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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Brand Name
Selexipag
Generic Name
Selexipag
Active Ingredient
SelexipagCategory
Prostacyclin Receptor Agonist [EPC]
Variants
16
Different strengths and dosage forms
| Strength | Form | Route | NDC |
|---|---|---|---|
| 600 ug/1 | TABLET, FILM COATED | ORAL | 70771-1795 |
| 1200 ug/1 | TABLET, FILM COATED | ORAL | 70771-1798 |
| 600 ug/1 | TABLET, FILM COATED | ORAL |
This page is for informational purposes only and does not replace medical advice. Before using any prescription or over-the-counter medication for Selexipag, you must consult a qualified healthcare professional.
| 1600 ug/1 | TABLET, FILM COATED | ORAL | 70771-1800 |
| 200 ug/1 | TABLET, FILM COATED | ORAL | 70710-1551 |
| 1200 ug/1 | TABLET, FILM COATED | ORAL | 70710-1556 |
| 1400 ug/1 | TABLET, FILM COATED | ORAL | 70710-1557 |
| 1400 ug/1 | TABLET, FILM COATED | ORAL | 70771-1799 |
| 800 ug/1 | TABLET, FILM COATED | ORAL | 70710-1554 |
| 800 ug/1 | TABLET, FILM COATED | ORAL | 70771-1796 |
| 1600 ug/1 | TABLET, FILM COATED | ORAL | 70710-1558 |
| 200 ug/1 | TABLET, FILM COATED | ORAL | 70771-1793 |
+ 4 more variants
Detailed information about Selexipag
Selexipag is a selective prostacyclin IP receptor agonist indicated for the treatment of pulmonary arterial hypertension (PAH) to delay disease progression and reduce the risk of hospitalization.
The dosing of Selexipag is highly individualized and follows a strict titration (gradual increase) schedule to ensure the patient reaches the highest dose they can tolerate without excessive side effects.
According to the FDA-approved labeling, the recommended starting dose is 200 mcg taken twice daily (BID). This initial phase allows the body to adjust to the medication's vasodilatory effects.
Healthcare providers typically instruct patients to increase the dose in increments of 200 mcg BID, usually at weekly intervals. For example, after one week at 200 mcg BID, the dose may be increased to 400 mcg BID, then 600 mcg BID the following week, and so on. This continues until the patient reaches their 'highest tolerated dose' or the maximum dose of 1600 mcg twice daily. If a patient experiences intolerable side effects (such as severe headache or jaw pain) at a certain level, the dose is usually decreased to the previous tolerated level.
The maintenance dose is the highest dose the patient tolerated during the titration phase. Patients should continue this dose consistently to maintain the therapeutic effect on the pulmonary vasculature.
As of 2026, the safety and effectiveness of Selexipag in pediatric patients (under the age of 18) have not been established. Clinical trials in children are ongoing, but currently, Selexipag is not FDA-approved for use in the pediatric population. Healthcare providers may occasionally use it off-label in specialized pediatric centers, but this is not standard practice and requires extreme caution.
For patients with mild or moderate renal impairment (kidney dysfunction), no adjustment to the starting dose is generally required. However, there is limited clinical data regarding the use of Selexipag in patients with severe renal impairment (estimated glomerular filtration rate < 30 mL/min/1.73 m²). In these cases, titration should be performed with extra caution.
Clinical studies did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function.
Selexipag should be taken twice daily, ideally in the morning and evening.
If a dose of Selexipag is missed, it should be taken as soon as possible unless the next scheduled dose is within the next 6 hours. If it is within 6 hours of the next dose, the missed dose should be skipped, and the regular schedule should be resumed. Patients should never take two doses at once to make up for a missed one. If treatment is missed for 3 days or more, patients should contact their doctor, as the dose may need to be restarted at a lower level and re-titrated.
Signs of a Selexipag overdose are typically exaggerations of its known side effects, including severe headache, nausea, vomiting, diarrhea, and a significant drop in blood pressure (hypotension). If an overdose is suspected, seek emergency medical attention immediately. There is no specific antidote for Selexipag; treatment is supportive and focused on maintaining blood pressure and hydration.
