH management.
- Macitentan is strictly contraindicated in pregnancy due to teratogenic effects; women of childbearing potential must use reliable contraception and undergo monthly pregnancy testing throughout treatment and for one month after discontinuation.
- Common side effects include headache, nasopharyngitis, anemia, and bronchitis; hemoglobin levels should be monitored regularly as clinically significant decreases may occur during treatment.
- Macitentan can be used as monotherapy or in combination with PDE-5 inhibitors (e.g., sildenafil, tadalafil) as part of guideline-recommended combination therapy for PAH, but co-administration with strong CYP3A4 inhibitors or inducers should be avoided.
What Is Macitentan Olpha and What Is It Used For?
Macitentan Olpha contains the active substance macitentan, a potent dual endothelin receptor antagonist (ERA) developed specifically for the treatment of pulmonary arterial hypertension (PAH). Macitentan belongs to a class of medications known as endothelin receptor antagonists, which work by blocking the biological effects of endothelin-1 (ET-1), a 21-amino acid peptide that is one of the most potent endogenous vasoconstrictors known. In PAH, circulating and pulmonary tissue concentrations of ET-1 are significantly elevated, and this peptide contributes to the characteristic pathological changes seen in the disease, including sustained vasoconstriction, smooth muscle cell proliferation, fibrosis, and inflammation of the pulmonary vasculature.
Pulmonary arterial hypertension is a progressive and debilitating condition characterized by increased blood pressure in the pulmonary arteries. The mean pulmonary arterial pressure at rest exceeds 20 mmHg (revised from the previous threshold of 25 mmHg in the 2022 ESC/ERS guidelines), with a pulmonary vascular resistance greater than 2 Wood Units and a normal pulmonary artery wedge pressure. This increased pressure places a significant burden on the right ventricle of the heart, which must work harder to pump blood through the narrowed and stiffened pulmonary vessels. Over time, this can lead to right ventricular hypertrophy, right heart failure, and ultimately death if the disease is not adequately treated.
The endothelin system plays a pivotal role in the pathogenesis of PAH. Endothelin-1 exerts its effects through two receptor subtypes: endothelin A (ETA) receptors and endothelin B (ETB) receptors. ETA receptors are located primarily on vascular smooth muscle cells and mediate vasoconstriction and cellular proliferation. ETB receptors are found on both endothelial cells and smooth muscle cells; on endothelial cells, ETB activation promotes the release of vasodilators such as nitric oxide and prostacyclin, while on smooth muscle cells, ETB activation contributes to vasoconstriction. In PAH, the balance between these receptor-mediated effects is disrupted, with a predominance of vasoconstriction and proliferation. Macitentan blocks both ETA and ETB receptors, thereby counteracting the pathological effects of elevated endothelin-1 in the pulmonary vasculature.
Macitentan was specifically designed with improved pharmacological properties compared to earlier endothelin receptor antagonists such as bosentan. It demonstrates sustained receptor binding, high tissue penetration, and an optimized pharmacokinetic profile that supports once-daily dosing. Unlike bosentan, macitentan exhibits slow receptor dissociation kinetics, meaning it remains bound to endothelin receptors for an extended period, providing prolonged pharmacological activity. This property is thought to contribute to the sustained clinical benefits observed in long-term use.
The efficacy of macitentan was definitively established in the SERAPHIN (Study with an Endothelin Receptor Antagonist in Pulmonary Arterial Hypertension to Improve CliNical Outcome) trial, a landmark, multinational, double-blind, placebo-controlled, event-driven phase III clinical trial that enrolled 742 patients with PAH across 151 centers in 39 countries. The primary endpoint was a composite of disease progression (worsening PAH, initiation of intravenous or subcutaneous prostanoid therapy, lung transplantation, atrial septostomy) or death from any cause. The trial demonstrated that macitentan 10 mg significantly reduced this composite endpoint by 45% compared with placebo (hazard ratio 0.55; 97.5% CI 0.39–0.76; p < 0.001). Notably, this benefit was observed both in treatment-naive patients and in those receiving background PAH therapy, supporting the use of macitentan in combination regimens.
