Last reviewed 2026-04-20 · How we verify

Adempas (RIOCIGUAT)

Adempas works by stimulating the soluble guanylate cyclase enzyme to increase levels of cyclic guanosine monophosphate (cGMP), a signaling molecule that helps to relax blood vessels.

Adempas (riociguat) is a small molecule soluble guanylate cyclase stimulator developed by Bayer Healthcare. It targets the guanylate cyclase soluble subunit beta-1 to treat chronic thromboembolic pulmonary hypertension and pulmonary arterial hypertension. Adempas was FDA-approved in 2013 and remains a patented product. Key safety considerations include the risk of hypotension and increased bleeding risk. As a patented product, Adempas is not yet available as a generic.

At a glance

Mechanism of action

Riociguat is stimulator of soluble guanylate cyclase (sGC), an enzyme in the cardiopulmonary system and the receptor for nitric oxide (NO).When NO binds to sGC, the enzyme catalyzes synthesis of the signaling molecule cyclic guanosine monophosphate (cGMP). Intracellular cGMP plays an important role in regulating processes that influence vascular tone, proliferation, fibrosis and inflammation.Pulmonary hypertension is associated with endothelial dysfunction, impaired synthesis of nitric oxide and insufficient stimulation of the NO-sGC-cGMP pathway.Riociguat has dual mode of action. It sensitizes sGC to endogenous NO by stabilizing the NO-sGC binding. Riociguat also directly stimulates sGC via different binding site, independently of NO.Riociguat stimulates the NO-sGC-cGMP pathway and leads to increased generation of cGMP with subsequent vasodilation.The active metabolite (M1) of riociguat is 1/3 to 1/10 as potent as riociguat.

Approved indications

• Chronic thromboembolic pulmonary hypertension
• Pulmonary arterial hypertension

Boxed warnings

• WARNING: EMBRYO-FETAL TOXICITY Do not administer Adempas to a pregnant female because it may cause fetal harm [see Contraindications ( 4.1 ), Warnings and Precautions ( 5.1 ) and Use in Specific Populations ( 8.1 )]. Females of reproductive potential: Exclude pregnancy before the start of treatment, monthly during treatment, and 1 month after stopping treatment. To prevent pregnancy, females of reproductive potential must use effective forms of contraception during treatment and for one month after [see Dosage and Administration ( 2.3 ), Warnings and Precautions ( 5.1 , 5.2 ),and Use in Specific Populations ( 8.3 )]. For all female patients, Adempas is available only through a restricted program called the Adempas Risk Evaluation and Mitigation Strategy (REMS) Program [see Warnings and Precautions ( 5.1 , 5.2 )]. WARNING: EMBRYO-FETAL TOXICITY See full prescribing information for complete boxed warning. • Do not administer Adempas to a pregnant female because it may cause fetal harm. ( 4.1 , 5.1 , 8.1 ) • Females of reproductive potential: Exclude pregnancy before start of treatment, monthly during treatment, and 1 month after treatment discontinuation. Prevent pregnancy during treatment and for one month after treatment discontinuation by use of effective forms of contraception. ( 2.3 , 5.1, 5.2 , 8.6 ) • For females, Adempas is available only through a restricted program called the Adempas REMS Program. ( 5.1, 5.2 )

Common side effects

• Headache
• Dyspepsia and Gastritis
• Dizziness
• Nausea
• Diarrhea
• Hypotension
• Vomiting
• Anemia (including laboratory parameters)
• Gastroesophageal reflux disease
• Constipation
• Palpitations
• Nasal congestion

Drug interactions

• Vasodilators Organic Nitrates
• amyl nitrite
• dipyridamole
• eritrityl tetranitrate
• glyceryl trinitrate
• isosorbide
• itraconazole
• ketoconazole
• nitroprusside
• pentaerithrityl tetranitrate
• sildenafil
• sodium nitrite

Key clinical trials

• Riociguat in Children With Pulmonary Arterial Hypertension (PAH) (PHASE3)
• Treatment of Exercise-Induced Pulmonary Vascular Dysfunction After Pulmonary Thromboendarterectomy or Balloon Pulmonary Angioplasty (PHASE2)
• Riociguat in Triple Therapy for Pulmonary Arterial Hypertension in Real-World Practice
• Efficacy and Safety of Riociguat in Incipient Pulmonary Vascular Disease as an Indicator for Early PAH (PHASE2)
• A Study of Sotatercept for Patients With Eisenmenger Syndrome or Unrepaired Shunt-Associated Pulmonary Arterial Hypertension Resistant to Vasodilator Therapy (PHASE4)
• Effects of Combination Medical Therapy Followed by BPA on Right Ventricular-PA Coupling and Hemodynamics in CTEPH (PHASE3)
• A Long-term Extension Study of Riociguat in Patients With Symptomatic Pulmonary Arterial Hypertension. (PHASE4)
• Effects of Riociguat on RIght VEntricular Size and Function in PAH and CTEPH (PHASE4)

Patents

Primary sources

Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.