Adempas (riociguat)
An approved treatment for Pulmonary Arterial Hypertension.
The same compound appears under different names depending on the context. Here is how to identify Riociguat wherever you encounter it, plus the key facts at a glance.
- Generic name
- Riociguat
- Brand name
- Adempas
- Development code
- BAY 63-2521
- Drug class
- Soluble guanylate cyclase stimulator
- Manufacturer
- Bayer
- How it's taken
- Taken orally 3 times daily, with or without food.
The first and only approved treatment for chronic thromboembolic pulmonary hypertension (CTEPH), and also approved for PAH. It is approved for adults only; it has not been shown to be safe and effective in children. Adempas works through a unique mechanism targeting the nitric oxide pathway to relax lung blood vessels.
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Where Riociguat fits
Unique PAH therapy that stimulates the NO-sGC-cGMP pathway through a different mechanism than PDE5 inhibitors. The only approved oral therapy for CTEPH.
How Riociguat works
In PAH, the nitric oxide signaling pathway is impaired. Normally, nitric oxide activates an enzyme called soluble guanylate cyclase (sGC), which produces cGMP to relax blood vessel walls.
Riociguat works in two ways: it makes sGC more sensitive to whatever nitric oxide is available, and it can also directly stimulate sGC even without nitric oxide. The result is increased cGMP, which relaxes and widens pulmonary blood vessels.
Mechanism: Soluble guanylate cyclase (sGC) stimulator that enhances the nitric oxide signaling pathway to dilate pulmonary blood vessels
Side effects and safety
Carries a black box warning for embryo-fetal toxicity (must not be used in pregnancy). Common side effects include headache, dizziness, indigestion, nausea, diarrhea, and low blood pressure. Must not be used with PDE5 inhibitors (sildenafil, tadalafil, vardenafil) or nonspecific PDE inhibitors such as dipyridamole or theophylline, with nitrates or nitric oxide donors, or with other sGC stimulators, and must not be used in pulmonary hypertension caused by idiopathic interstitial pneumonias. Women who can become pregnant need effective birth control before, during and for 1 month after treatment. The label also warns about serious bleeding, including coughing up blood (1 case in trials was fatal), and about fluid in the lungs in people with pulmonary veno-occlusive disease.
This is not a complete list of side effects. Talk to your doctor or pharmacist about what to expect and when to seek medical attention.
Taking Riociguat
Taken orally 3 times daily, with or without food. Tablets can be crushed and mixed with water or soft food such as applesauce for people who have trouble swallowing. Starting dose is 1 mg 3 times daily, gradually increased to a maximum of 2.5 mg 3 times daily based on blood pressure tolerance. Requires negative pregnancy testing.
Availability and cost
Generic versions may be available at a lower cost. Ask your pharmacist.
First-in-class soluble guanylate cyclase stimulator, the only oral therapy approved for both PAH and chronic thromboembolic pulmonary hypertension (CTEPH). Unique dual indication.
Help paying for Adempas
Pick your insurance to see which help fits. Drugmaker copay cards can't be used with Medicare, Medicaid or TRICARE; charity funds are the usual route there.
- Copay help
With private or commercial insurance you may pay as little as $0. Annual cap; re-apply yearly; not for Medicare or Medicaid.
For: private insurance · source - Free medicine program
The Bayer US Patient Assistance Foundation may provide Bayer medicines at no cost to eligible patients. Call 1-866-228-7723.
The official page does not say who qualifies. Ask the program. · source - Other support
Aim Nursing Support, including possible at-home nurse visits to help with dose adjustment if your doctor agrees.
For: private insurance, Medicare, Medicaid, TRICARE, no insurance, underinsured · source
Good to know: Adempas is sold by Bayer in the US. The foundation is at patientassistance.bayer.us; its eligibility rules are not stated on the official page.
- From a charity · HealthWell FoundationPulmonary Hypertension (Medicare Access) fundOpen
Pays for: Copays, premiums or other treatment costs. Medicare patients only.
- From a charity · TotalAssist (formerly PAN Foundation)Pulmonary Hypertension fundOpen
Pays for: Out-of-pocket costs for approved medications, up to $9,500 per year. Requires health insurance (any kind).
- From a charity · The Assistance FundPulmonary Hypertension fundWaitlist
Pays for: Copays, coinsurance, deductibles and other health-related expenses.