In the SERAPHIN trial, macitentan 10 mg demonstrated: (1) a 45% reduction in the composite endpoint of morbidity and mortality, (2) significant improvement in 6-minute walk distance, (3) improvement in WHO functional class, and (4) sustained benefits in both monotherapy and combination therapy settings. These results established macitentan as a first-line oral therapy option for PAH in international guidelines.
What Should You Know Before Taking Macitentan Olpha?
Contraindications
Macitentan Olpha is contraindicated in several important clinical situations. Understanding these contraindications is essential for the safe use of the medication. The following patients must not take macitentan:
- Pregnancy: Macitentan is classified as a teratogen and is absolutely contraindicated during pregnancy. Animal studies have demonstrated severe developmental toxicities including cardiovascular malformations, mandibular and other craniofacial abnormalities, and thymic abnormalities at plasma exposures below the clinical dose. There are no adequate studies in pregnant women, and the potential risk to a developing fetus is considered unacceptable.
- Hypersensitivity: Patients with known hypersensitivity to macitentan, soy (the formulation contains lecithin derived from soya), or any of the other excipients should not use this medication.
- Severe hepatic impairment: Macitentan is extensively metabolized in the liver by cytochrome P450 enzymes. In patients with severe hepatic impairment (Child-Pugh Class C), the pharmacokinetics are significantly altered, and safety has not been established. Use in these patients is contraindicated.
- Baseline hepatic aminotransferases greater than 3 times ULN: Patients with significantly elevated liver enzymes at baseline should not initiate treatment with macitentan until values have been adequately investigated and resolved.
- Women of childbearing potential not using reliable contraception: Due to teratogenic risk, contraception must be established before starting treatment.
Warnings and Precautions
Macitentan causes birth defects and is strictly contraindicated during pregnancy. Before starting treatment, a negative pregnancy test must be confirmed. Women of childbearing potential must use two reliable methods of contraception during treatment and for at least one month after the last dose. Monthly pregnancy testing is mandatory throughout treatment. If pregnancy is suspected, discontinue macitentan immediately and consult your doctor.
Several important precautions should be observed before and during treatment with macitentan:
- Hepatotoxicity: Endothelin receptor antagonists as a class have been associated with liver injury. Although the incidence of hepatic aminotransferase elevations with macitentan was similar to placebo in the SERAPHIN trial, liver function tests (ALT and AST) should be obtained before initiating treatment. Periodic monitoring during treatment is recommended, particularly in patients with risk factors for hepatic dysfunction. If clinically relevant elevations of liver enzymes occur (sustained elevations > 3 times ULN or accompanied by signs or symptoms of liver injury), macitentan should be discontinued.
- Anemia and hemoglobin decrease: Treatment with macitentan is associated with a decrease in hemoglobin concentration, likely related to the mechanism of action of endothelin receptor antagonists. In the SERAPHIN trial, a hemoglobin decrease to below 10 g/dL was observed in approximately 8.7% of patients receiving macitentan 10 mg compared with 3.4% receiving placebo. Hemoglobin levels should be measured before treatment, after 1 month of treatment, and periodically thereafter. Macitentan is not recommended in patients with severe anemia, and treatment should not be initiated in patients with hemoglobin levels below 8 g/dL.
- Fluid retention and edema: PAH patients are predisposed to fluid retention, and endothelin receptor antagonists may cause or exacerbate peripheral edema. If clinically significant fluid retention develops, further evaluation is needed to determine the cause and whether specific treatment or discontinuation of macitentan is required.
- Pulmonary veno-occlusive disease (PVOD): If signs of pulmonary edema occur during treatment, the possibility of associated PVOD should be considered. If PVOD is confirmed, macitentan should be discontinued.
