Stem definition | Drug id | CAS RN |
---|---|---|
adenosine A receptor agonists | 2362 | 313348-27-5 |
Dose | Unit | Route |
---|---|---|
0.40 | mg | P |
Property | Value | Reference |
---|---|---|
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 |
Date | Agency | Company | Orphan |
---|---|---|---|
April 10, 2008 | FDA | ASTELLAS |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 |
None
Source | Code | Description |
---|---|---|
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 |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
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 |
None
None
Dissociation level | Dissociation constant | Type (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 |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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 |
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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 |
ID | Source |
---|---|
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 |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
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 |