regadenoson ๐Ÿถ Veterinary Use | 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: -1.67
  • LIPINSKI: 1
  • HAC: 13
  • HDO: 5
  • TPSA: 186.46
  • ALOGS: -1.91
  • ROTB: 4

  • Status: OFP

  • 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 ยตM/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 524.65 49.77 108 2034 7393 50595589
Incorrect product administration duration 87.79 49.77 27 2115 9248 50593734
Nausea 78.73 49.77 120 2022 705278 49897704
Unresponsive to stimuli 78.64 49.77 34 2108 30575 50572407
Infusion site extravasation 64.70 49.77 20 2122 6956 50596026
Headache 63.14 49.77 91 2051 506444 50096538
Seizure 61.57 49.77 46 2096 117828 50485154
Tremor 58.13 49.77 44 2098 114859 50488123
Chest pain 52.86 49.77 50 2092 176832 50426150
Extravasation 52.55 49.77 13 2129 1989 50600993

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 555.87 55.29 97 1361 2336 29570733
Incorrect product administration duration 96.22 55.29 25 1433 4016 29569053
Cardiac arrest 93.95 55.29 56 1402 85535 29487534
Unresponsive to stimuli 73.62 55.29 32 1426 25094 29547975
Seizure 72.30 55.29 49 1409 93074 29479995
Hypotension 72.06 55.29 66 1392 194288 29378781
Bradycardia 72.03 55.29 43 1415 65586 29507483
Blood pressure decreased 63.79 55.29 35 1423 45442 29527627

FDA Adverse Event Reporting System (Geriatric)

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 801.69 53.62 158 2829 7928 64487817
Incorrect product administration duration 181.47 53.62 49 2938 9709 64486036
Unresponsive to stimuli 134.45 53.62 59 2928 50334 64445411
Seizure 99.37 53.62 73 2914 166819 64328926
Cardiac arrest 97.65 53.62 70 2917 153994 64341751
Bradycardia 94.49 53.62 62 2925 118157 64377588
Blood pressure decreased 85.86 53.62 52 2935 86147 64409598
Hypotension 83.59 53.62 95 2892 380879 64114866
Dyspnoea 73.78 53.62 124 2863 718550 63777195
Chest pain 73.40 53.62 71 2916 235909 64259836
Sinus arrest 59.65 53.62 16 2971 3074 64492671
Dizziness 58.96 53.62 85 2902 430078 64065667
Heart rate increased 58.21 53.62 43 2944 98632 64397113
Nausea 57.14 53.62 117 2870 785683 63710062
Loss of consciousness 56.42 53.62 50 2937 148315 64347430

FDA Adverse Event Reporting System (Pediatric)

None

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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
0.4MG/5ML (0.08MG/ML) LEXISCAN ASTELLAS N022161 April 10, 2008 RX SOLUTION INTRAVENOUS 6403567 April 10, 2022 METHOD FOR STIMULATING CORONARY VASODILATION FOR PURPOSES OF IMAGING THE HEART

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 A2b GPCR EC50 5 CHEMBL
Adenosine receptor A3 GPCR Ki 5 CHEMBL
Adenosine receptor A2a GPCR Ki 6.54 CHEMBL

External reference:

IDSource
4027430 VUID
N0000176153 NUI
D05711 KEGG_DRUG
4027430 VANDF
C1698215 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
875148-45-1 SECONDARY_CAS_RN

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
Regadenoson HUMAN PRESCRIPTION DRUG LABEL 1 71288-201 INJECTION, SOLUTION 0.08 mg INTRAVENOUS ANDA 26 sections