Pregnancy and Breastfeeding
Macitentan is absolutely contraindicated during pregnancy. All endothelin receptor antagonists are considered teratogenic based on preclinical data. The pregnancy prevention program for macitentan requires:
- A negative pregnancy test before initiation of treatment (within 3 days prior to the first dose)
- Use of at least one (preferably two) reliable methods of contraception during treatment
- Monthly pregnancy testing during treatment
- Continuation of contraception for at least one month after the last dose of macitentan
It is not known whether macitentan or its metabolites are excreted in human breast milk. In animal studies, macitentan and its active metabolite were detected in the milk of lactating rats. Given the potential risk to the nursing infant, breastfeeding is not recommended during treatment with macitentan. A decision must be made whether to discontinue breastfeeding or to discontinue the drug, taking into account the importance of the therapy for the mother.
Macitentan does not appear to have clinically significant effects on male fertility based on available preclinical data. However, the effects on human fertility have not been formally studied in controlled clinical trials.
How Does Macitentan Olpha Interact with Other Drugs?
Macitentan is primarily metabolized by cytochrome P450 3A4 (CYP3A4) and, to a lesser extent, by CYP2C19. Its active metabolite, ACT-132577, also contributes to the pharmacological effect. Because of this metabolic pathway, drugs that significantly alter CYP3A4 activity can affect the plasma concentrations and therapeutic efficacy of macitentan. Understanding these interactions is essential for safe and effective PAH treatment.
Major Interactions
| Interacting Drug | Mechanism | Effect | Recommendation |
|---|---|---|---|
| Ketoconazole | Strong CYP3A4 inhibitor | Approximately 2-fold increase in macitentan exposure | Avoid co-administration |
| Ritonavir | Strong CYP3A4 inhibitor | Significantly increased macitentan levels | Avoid co-administration |
| Rifampicin | Strong CYP3A4 inducer | Approximately 79% reduction in macitentan exposure | Avoid co-administration |
| Carbamazepine, Phenytoin | Strong CYP3A4 inducers | Significantly reduced macitentan levels | Avoid co-administration |
| St. John’s Wort | Strong CYP3A4 inducer | Unpredictable reduction in macitentan exposure | Do not use together |
Minor Interactions and Co-administered Medications
| Interacting Drug | Mechanism | Effect | Recommendation |
|---|---|---|---|
| Sildenafil | PDE-5 inhibitor (PAH therapy) | No clinically relevant interaction | Safe to combine; commonly used together |
| Tadalafil | PDE-5 inhibitor (PAH therapy) | No clinically relevant interaction | Safe to combine |
| Warfarin | CYP2C9 substrate | No significant effect on INR | No dose adjustment; monitor INR as standard practice |
| Cyclosporine A | CYP3A4 and P-gp inhibitor | Modest increase in macitentan exposure | Monitor; no dose adjustment typically required |
| Hormonal contraceptives | No known interaction | No effect on contraceptive efficacy | Safe to use; essential for pregnancy prevention |
Unlike bosentan, macitentan does not induce CYP3A4 or CYP2C9, meaning it is not expected to reduce the plasma concentrations of drugs metabolized by these enzymes. This is a clinically important distinction, as bosentan is known to reduce the efficacy of hormonal contraceptives and warfarin through enzyme induction. Macitentan does not share this interaction profile, which simplifies co-medication management in clinical practice.
Macitentan is neither a substrate nor an inhibitor of clinically relevant drug transporters including P-glycoprotein (P-gp) and organic anion transporting polypeptides (OATPs) at therapeutic concentrations. Therefore, transporter-mediated drug interactions are not expected to be clinically significant.
What Is the Correct Dosage of Macitentan Olpha?
Adults
Standard Adult Dosage
The recommended dose is 10 mg once daily, taken orally with or without food. The tablet should be swallowed whole. Treatment should be initiated and supervised by a physician experienced in the management of pulmonary arterial hypertension. The same dose applies whether macitentan is used as monotherapy or in combination with other PAH-specific therapies.
