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regadenoson

Trade name: lexiscan

Small moleculeapproved

Approved

Apr 10, 2008

Regadenoson (Lexiscan), a low affinity agonist of the A2A adenosine receptor, increases coronary blood flow (CBF) and mimics the increase in CBF caused by exercise. Myocardial uptake of the radiopharmaceutical is proportional to CBF creating the contrast required to identify stenotic coronary arteries. It is a pharmacologic stress agent indicated for radionuclide myocardial perfusion imaging (MPI) in patients unable to undergo adequate exercise stress. The most common adverse reactions to Lexiscan are dyspnea, headache, flushing, chest discomfort, dizziness, angina pectoris, chest pain, and nausea. Methylxanthines, e.g., caffeine and theophylline, may interfere with the activity of Lexiscan. Aminophylline may be used to attenuate severe and/or persistent adverse reactions to Lexiscan. — NCATS

Clinical trial activity

58 trials · 53 clinical orgs · 19 marketing orgs

Phase 1
10
Phase 2
18
Phase 3
6
Phase 4
16

Earliest trial started Oct 1, 2003 (NCT00208299)

Timeline

2000s

  1. Jan 1, 2003

    Earliest Phase 3 Sponsor(trial)

  2. Apr 10, 2008

    CV Therapeutics — Earliest FDA Approval

  3. Apr 10, 2008

    Astellas — NDA Secondary Org

  4. Apr 10, 2008

    CV Therapeutics — NDA Organization

  5. Jan 1, 2009

    Earliest Phase 1 Sponsor(trial)

  6. Jan 1, 2009

    Earliest Phase 2 Sponsor(trial)

2020s

  1. Jan 15, 2021

    Dr. Reddy's Laboratories — Marketing Organization

  2. Mar 11, 2022

    Mylan — Marketing Organization

  3. Apr 11, 2022

    Apotex — Marketing Organization

  4. Apr 11, 2022

    Accord Research — Marketing Organization

  5. Apr 11, 2022

    Meitheal — Marketing Organization

  6. May 23, 2022

    IMS Health — Marketing Organization

  7. May 23, 2022

    IQVIA — Marketing Organization

  8. Jul 12, 2022

    Gland Pharma Ltd — Marketing Organization

  9. Jul 12, 2022

    Fosun — Marketing Organization

  10. Aug 31, 2022

    Hospira — Marketing Organization

  11. Aug 31, 2022

    Pfizer — Marketing Organization

  12. Oct 26, 2022

    Eugia Pharma — Marketing Organization

  13. Feb 2, 2023

    Hikma — Marketing Organization

  14. May 23, 2023

    Baxalta — Marketing Organization

  15. May 23, 2023

    Takeda — Marketing Organization

  16. Aug 5, 2024

    General Electric — Marketing Organization

  17. Aug 22, 2024

    INDIES PHARMA — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedApr 10, 2008

Chemistry & pharmacology

Loading structure…

SMILES

CNC(=O)c1cnn(-c2nc(N)c3ncn([C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)c3n2)c1.O
Mol. weight
408.38 g/mol
Lipinski Ro5
1 violation(s)
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Parenteral
Availability
Prescription Only

Oral

No

Parenteral

Yes

Topical

No

Sources

Also known as

  • (1-(9-(3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl)-6-aminopurin-2-yl)pyrazol-4-yl)-n-methylcarboxamide
  • cvt3146
  • cvt 3146
  • cvt-3146
  • cvt-3146
  • cvt-3146
  • cvt-3146
  • cvt-3146
  • cvt-3146
  • lexiscan
  • lexiscan
  • lexiscan
  • lexiscan
  • lexiscan
  • rapiscan
  • regadenoson
  • regadenoson
  • regadenoson
  • regadenoson
  • regadenoson
  • regadenoson
  • regadenoson
  • regadenoson
  • regadenoson
  • regadenoson anhydrous
  • regadenoson anhydrous
  • regadenson

