Last reviewed 2026-04-20 · How we verify

Regadenoson

Regadenoson is a low affinity A2A adenosine receptor agonist that produces coronary vasodilation and increases coronary blood flow.

Regadenoson is a selective A2A adenosine receptor agonist indicated for radionuclide myocardial perfusion imaging in patients unable to exercise. It demonstrates rapid onset (1-4 minutes) with a short initial half-life (2-4 minutes) and is primarily renally excreted unchanged. Key risks include contraindication in patients with second- or third-degree AV block or sinus node dysfunction without pacemakers, and significant interactions with methylxanthines that must be avoided for 12 hours prior to administration. The drug's pharmacokinetics are minimally affected by age, gender, or race, with dose adjustment unnecessary even in renal or hepatic impairment.

At a glance

Mechanism of action

Regadenoson is a low affinity agonist for the A2A adenosine receptor with a Ki of approximately 1.3 µM, demonstrating at least 10-fold lower affinity for the A1 adenosine receptor (Ki > 16.5 µM) and weak or no affinity for A2B and A3 adenosine receptors. Activation of the A2A adenosine receptor by regadenoson produces coronary vasodilation and increases coronary blood flow. This mechanism enables its use as a pharmacologic stress agent for cardiac imaging in patients unable to undergo adequate exercise stress.

Approved indications

• Myocardial Perfusion Imaging Adjunct

Common side effects

• Headache
• Dyspnoea
• Shortness of Breath
• Flushing
• Angina pectoris
• Chest discomfort
• Dizziness
• Nausea
• Chest pain
• Stomach discomfort
• Chest Pain
• Abdominal discomfort

Drug interactions

• Methylxanthines (caffeine, aminophylline, theophylline)
• Aminophylline
• Dipyridamole
• Beta-blockers, calcium channel blockers, ACE inhibitors, nitrates, cardiac glycosides, angiotensin receptor blockers

Key clinical trials

• The Multicenter Stress Cardiac Magnetic Resonance Quantitative Perfusion Imaging in the United States Study (NA)
• Technical Development of Cardiovascular Magnetic Resonance Imaging (CMR) Using a Low Specific Absorption Rate (SAR) Scanner System (NA)
• Hyperpolarized 13C Pyruvate-MRI and FDG-PET in a Single Exam for the Prognosis of Ischemic Cardiomyopathy
• Stress Test in Detecting Heart Damage in Premenopausal Women With Stage I-III Breast Cancer
• The MATCH Investigation: CT Myocardial Perfusion and CT-FFR vs PET MPI (NA)
• Relationship Between Abnormal Myocardial Perfusion and Diastolic Dysfunction in Sickle Cell Disease Using PET (PHASE2)
• A Study to Evaluate the Safety and Pharmacokinetics of Regadenoson in Pediatric Patients (PHASE1, PHASE2)
• Improvement Assessment of Coronary Flow Dysfunction Using Fundamental Fluid Dynamics

Patents

Primary sources

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