Macitentan has a straightforward dosing regimen that does not require titration. The fixed dose of 10 mg once daily was established based on the results of the SERAPHIN trial, where this dose provided the optimal balance of efficacy and safety. A lower dose of 3 mg was also studied in the trial but did not achieve statistical significance for the primary composite morbidity/mortality endpoint, supporting the use of the 10 mg dose as the standard therapeutic dose.
The tablet can be taken at any time of day, although consistent timing is recommended to maintain steady-state plasma concentrations. Food does not significantly affect the absorption of macitentan, so it can be taken with or without meals. If a dose is missed, it should be taken as soon as remembered; however, if it is close to the time of the next dose, the missed dose should be skipped. The dose should not be doubled to compensate for a missed dose.
Children and Adolescents
Pediatric Use
The safety and efficacy of macitentan in children and adolescents below 18 years of age have not been established. No data are available. Use in this population is therefore not recommended until adequate clinical studies have been conducted.
Elderly Patients
Dosage in Elderly Patients
No dose adjustment is required in elderly patients. Clinical experience in patients over 75 years of age is limited, and macitentan should be used with caution in this age group. Age-related changes in hepatic and renal function should be taken into account during monitoring.
Renal impairment: No dose adjustment is necessary in patients with renal impairment, including those with severely reduced renal function. However, there is no clinical experience with macitentan in PAH patients undergoing dialysis. As macitentan and its active metabolite are highly protein-bound, they are unlikely to be removed by dialysis.
Hepatic impairment: No dose adjustment is required in patients with mild or moderate hepatic impairment (Child-Pugh Class A or B). However, macitentan exposure is increased in patients with hepatic impairment, and caution is advised in those with moderate impairment. Macitentan is contraindicated in patients with severe hepatic impairment (Child-Pugh Class C) and in patients with baseline aminotransferases > 3 times the upper limit of normal.
Missed Dose
If you miss a dose of Macitentan Olpha, take it as soon as you remember on the same day. If you do not remember until the next day, skip the missed dose and take the next dose at the regular scheduled time. Do not take a double dose to make up for a missed one. Consistent daily dosing is important to maintain therapeutic drug levels and optimal disease management. If you frequently forget to take your medication, discuss strategies with your healthcare provider, such as setting a daily alarm or using a pill organizer.
Overdose
In clinical studies, single doses of macitentan up to 600 mg have been administered to healthy subjects. The most commonly observed adverse effects were headache, nausea, and vomiting. In the event of an overdose, standard supportive measures should be instituted as needed. Due to the high protein binding of macitentan and its active metabolite (approximately 99%), dialysis is unlikely to be effective in removing the drug from the systemic circulation. There is no specific antidote for macitentan overdose. If overdose is suspected, contact your local poison control center or seek emergency medical attention immediately.
What Are the Side Effects of Macitentan Olpha?
Like all medicines, Macitentan Olpha can cause side effects, although not everybody gets them. The side effects of macitentan have been well characterized in clinical trials, most notably the SERAPHIN trial and its long-term extension study. The side effect profile reflects both the pharmacological action of the drug on the endothelin system and the underlying disease being treated. The following categorization is based on frequency data from clinical studies and post-marketing surveillance.