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT05583721Phase 2Jan 31, 2023St. Jude Children's Hospital
NCT04606069Phase 1/Phase 2 (Phase 2)Nov 1, 2020University of Maryland
NCT04604782Phase 1/Phase 2 (Phase 2)Oct 31, 2020Covance, General Electric, University of London
NCT04521569Early Phase 1 (Phase 1)Jun 22, 2020National Heart, Lung, and Blood Institute (NHLBI), University of Maryland
NCT04316676N/AMay 31, 2020Emory University, Siemens
NCT03354273Phase 3Jun 8, 2018General Electric
NCT03236311Phase 2Oct 12, 2017Sanofi
NCT03249272Phase 4Sep 5, 2017Duke University
NCT03072589Phase 1Aug 1, 2017National Heart, Lung, and Blood Institute (NHLBI), University of Virginia
NCT03102125Phase 4Apr 1, 2017Astellas, University of California, San Diego
NCT03090087Phase 2Mar 22, 2017Aarhus University
NCT04600115Early Phase 1 (Phase 1)Mar 3, 2017National Heart, Lung, and Blood Institute (NHLBI), University of Utah
NCT03103061Phase 2Feb 9, 2016Astellas, Medical University of South Carolina, University of South Carolina
NCT02597543Phase 4Nov 1, 2015Astellas, Stanford University, University of California, San Diego
NCT02589977Phase 4Nov 1, 2015Astellas, Vanderbilt University
NCT02389738Early Phase 1 (Phase 1)Feb 1, 2015Johns Hopkins University
NCT02115308Phase 4Aug 1, 2014Aspire Foundation, Cardiovascular Imaging Technologies, Saint Luke's Health System
NCT02130453Phase 4Aug 1, 2014Astellas, University of Texas at Houston
NCT02220634N/AAug 1, 2014Astellas, University of Colorado, Denver
NCT01969916N/AJun 1, 2014Astellas, University of Chicago
Showing 20 of 58 trials
Page 1 / 3

Organizations

Research & Development (53)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
AstellasFor profit34652003
National Heart, Lung, and Blood Institute (NHLBI)Government5022010
Harvard UniversityAcademic/Hospital4342010
University of UtahAcademic/Hospital4432009
Washington University in St. LouisAcademic/Hospital4232009
Cardiovascular Imaging TechnologiesFor profit3312008
General ElectricFor profit3232012
Gilead SciencesFor profit3322003
Johns Hopkins UniversityAcademic/Hospital3122010
La Jolla Institute for Allergy & ImmunologyAcademic/Hospital3032010
Medical College of WisconsinAcademic/Hospital3032010
University of ChicagoAcademic/Hospital3312009
University of MarylandAcademic/Hospital3332009
Duke UniversityAcademic/Hospital2122013
Emory UniversityAcademic/Hospital2222013
Mayo ClinicAcademic/Hospital2112009
University of California, San DiegoAcademic/Hospital2212015
University of Colorado, DenverAcademic/Hospital2222009
University of Illinois at ChicagoAcademic/Hospital2022012
University of LondonAcademic/Hospital2012009
53 organizations
Page 1 / 3

Marketing (23)

OrganizationOrg typeRelationshipDate
Accord ResearchFor profitMKTGApr 11, 2022
ApotexFor profitMKTGMay 27, 2020
ApotexFor profitMKTGApr 11, 2022
AstellasFor profitNDA2Apr 10, 2008
BaxaltaFor profitMKTGMay 23, 2023
CV TherapeuticsFor profitNDAApr 10, 2008
Dr. Reddy's LaboratoriesFor profitMKTGJan 15, 2021
Dr. Reddy's LaboratoriesFor profitMKTGApr 11, 2022
Eugia PharmaFor profitMKTGOct 26, 2022
FosunFor profitMKTGJul 12, 2022
General ElectricFor profitMKTGAug 5, 2024
Gland Pharma LtdFor profitMKTGJul 12, 2022
Gland Pharma LtdFor profitSYNJul 12, 2022
HikmaFor profitMKTGFeb 2, 2023
HospiraFor profitMKTGAug 31, 2022
IMS HealthFor profitMKTGMay 23, 2022
INDIES PHARMAFor profitMKTGAug 22, 2024
IQVIAFor profitMKTGMay 23, 2022
MeithealFor profitMKTGApr 11, 2022
MylanFor profitMKTGMar 11, 2022
MylanFor profitSYNApr 4, 2023
PfizerFor profitMKTGAug 31, 2022
TakedaFor profitMKTGMay 23, 2023