Regadenoson

Regadenoson

Regadenoson
Systematic (IUPAC) name
2-{4-[(methylamino)carbonyl]- 1H-pyrazol-1-yl}adenosine
Clinical data
AHFS/Drugs.com
Licence data US FDA:
Pregnancy
category
  • US: C (Risk not ruled out)
Legal status
Routes of
administration
Intravenous
Identifiers
CAS Registry Number  YesY 875148-45-1
ATC code C01
PubChem CID:
IUPHAR/BPS
DrugBank  N
ChemSpider  N
UNII  N
KEGG  YesY
ChEMBL  N
Synonyms 1-[6-amino-9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]purin-2-yl]- N-methylpyrazole-4-carboxamide
Chemical data
Formula C15H18N8O5
Molecular mass 390.354 g/mol
 N   

Regadenoson (INN, code named CVT-3146) is an A2A adenosine receptor agonist that is a coronary vasodilator that is commonly used in pharmacologic stress testing. It produces hyperemia quickly and maintains it for a duration that is useful for radionuclide myocardial perfusion imaging.[1] The selective nature of the drug makes it preferable to other stress agents such as adenosine, which are less selective and therefore cause more side-effects.

Regadenoson was approved by the United States Food and Drug Administration on April 10, 2008 and is marketed by Astellas Pharma under the tradename Lexiscan.[2] It is approved for use in the European Union and under the name of Rapiscan. It is currently being marketed by GE Healthcare and is being sold in both the United Kingdom and Germany.

Regadenoson has a 2 to 3 minute biological half-life, as compared with adenosine's 10-second half-life. As a result, regadenoson stress protocols use a single bolus, instead of a 4-6 minute continuous infusion, which was needed with adenosine. Another difference is that adenosine infusion is weight based (140mcg/kg/minute), while with regadenoson, a 0.4mg/5mL preloaded syringe dose is standard for all weights. Regadenoson stress tests are not affected by the presence of beta blockers, as regadenoson vasodilates via the adenosine pathway without stimulating beta adrenergic receptors.

References

  1. ^
  2. ^ CV Therapeutics and Astellas Announce FDA Approval for Lexiscan(TM)