Very Common
Affects more than 1 in 10 patients
- Headache
- Nasopharyngitis (common cold symptoms, sore throat)
- Anemia / decreased hemoglobin
Common
Affects 1 in 10 to 1 in 100 patients
- Bronchitis (inflammation of the airways)
- Pharyngitis (sore throat)
- Urinary tract infection
- Influenza (flu)
- Peripheral edema (swelling of ankles and feet)
- Hypotension (low blood pressure)
- Nasal congestion
Uncommon
Affects 1 in 100 to 1 in 1,000 patients
- Elevated hepatic aminotransferases (ALT/AST > 3 × ULN)
- Hepatitis
- Leukopenia (low white blood cell count)
- Thrombocytopenia (low platelet count)
- Hypersensitivity reactions (rash, pruritus, angioedema)
Rare
Affects fewer than 1 in 1,000 patients
- Severe hepatic injury
- Anaphylaxis
- Severe anemia requiring transfusion
Contact your healthcare provider immediately if you experience: yellowing of the skin or eyes (jaundice), dark urine, persistent nausea or vomiting, upper right abdominal pain (signs of liver injury), unusual tiredness or weakness with pale skin (signs of severe anemia), sudden weight gain or increasing swelling of the ankles and legs (worsening fluid retention), or difficulty breathing that is new or worsening.
The anemia associated with macitentan deserves particular attention. The mechanism is thought to be related to the dual blockade of endothelin receptors, which may affect erythropoiesis. In the SERAPHIN trial, a decrease in hemoglobin to below 10 g/dL was reported in 8.7% of patients receiving macitentan 10 mg versus 3.4% on placebo. A decrease below 8 g/dL was observed in 3.4% versus 0.4%. Most cases were mild to moderate and did not require treatment discontinuation, but some patients required iron supplementation or erythropoiesis-stimulating agents. Regular monitoring of hemoglobin levels is essential, particularly during the first few months of treatment.
Regarding hepatic safety, while the earlier ERA bosentan was associated with a significant rate of clinically relevant liver enzyme elevations (requiring monthly monitoring), macitentan showed a much more favorable hepatic safety profile in the SERAPHIN trial. The incidence of aminotransferase elevations > 3 times the upper limit of normal was 3.4% with macitentan 10 mg compared with 4.5% with placebo, suggesting that the liver enzyme changes were not attributable to the drug. Nevertheless, baseline liver function tests are recommended, and periodic monitoring is prudent, particularly in patients with hepatic risk factors.
Peripheral edema and fluid retention may occur or worsen during treatment with macitentan, as is common with all endothelin receptor antagonists and indeed with the natural progression of PAH itself. Patients should be counseled to monitor for increasing swelling of the ankles and legs, sudden weight gain, and increasing shortness of breath, all of which should be reported promptly to their healthcare provider.
How Should You Store Macitentan Olpha?
Proper storage of Macitentan Olpha is important to maintain the quality, safety, and efficacy of the medication throughout its shelf life. The following storage conditions should be observed:
- Temperature: Store at room temperature, not exceeding 30°C (86°F). Do not refrigerate or freeze the medication.
- Moisture protection: Keep the tablets in the original packaging (blister pack) to protect from moisture. Do not remove tablets from the blister until ready to take them.
- Light protection: While no specific light protection requirements are stated, storing in the original packaging provides adequate protection.
- Child safety: Keep out of the sight and reach of children. The packaging should not be left accessible, as accidental ingestion by children could be extremely dangerous given the teratogenic properties of the drug.
- Expiry date: Do not use Macitentan Olpha after the expiry date stated on the carton and blister. The expiry date refers to the last day of that month.
Do not dispose of medications via wastewater or household waste. Ask your pharmacist about proper disposal methods for medications you no longer use. Proper disposal helps protect the environment and prevents accidental exposure to others.
What Does Macitentan Olpha Contain?
Each Macitentan Olpha film-coated tablet contains the following:
Active substance: Macitentan 10 mg per tablet.
Excipients (inactive ingredients): The tablet core typically contains lactose monohydrate, microcrystalline cellulose, sodium starch glycolate, povidone, magnesium stearate, and polysorbate 80. The film coating contains polyvinyl alcohol, titanium dioxide (E171), talc, soy lecithin (E322), and xanthan gum. The exact composition may vary slightly between manufacturers.
Appearance: Macitentan Olpha tablets are white to off-white, round, biconvex, film-coated tablets.
