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 | 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 |
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 | 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 |
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 | 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 |
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 |
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 |
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 | 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 |