regadenoson Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
adenosine A receptor agonists 2362 313348-27-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • CVT-3146
  • rapiscan
  • regadenoson
  • lexiscan
  • Molecular weight: 390.36
  • Formula: C15H18N8O5
  • CLOGP: -2.86
  • LIPINSKI: 1
  • HAC: 13
  • HDO: 5
  • TPSA: 186.46
  • ALOGS: -1.91
  • ROTB: 4

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.40 mg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.05 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 65 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 7.48 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 0.94 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 7.30 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.70 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
April 10, 2008 FDA ASTELLAS

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Injection site extravasation 495.73 47.28 101 1843 6684 46677434
Infusion site extravasation 70.62 47.28 20 1924 5236 46678882
Unresponsive to stimuli 67.96 47.28 31 1913 32143 46651975
Nausea 67.07 47.28 109 1835 687345 45996773
Headache 57.89 47.28 84 1860 478268 46205850
Incorrect product administration duration 54.90 47.28 19 1925 9558 46674560
Extravasation 52.06 47.28 13 1931 2102 46682016
Tremor 51.97 47.28 41 1903 115598 46568520
Seizure 51.83 47.28 42 1902 123012 46561106
Chest pain 48.01 47.28 47 1897 176277 46507841

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Injection site extravasation 526.21 57.85 90 1259 2110 29949019
Cardiac arrest 86.68 57.85 53 1296 92797 29858332
Bradycardia 73.05 57.85 42 1307 65484 29885645
Incorrect product administration duration 70.19 57.85 19 1330 3903 29947226
Unresponsive to stimuli 68.32 57.85 30 1319 26389 29924740
Hypotension 67.52 57.85 62 1287 200503 29750626
Seizure 64.32 57.85 45 1304 98430 29852699

Pharmacologic Action:

SourceCodeDescription
ATC C01EB21 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
OTHER CARDIAC PREPARATIONS
Other cardiac preparations
MeSH PA D058908 Adenosine A2 Receptor Agonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D058913 Purinergic Agonists
MeSH PA D058906 Purinergic P1 Receptor Agonists
FDA MoA N0000175788 Adenosine Receptor Agonists
FDA EPC N0000178375 Adenosine Receptor Agonist

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Myocardial Perfusion Imaging Adjunct indication
Pericarditis contraindication 3238004 DOID:1787
Bronchospasm contraindication 4386001
Chronic obstructive lung disease contraindication 13645005 DOID:3083
Disorder of autonomic nervous system contraindication 15241006
Complete atrioventricular block contraindication 27885002
Hypovolemia contraindication 28560003
Acute cerebrovascular insufficiency contraindication 29322000
Sick sinus syndrome contraindication 36083008 DOID:13884
Hypertensive disorder contraindication 38341003 DOID:10763
Low blood pressure contraindication 45007003
Bradycardia contraindication 48867003
Sinus bradycardia contraindication 49710005
Wheezing contraindication 56018004
Aortic valve stenosis contraindication 60573004 DOID:1712
Carotid artery stenosis contraindication 64586002 DOID:13001
Mitral valve stenosis contraindication 79619009 DOID:1754
Seizure disorder contraindication 128613002
Second degree atrioventricular block contraindication 195042002
Asthma contraindication 195967001 DOID:2841
Transient ischemic attack contraindication 266257000 DOID:224
Syncope contraindication 271594007
Left main coronary artery disease contraindication 371804009
Pericardial effusion contraindication 373945007 DOID:118

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.38 acidic
pKa2 11.67 acidic
pKa3 12.33 acidic
pKa4 13.34 acidic
pKa5 5.37 Basic
pKa6 4.79 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Adenosine receptor A2a GPCR AGONIST EC50 5.89 WOMBAT-PK CHEMBL
Adenosine receptor A1 GPCR EC50 4.40 WOMBAT-PK
Adenosine receptor A2a GPCR Ki 6.54 CHEMBL

External reference:

IDSource
4027430 VUID
N0000176153 NUI
D05711 KEGG_DRUG
875148-45-1 SECONDARY_CAS_RN
4027430 VANDF
C0971703 UMLSCUI
CHEBI:135613 CHEBI
CHEMBL3989695 ChEMBL_ID
CHEMBL317052 ChEMBL_ID
DB06213 DRUGBANK_ID
C430916 MESH_SUPPLEMENTAL_RECORD_UI
219024 PUBCHEM_CID
5596 IUPHAR_LIGAND_ID
2XLN4Y044H UNII
640062 RXNORM
136259 MMSL
25274 MMSL
d07131 MMSL
012689 NDDF
430242005 SNOMEDCT_US
433327005 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
LEXISCAN HUMAN PRESCRIPTION DRUG LABEL 1 0469-6501 INJECTION, SOLUTION 0.08 mg INTRAVENOUS NDA 28 sections
LEXISCAN(R) (REGADENOSON) HUMAN PRESCRIPTION DRUG LABEL 1 51662-1448 INJECTION, SOLUTION 0.08 mg INTRAVENOUS NDA 18 sections