Regadenoson
Adenosine Receptor Agonist — CARDIOVASCULAR SYSTEM
Also known as: CVT-3146, lexiscan, rapiscan
Data last refreshed: (DrugCentral release 2024-11-01)
Key facts
Regadenoson is an ofp drug in the Adenosine Receptor Agonist class catalogued in DrugCentral. It was first approved by the FDA in 2008. Its mechanism of action is classified as Adenosine Receptor Agonists. DrugCentral lists 5 molecular targets, including Adora2a, ADORA2A and ADORA2B. Recorded indications include Myocardial Perfusion Imaging Adjunct.
- Approval status: ofp (first approved 2008 by the FDA).
- Drug class: Adenosine Receptor Agonist.
- Mechanism of action: Adenosine Receptor Agonists.
- Molecular targets: Adora2a, ADORA2A, ADORA2B and ADORA3 (5 listed in DrugCentral).
- Indications: Myocardial Perfusion Imaging Adjunct.
- ATC code: C01EB21 (Other cardiac preparations).
- Molecular formula: C15H18N8O5; molecular weight 390.36 g/mol.
Indications & contraindications
Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).
Indications (1)
- Myocardial Perfusion Imaging Adjunct
Contraindications (23)
- Acute cerebrovascular insufficiency
- Aortic valve stenosis
- Asthma
- Bradycardia
- Bronchospasm
- Carotid artery stenosis
- Chronic obstructive lung disease
- Complete atrioventricular block
- Disorder of autonomic nervous system
- Hypertensive disorder
- Hypovolemia
- Left main coronary artery disease
- Low blood pressure
- Mitral valve stenosis
- Pericardial effusion
- Pericarditis
- Second degree atrioventricular block
- Seizure disorder
- Sick sinus syndrome
- Sinus bradycardia
- Syncope
- Transient ischemic attack
- Wheezing
Mechanism & targets
| Mechanism of action (MoA) | Adenosine Receptor Agonists |
|---|---|
| Established pharmacologic class | Adenosine Receptor Agonist |
Molecular targets (5)
| Target | Gene | Action | Activity |
|---|---|---|---|
| Adenosine receptor A2a | Adora2a | unknown | Ki 6.54 |
| Adenosine receptor A2a | ADORA2A | agonist | EC50 5.89 |
| Adenosine receptor A2b | ADORA2B | unknown | EC50 5.00 |
| Adenosine receptor A3 | ADORA3 | unknown | Ki 5.00 |
| Adenosine receptor A1 | ADORA1 | unknown | EC50 4.40 |
Regulatory approvals (1)
| Date | Agency | Marketed as | Applicant | Orphan |
|---|---|---|---|---|
| 2008-04-10 | FDA | — | ASTELLAS |
ATC classification
| ATC code | Therapeutic hierarchy |
|---|---|
C01EB21 | CARDIOVASCULAR SYSTEM › CARDIAC THERAPY › OTHER CARDIAC PREPARATIONS › Other cardiac preparations |
Reported adverse-event signals
Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.
| MedDRA term | LLR |
|---|---|
| Injection site extravasation | 1616.3 |
| Unresponsive to stimuli | 241.1 |
| Hypotension | 222.3 |
| Incorrect product administration duration | 211.6 |
| Bradycardia | 184.7 |
| Seizure | 180.5 |
| Cardiac arrest | 179.6 |
| Nausea | 175.2 |
| Extravasation | 170.7 |
| Blood pressure decreased | 162.1 |
| Infusion site extravasation | 151.8 |
| Dyspnoea | 135.3 |
Chemical structure
| Molecular formula | C15H18N8O5 |
|---|---|
| Molecular weight | 390.36 g/mol |
| CAS number | — |
| InChIKey | LZPZPHGJDAGEJZ-AKAIJSEGSA-N |
| PubChem CID | 219024 |
Frequently asked questions
Answers are generated from the structured data on this page, not written by hand.
What is Regadenoson used for?
DrugCentral lists the following indications for Regadenoson: Myocardial Perfusion Imaging Adjunct.
How does Regadenoson work?
Regadenoson is classified as Adenosine Receptor Agonists; its molecular targets in DrugCentral include Adora2a, ADORA2A (agonist), ADORA2B and ADORA3.
When was Regadenoson first approved?
Regadenoson was first approved by the FDA in 2008.
What drug class does Regadenoson belong to?
Regadenoson is in the Adenosine Receptor Agonist class.
What is the chemical formula of Regadenoson?
Regadenoson has the molecular formula C15H18N8O5 and a molecular weight of 390.36 g/mol.
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Sources
- DrugCentral drug card 2362 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
- ChEMBL CHEMBL3989695 — compound record and bioactivity
- PubChem CID 219024 — chemical identifiers
- DrugBank DB06213 — drug record
- FDA UNII 2XLN4Y044H — substance identity
- DailyMed: FDA labels for Regadenoson — current prescribing information (label search)
- UniProt P29274 (ADORA2A) — target protein
- UniProt P29275 (ADORA2B) — target protein
- UniProt P0DMS8 (ADORA3) — target protein
- UniProt P30542 (ADORA1) — target protein
- FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
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