The foundation says: “WAITLIST — Accepting Waitlist Patients. TAF is currently accepting requests to join the enrollment waitlist for this program. Waitlists a…”
Clinical trial results
PATENT-1 (PAH): significant improvement in 6-minute walk distance and pulmonary vascular resistance. CHEST-1 (CTEPH): first drug to show benefit in inoperable CTEPH patients, with a 46-meter improvement in walk distance versus placebo.
Development history
Developed by Bayer. Approved October 2013 for PAH and CTEPH, making it the first drug approved for CTEPH. Represents a first-in-class mechanism (sGC stimulation) distinct from the endothelin and prostacyclin pathways used by other PAH drugs.
Explore Pulmonary Arterial Hypertension trials
Other Pulmonary Arterial Hypertension treatments
Common questions about Riociguat
▸What is Riociguat (Adempas)?
The first and only approved treatment for chronic thromboembolic pulmonary hypertension (CTEPH), and also approved for PAH. It is approved for adults only; it has not been shown to be safe and effective in children. Adempas works through a unique mechanism targeting the nitric oxide pathway to relax lung blood vessels.
▸How does Riociguat work?
In PAH, the nitric oxide signaling pathway is impaired. Normally, nitric oxide activates an enzyme called soluble guanylate cyclase (sGC), which produces cGMP to relax blood vessel walls.
Riociguat works in two ways: it makes sGC more sensitive to whatever nitric oxide is available, and it can also directly stimulate sGC even without nitric oxide. The result is increased cGMP, which relaxes and widens pulmonary blood vessels.
▸What are the side effects of Riociguat?
Carries a black box warning for embryo-fetal toxicity (must not be used in pregnancy). Common side effects include headache, dizziness, indigestion, nausea, diarrhea, and low blood pressure. Must not be used with PDE5 inhibitors (sildenafil, tadalafil, vardenafil) or nonspecific PDE inhibitors such as dipyridamole or theophylline, with nitrates or nitric oxide donors, or with other sGC stimulators, and must not be used in pulmonary hypertension caused by idiopathic interstitial pneumonias. Women who can become pregnant need effective birth control before, during and for 1 month after treatment. The label also warns about serious bleeding, including coughing up blood (1 case in trials was fatal), and about fluid in the lungs in people with pulmonary veno-occlusive disease.
▸How is Riociguat taken?
Taken orally 3 times daily, with or without food. Tablets can be crushed and mixed with water or soft food such as applesauce for people who have trouble swallowing. Starting dose is 1 mg 3 times daily, gradually increased to a maximum of 2.5 mg 3 times daily based on blood pressure tolerance. Requires negative pregnancy testing.
▸Is Riociguat FDA approved?
Yes, Riociguat (Adempas) is FDA approved (2013) for the treatment of Pulmonary Arterial Hypertension.
▸Can riociguat be used with sildenafil or tadalafil?
No. Riociguat must not be combined with PDE5 inhibitors (sildenafil, tadalafil) because both drugs increase cGMP levels through complementary mechanisms, and the combination can cause severe hypotension (dangerously low blood pressure). This contraindication is absolute. Patients switching from a PDE5 inhibitor to riociguat must allow an appropriate washout period. Conversely, patients on riociguat should not start a PDE5 inhibitor.
▸What makes riociguat unique among PAH drugs?
Riociguat is the only drug approved for chronic thromboembolic pulmonary hypertension (CTEPH), a distinct form of pulmonary hypertension caused by blood clots in the lungs that cannot be surgically removed or that persist after surgery. It is also the only sGC stimulator approved for PAH, representing a mechanism of action distinct from endothelin receptor antagonists, prostacyclins, and PDE5 inhibitors.
▸Why is riociguat taken 3 times daily?
Riociguat has a relatively short half-life of about 7-12 hours, which requires three-times-daily dosing to maintain adequate drug levels throughout the day and night. While less convenient than once-daily drugs like macitentan or tadalafil, the three-times-daily schedule is necessary to provide consistent sGC stimulation. Riociguat can be taken with or without food.
▸What is the dose titration process?
Riociguat is started at 1 mg 3 times daily and gradually increased by 0.5 mg increments every 2 weeks, up to a maximum of 2.5 mg 3 times daily. The dose is titrated based on systolic blood pressure (must stay above 95 mmHg) and tolerability. This careful titration helps avoid hypotension while finding the optimal dose for each patient.