The film coating of Macitentan Olpha tablets contains soy lecithin (E322). If you are allergic to soya or peanuts, do not use this medication. Inform your healthcare provider of any known allergies before starting treatment.
Macitentan is a sulfonamide-derived compound with the chemical name N-[5-(4-Bromophenyl)-6-{2-[(5-bromopyrimidin-2-yl)oxy]ethoxy}pyrimidin-4-yl]-N'-propylsulfamide. It has a molecular weight of 588.27 g/mol and is practically insoluble in water. The compound is a white to yellowish powder in its pure form.
Frequently Asked Questions About Macitentan Olpha
Macitentan Olpha is used for the long-term treatment of pulmonary arterial hypertension (PAH) in adult patients classified as WHO functional class II to III. PAH is a serious condition where the blood pressure in the arteries of the lungs is abnormally high, making the heart work harder to pump blood through the lungs. Macitentan helps by blocking the action of endothelin-1, a substance that causes narrowing and thickening of the blood vessels in the lungs. By blocking this substance, macitentan relaxes the pulmonary blood vessels, reduces the workload on the heart, and improves exercise capacity and disease outcomes.
No, absolutely not. Macitentan is classified as teratogenic, meaning it can cause severe birth defects. It is strictly contraindicated during pregnancy. Women of childbearing potential must have a confirmed negative pregnancy test before starting treatment, use reliable contraception (two methods recommended) during treatment, undergo monthly pregnancy testing throughout the treatment period, and continue contraception for at least one month after stopping the medication. If you become pregnant while taking macitentan, stop the medication immediately and contact your doctor.
The most commonly reported side effects of macitentan include headache, nasopharyngitis (cold-like symptoms), anemia (decreased hemoglobin levels), bronchitis, urinary tract infections, and pharyngitis. Anemia is an important side effect to watch for, as hemoglobin levels can decrease significantly during treatment. Your doctor will monitor your blood counts regularly. Most side effects are mild to moderate in severity and are manageable with appropriate supportive care. If you experience any severe or persistent symptoms, contact your healthcare provider promptly.
Both macitentan and bosentan are dual endothelin receptor antagonists, but macitentan represents a newer generation with several pharmacological advantages. Macitentan has sustained receptor binding with slow dissociation kinetics, meaning it remains active at the receptor for longer. It has improved tissue penetration, particularly in the lungs. Unlike bosentan, macitentan does not induce CYP enzymes, so it has fewer drug interactions and does not reduce the effectiveness of hormonal contraceptives. Macitentan also showed a more favorable hepatic safety profile in clinical trials, with liver enzyme elevations comparable to placebo. The SERAPHIN trial provided robust morbidity and mortality data for macitentan, which was not available for bosentan at the time of its approval.
Yes. Macitentan can be used as part of combination therapy, which is now the standard approach for managing many PAH patients according to current ESC/ERS guidelines. In the SERAPHIN trial, approximately 64% of patients were on background PAH therapy when they started macitentan, and the benefit of macitentan was maintained in this population. Commonly used combinations include macitentan with phosphodiesterase-5 (PDE-5) inhibitors such as sildenafil or tadalafil. Triple combination therapy with macitentan, a PDE-5 inhibitor, and a prostacyclin pathway agent may be used in more severe cases. Your doctor will determine the most appropriate combination based on your disease severity and treatment response.
Macitentan is intended for long-term, ongoing treatment. PAH is a chronic, progressive disease, and stopping treatment can lead to deterioration. In the SERAPHIN trial, the average treatment duration was approximately 2 years, and long-term extension studies have followed patients for over 5 years with sustained benefit. Treatment should continue for as long as the patient is deriving clinical benefit and tolerating the medication. Your doctor will regularly assess your response to treatment through exercise testing, echocardiography, and other evaluations. Do not stop taking macitentan without consulting your healthcare provider, as abrupt discontinuation may worsen your condition.
References
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