> Important: Follow your healthcare provider's dosing instructions exactly. Do not adjust your dose or stop taking Selexipag without medical guidance, as sudden discontinuation can lead to a worsening of PAH symptoms.
Because Selexipag works by dilating blood vessels throughout the body, not just in the lungs, it commonly causes 'prostacyclin-type' side effects. These are most frequent during the titration phase as the body adjusts to the medication. According to data from the GRIPHON trial (2015), the most common adverse reactions include:
Selexipag is a potent vasodilator and must be used with caution, particularly during the initiation and titration phases. Patients should be aware that while the drug is effective at delaying disease progression, it is not a cure for PAH. It requires strict adherence to the twice-daily schedule and regular follow-up appointments with a pulmonary hypertension specialist. Patients should also be warned about the risk of Pulmonary Veno-Occlusive Disease (PVOD), a rare but serious condition where the small veins in the lungs become blocked. If signs of pulmonary edema occur, the drug must be stopped immediately.
No FDA black box warnings for Selexipag. However, this does not mean the drug is without risk; it simply means the FDA has not identified a single catastrophic risk that requires the highest level of boxed warning. Standard precautions and monitoring remain mandatory.
There are specific circumstances where the risks of Selexipag clearly outweigh any potential benefits. In these cases, the drug must never be used:
Selexipag is classified as having limited data regarding its use in pregnant women. Animal studies (in rats and rabbits) using doses much higher than the human therapeutic dose did not show evidence of fetal harm or teratogenicity (birth defects). However, because animal studies are not always predictive of human response, Selexipag should only be used during pregnancy if the potential benefit to the mother outweighs the potential risk to the fetus. It is important to note that untreated PAH poses a significant risk of maternal and fetal mortality. There is no specific data regarding its use in fertility treatments.
It is not known whether Selexipag or its metabolites are excreted in human milk. In animal studies, the drug was found to be present in the milk of lactating rats. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants (such as hypotension or GI distress), a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Selexipag is not approved for use in children under 18 years of age. The safety and efficacy in this population have not been established. Growth effects have not been specifically studied, but the drug's mechanism does not suggest a direct impact on bone growth. Pediatric PAH is a complex condition, and treatment usually involves other approved therapies like Sildenafil or Bosentan.
Selexipag is a selective, non-prostanoid agonist of the prostacyclin (IP) receptor. Unlike prostacyclin analogs which can bind to multiple prostanoid receptors (EP1-4, DP, TP, and FP), Selexipag is highly specific for the IP receptor.
Common questions about Selexipag
Selexipag is primarily used for the treatment of Pulmonary Arterial Hypertension (PAH), specifically WHO Group 1. It is prescribed to help delay the progression of the disease and reduce the risk of being hospitalized due to PAH-related complications. By targeting the prostacyclin pathway, it helps to relax and widen the blood vessels in the lungs, which lowers the blood pressure that the heart must pump against. It is often used in combination with other PAH medications to provide a comprehensive approach to managing the condition. Patients in WHO Functional Classes II through IV are the typical candidates for this therapy.
The most common side effects of Selexipag are related to its action as a vasodilator and are often referred to as 'prostacyclin-like' effects. These include headache, which affects over half of all patients, as well as diarrhea, jaw pain, nausea, and vomiting. Some patients also experience muscle or joint pain and facial flushing. These symptoms are usually most intense during the titration phase when the dose is being increased. Most patients find that these side effects become more manageable over time or can be controlled with simple over-the-counter remedies and by taking the medication with food.
While there is no direct chemical interaction between alcohol and Selexipag, caution is highly recommended. Alcohol acts as a vasodilator, which means it can widen blood vessels and lower blood pressure, similar to the effects of Selexipag. Combining the two may lead to an additive effect, increasing the likelihood of feeling dizzy, lightheaded, or even fainting. Furthermore, alcohol can worsen the flushing and headaches already associated with the medication. It is best to discuss your alcohol consumption with your healthcare provider to determine what is safe for your specific cardiovascular health.
