regadenoson 🐶 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 µM/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 539.24 53.93 111 2132 8073 56281751
Incorrect product administration duration 103.61 53.93 31 2212 10295 56279529
Nausea 86.96 53.93 127 2116 764051 55525773
Unresponsive to stimuli 82.75 53.93 35 2208 31690 56258134
Headache 66.27 53.93 95 2148 558949 55730875
Seizure 63.83 53.93 47 2196 125072 56164752
Infusion site extravasation 62.68 53.93 20 2223 8190 56281634
Tremor 58.43 53.93 44 2199 121045 56168779
Chest pain 54.33 53.93 51 2192 189746 56100078

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 565.81 59.85 99 1410 2511 31693324
Cardiac arrest 101.60 59.85 59 1450 89003 31606832
Incorrect product administration duration 100.37 59.85 26 1483 4276 31691559
Unresponsive to stimuli 80.49 59.85 34 1475 25766 31670069
Hypotension 77.01 59.85 69 1440 204549 31491286
Seizure 73.14 59.85 50 1459 99718 31596117
Bradycardia 71.22 59.85 43 1466 69284 31626551
Blood pressure decreased 68.65 59.85 37 1472 48054 31647781

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 827.79 55.18 163 2955 8583 70916743
Incorrect product administration duration 202.45 55.18 54 3064 10770 70914556
Unresponsive to stimuli 145.56 55.18 62 3056 51869 70873457
Cardiac arrest 110.36 55.18 75 3043 159759 70765567
Seizure 103.08 55.18 75 3043 177887 70747439
Bradycardia 101.84 55.18 65 3053 124550 70800776
Blood pressure decreased 95.93 55.18 56 3062 91459 70833867
Hypotension 88.12 55.18 98 3020 404283 70521043
Chest pain 80.37 55.18 75 3043 251185 70674141
Dyspnoea 78.91 55.18 129 2989 769931 70155395
Atrioventricular block 63.18 55.18 23 3095 12665 70912661
Nausea 63.12 55.18 124 2994 851964 70073362
Dizziness 60.29 55.18 87 3031 464054 70461272
Sinus arrest 59.85 55.18 16 3102 3199 70922127
Loss of consciousness 58.58 55.18 51 3067 155665 70769661
Heart rate increased 57.40 55.18 43 3075 106105 70819221
Injection site pain 55.63 55.18 44 3074 117575 70807751

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 | Suggest Off label Use Form| |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




🐶 Veterinary Drug Use

None

🐶 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
875148-45-1 SECONDARY_CAS_RN
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

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 55150-443 INJECTION 0.08 mg INTRAVENOUS ANDA 26 sections
Regadenoson Human Prescription Drug Label 1 68083-175 INJECTION, SOLUTION 0.08 mg INTRAVENOUS ANDA 27 sections
Regadenoson HUMAN PRESCRIPTION DRUG LABEL 1 71288-201 INJECTION, SOLUTION 0.08 mg INTRAVENOUS ANDA 26 sections