regadenoson 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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) 4 Bocci G, Oprea TI, Benet LZ
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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AXL,CAMK2D,CDK5,CDK9,CLK2,DYRK1B,EIF2AK3,FLT3,GRK2,ITK,MAP3K21,NTRK1,NTRK2,PDK1,PDK2,PIK3CD,PRKDC 18
kinase-selectivity-class MAP3K21,PDK1 2
pfas-class PFAS structural alert (1 = True, 0 = False) 0

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 619.60 55.67 120 2484 8899 90616944
Incorrect product administration duration 110.82 55.67 35 2569 19287 90606556
Nausea 107.41 55.67 144 2460 1110172 89515671
Unresponsive to stimuli 105.30 55.67 40 2564 38081 90587762
Tremor 88.80 55.67 55 2549 153118 90472725
Seizure 78.94 55.67 51 2553 152578 90473265
Hypotension 76.94 55.67 68 2536 325329 90300514
Bradycardia 69.47 55.67 38 2566 83809 90542034
Headache 68.24 55.67 102 2502 862644 89763199
Dyspnoea 68.05 55.67 103 2501 880852 89744991
Infusion site extravasation 64.58 55.67 20 2584 10308 90615535
Extravasation 62.70 55.67 15 2589 2949 90622894
Chest pain 62.30 55.67 60 2544 319585 90306258
Blood pressure decreased 62.19 55.67 34 2570 74861 90550982
Cardiac arrest 59.01 55.67 37 2567 104898 90520945

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 608.73 56.30 106 1656 3016 42616557
Unresponsive to stimuli 116.40 56.30 45 1717 31358 42588215
Cardiac arrest 105.83 56.30 62 1700 109258 42510315
Bradycardia 103.05 56.30 56 1706 85428 42534145
Hypotension 99.58 56.30 83 1679 257548 42362025
Incorrect product administration duration 95.92 56.30 26 1736 5854 42613719
Seizure 85.20 56.30 56 1706 120505 42499068
Blood pressure decreased 83.76 56.30 43 1719 58289 42561284
Loss of consciousness 58.16 56.30 40 1722 92314 42527259

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 915.23 54.88 174 3537 9995 110575593
Incorrect product administration duration 209.28 54.88 60 3651 20438 110565150
Unresponsive to stimuli 198.18 54.88 76 3635 63714 110521874
Bradycardia 149.89 54.88 82 3629 155435 110430153
Cardiac arrest 144.81 54.88 87 3624 196666 110388922
Hypotension 133.42 54.88 122 3589 523727 110061861
Seizure 128.03 54.88 84 3627 221101 110364487
Blood pressure decreased 117.23 54.88 63 3648 115028 110470560
Dyspnoea 96.85 54.88 149 3562 1106723 109478865
Chest pain 92.34 54.88 86 3625 376289 110209299
Nausea 79.46 54.88 145 3566 1235545 109350043
Dizziness 75.32 54.88 104 3607 698089 109887499
Loss of consciousness 70.77 54.88 56 3655 196250 110389338
Heart rate increased 69.66 54.88 49 3662 143785 110441803
Tremor 67.19 54.88 55 3656 202177 110383411
Sinus arrest 64.49 54.88 17 3694 4225 110581363
Atrioventricular block 62.83 54.88 23 3688 16854 110568734
Atrioventricular block complete 58.94 54.88 23 3688 20059 110565529
Injection site pain 56.18 54.88 47 3664 177875 110407713
Hemiplegic migraine 55.83 54.88 9 3702 191 110585397

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C01EB21 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
OTHER CARDIAC PREPARATIONS
Other cardiac preparations
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D058906 Purinergic P1 Receptor Agonists
MeSH PA D058908 Adenosine A2 Receptor Agonists
MeSH PA D058913 Purinergic Agonists
FDA MoA N0000175788 Adenosine Receptor Agonists
FDA EPC N0000178375 Adenosine Receptor Agonist
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:75835 anti-anaemic agent

Related Drugs by ATC class:

C01EB Other cardiac preparations 15 drugs
acadesineacoramidisadenosinecamphorcreatinolfosfateibuprofenindomethacinivabradinemavacamtenmeldoniumphosphocreatineranolazine show all 15 →

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)

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 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
CHEMBL3989695 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
365575 MMSL
d07131 MMSL
012689 NDDF
430242005 SNOMEDCT_US
433327005 SNOMEDCT_US
CHEBI:135613 CHEBI
2XLN4Y044H INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
LEXISCAN HUMAN PRESCRIPTION DRUG LABEL 1 0469-6501 INJECTION, SOLUTION 0.08 mg INTRAVENOUS NDA 28 sections
Regadenoson HUMAN PRESCRIPTION DRUG LABEL 1 10135-803 INJECTION, SOLUTION 0.08 mg INTRAVENOUS ANDA 18 sections
regadenoson HUMAN PRESCRIPTION DRUG LABEL 1 36000-364 INJECTION, SOLUTION 0.08 mg INTRAVENOUS ANDA 26 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 60505-6116 INJECTION, SOLUTION 0.08 mg INTRAVENOUS ANDA 26 sections
Regadenoson HUMAN PRESCRIPTION DRUG LABEL 1 60505-6288 INJECTION, SOLUTION 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
Regadenoson HUMAN PRESCRIPTION DRUG LABEL 1 72611-874 INJECTION, SOLUTION 0.08 mg INTRAVENOUS ANDA 26 sections
Regadenoson HUMAN PRESCRIPTION DRUG LABEL 1 83032-001 INJECTION, SOLUTION 0.08 mg INTRAVENOUS ANDA 18 sections
Regadenoson HUMAN PRESCRIPTION DRUG LABEL 1 85742-012 INJECTION, SOLUTION 0.08 mg INTRAVENOUS ANDA 18 sections