The safety of Selexipag during pregnancy has not been definitively established in humans, as there is limited clinical data. Animal studies have not shown a high risk of birth defects, but these results do not always translate perfectly to human pregnancies. Because pulmonary arterial hypertension itself carries a very high risk of complications for both the mother and the baby, the decision to use Selexipag must be made carefully by a specialist. If you are pregnant or planning to become pregnant, you must discuss the risks and benefits of all your PAH medications with your doctor. Breastfeeding is generally not recommended while taking this drug because it is unknown if it passes into breast milk.
Selexipag does not provide immediate symptom relief; rather, it works gradually over several weeks and months. The full therapeutic benefit is usually not seen until a patient has completed the titration phase and reached their stable maintenance dose, which typically takes 8 to 12 weeks. Clinical trials, such as the GRIPHON study, measured the drug's effectiveness over long periods, showing a significant reduction in disease progression over several years of treatment. Patients should continue taking the medication even if they do not feel an immediate difference in their breathing or energy levels. Consistent use is key to preventing the long-term worsening of PAH.
No, you should never stop taking Selexipag suddenly unless specifically instructed to do so by your healthcare provider in an emergency. Abruptly discontinuing prostacyclin-pathway medications can cause a sudden and severe increase in pulmonary artery pressure, known as 'rebound pulmonary hypertension.' This can lead to a rapid worsening of symptoms, heart failure, or even death. If you need to stop the medication due to side effects or other medical reasons, your doctor will provide a schedule to gradually taper the dose. Always ensure you have an adequate supply of the medication and do not wait until you are completely out to request a refill.
If you miss a dose of Selexipag, you should take it as soon as you remember, provided that your next scheduled dose is more than 6 hours away. If your next dose is due in less than 6 hours, skip the missed dose entirely and return to your regular twice-daily schedule. Do not take two doses at the same time to make up for the one you missed, as this increases the risk of severe side effects like low blood pressure and intense headache. If you miss your medication for more than three days in a row, you must contact your doctor before restarting, as you may need to begin again at a lower dose and re-titrate.
Weight gain is not a commonly reported direct side effect of Selexipag. In fact, some patients may experience a decrease in appetite or weight loss due to gastrointestinal side effects like nausea or diarrhea. However, patients with pulmonary arterial hypertension should monitor their weight closely for other reasons. Rapid weight gain (such as 3-5 pounds in a single week) can be a sign of fluid retention and worsening heart failure, rather than a side effect of the drug itself. If you notice sudden swelling in your ankles or an increase in your weight, you should notify your healthcare provider immediately to check your heart and lung function.
Selexipag is frequently taken in combination with other PAH medications, such as sildenafil (a PDE-5 inhibitor) or macitentan (an ERA), and this 'triple therapy' is often very effective. However, it can have dangerous interactions with other types of drugs. Specifically, it must never be taken with gemfibrozil, a cholesterol medication, because it can cause Selexipag levels to rise to toxic levels. It may also interact with blood thinners and certain antibiotics like rifampin. Because of these risks, it is vital that you provide your doctor and pharmacist with a complete list of every medication, supplement, and herbal product you are currently taking.
As of 2026, Selexipag is primarily available as the brand-name medication Uptravi. While the initial patents for the compound have begun to expire in some regions, widespread generic availability may still be limited depending on your country's patent laws and the specific orange book listings. Generic versions must undergo rigorous FDA testing to prove they are bioequivalent to the brand-name drug, meaning they work in the exact same way and have the same safety profile. Patients should check with their insurance provider and specialty pharmacy for the most current information regarding the availability of a lower-cost generic version of Selexipag.
Other drugs with the same active ingredient (Selexipag)
While most side effects of Selexipag are manageable, some require urgent medical evaluation.
> Warning: Stop taking Selexipag and call your doctor immediately if you experience any of these:
Long-term use of Selexipag is generally well-tolerated once the maintenance dose is established. However, chronic prostacyclin stimulation can lead to persistent mild GI issues or a slight, stable reduction in hemoglobin levels. There is no evidence currently suggesting that Selexipag causes long-term organ damage to the liver or kidneys, provided it is used as directed and monitored by a specialist.
As of the current 2026 clinical guidelines, there are no FDA black box warnings for Selexipag. Unlike some other PAH medications (like ERAs), Selexipag does not have a REMS (Risk Evaluation and Mitigation Strategy) program for hepatotoxicity or teratogenicity, though precautions regarding pregnancy still apply.
Report any unusual symptoms to your healthcare provider. Many side effects can be managed by adjusting the titration schedule or using supportive medications, rather than stopping the drug entirely.
To ensure the safe use of Selexipag, healthcare providers typically require the following monitoring:
Selexipag may cause dizziness or headaches, particularly during the titration phase. Patients should determine how they react to the medication before driving or operating heavy machinery. If you feel lightheaded or have a severe headache, avoid these activities until the symptoms resolve.
There is no direct chemical interaction between Selexipag and alcohol. However, alcohol is a vasodilator and can lower blood pressure. Combining alcohol with Selexipag may increase the risk of dizziness, fainting, or flushing. It is generally recommended to limit alcohol consumption while taking this medication.
Abruptly stopping Selexipag can lead to a 'rebound' effect, where pulmonary blood pressure rises rapidly, potentially leading to a life-threatening crisis. If the drug must be stopped, it should ideally be tapered down under strict medical supervision. If you run out of medication, contact your specialty pharmacy or doctor immediately to ensure you do not miss doses.
> Important: Discuss all your medical conditions, including any history of liver disease, thyroid problems, or anemia, with your healthcare provider before starting Selexipag.
Selexipag is not known to interfere with common laboratory tests, such as glucose, electrolytes, or basic metabolic panels. However, it does cause a physiological decrease in hemoglobin, which will be reflected in a Complete Blood Count (CBC). It may also affect thyroid function tests (TSH, T3, T4).
For each major interaction, the mechanism usually involves the CYP2C8 enzyme system. Inhibition of this enzyme leads to toxic accumulation, while induction leads to therapeutic failure. Management strategies always involve either avoiding the combination or performing more frequent clinical monitoring and dose adjustments.
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking, including over-the-counter pain relievers and vitamins.
There is no known cross-sensitivity between Selexipag and other classes of PAH medications, such as endothelin receptor antagonists or PDE-5 inhibitors. However, patients who have had severe adverse reactions to other prostacyclin analogs (like Epoprostenol or Treprostinil) should be monitored closely, as they may be more sensitive to the systemic vasodilatory effects of Selexipag.
> Important: Your healthcare provider will evaluate your complete medical history, including liver function and current medications, before prescribing Selexipag.
In the GRIPHON clinical trial, 19% of patients were 65 years of age or older. No overall differences in safety or effectiveness were observed between these patients and younger patients. However, geriatric patients are more likely to have decreased hepatic or renal function and may be taking multiple other medications (polypharmacy). This increases the risk of drug interactions and side effects like dizziness, which could lead to falls. Dose titration in the elderly should be slow and cautious.
> Important: Special populations require individualized medical assessment and more frequent monitoring by a healthcare team.
Selexipag produces a dose-dependent increase in cardiac index and a decrease in pulmonary vascular resistance (PVR). The onset of effect is gradual, with significant improvements in hemodynamics typically observed after the maintenance dose is reached (usually 4-12 weeks). Unlike some other vasodilators, Selexipag does not typically cause significant 'rebound' hypertension if a single dose is missed, but chronic tolerance (loss of effect) has not been a major issue in long-term clinical trials.
| Parameter | Value |
|---|---|
| Bioavailability | ~49% |
| Protein Binding | ~99% (Albumin and AAG) |
| Half-life | 0.8–2.5h (Parent), 6.2–13.5h (Metabolite) |
| Tmax | 1–3h (Parent), 3–4h (Metabolite) |
| Metabolism | Hepatic (CE1, CYP2C8, CYP3A4) |
| Excretion | Fecal (93%), Renal (12%) |
Selexipag is classified as a Prostacyclin Receptor Agonist [EPC]. It is the first and currently only drug in the non-prostanoid IP receptor agonist class. It is grouped therapeutically with other PAH treatments like Endothelin Receptor Antagonists (e.g., Macitentan) and Soluble Guanylate Cyclase Stimulators (e.g., Riociguat).