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regadenoson 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
adenosine A receptor agonists	2362	313348-27-5

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
0.40	mg	P

ADMET properties:

Property	Value	Reference
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

Approvals:

Date	Agency	Company	Orphan
April 10, 2008	FDA	ASTELLAS

FDA Adverse Event Reporting System (Female)

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	558.75	51.38	114	2189	8727	63477992
Incorrect product administration duration	120.58	51.38	35	2268	11511	63475208
Unresponsive to stimuli	90.55	51.38	37	2266	33779	63452940
Nausea	86.63	51.38	128	2175	854343	62632376
Seizure	67.63	51.38	48	2255	132586	63354133
Tremor	65.45	51.38	47	2256	132192	63354527
Headache	65.45	51.38	96	2207	633145	62853574
Infusion site extravasation	59.82	51.38	20	2283	10406	63476313
Hypotension	56.80	51.38	59	2244	272545	63214174
Bradycardia	55.55	51.38	34	2269	73193	63413526
Chest pain	54.69	51.38	52	2251	215907	63270812
Dyspnoea	53.96	51.38	90	2213	661223	62825496
Extravasation	52.36	51.38	13	2290	2359	63484360
Blood pressure decreased	51.39	51.38	31	2272	64991	63421728

FDA Adverse Event Reporting System (Male)

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	572.00	56.76	101	1484	2841	34952505
Cardiac arrest	105.33	56.76	61	1524	96098	34859248
Incorrect product administration duration	98.73	56.76	26	1559	4785	34950561
Unresponsive to stimuli	86.61	56.76	36	1549	27533	34927813
Bradycardia	85.54	56.76	49	1536	75369	34879977
Blood pressure decreased	85.12	56.76	43	1542	51472	34903874
Hypotension	81.06	56.76	72	1513	221577	34733769
Seizure	73.06	56.76	50	1535	104807	34850539
Injection site pain	56.95	56.76	30	1555	38975	34916371

FDA Adverse Event Reporting System (Geriatric)

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	849.23	54.00	167	3059	9502	79731660
Incorrect product administration duration	220.32	54.00	58	3168	11964	79729198
Unresponsive to stimuli	152.93	54.00	64	3162	55724	79685438
Cardiac arrest	118.22	54.00	78	3148	172018	79569144
Bradycardia	116.98	54.00	71	3155	135486	79605676
Blood pressure decreased	106.64	54.00	60	3166	99406	79641756
Seizure	104.66	54.00	75	3151	188759	79552403
Hypotension	94.92	54.00	102	3124	440215	79300947
Dyspnoea	79.28	54.00	131	3095	856894	78884268
Chest pain	78.21	54.00	75	3151	282229	79458933
Atrioventricular block	62.77	54.00	23	3203	14018	79727144
Nausea	61.39	54.00	125	3101	957071	78784091
Loss of consciousness	60.94	54.00	52	3174	167891	79573271
Dizziness	60.29	54.00	89	3137	526352	79214810
Heart rate increased	60.07	54.00	45	3181	120679	79620483
Injection site pain	59.33	54.00	46	3180	129792	79611370
Sinus arrest	59.28	54.00	16	3210	3606	79737556
Atrioventricular block complete	55.49	54.00	22	3204	16588	79724574

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

Drug Use | Suggest Off label Use Form| |View source of the data|

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

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Adenosine receptor A2a	GPCR	P29274	AA2AR_HUMAN	AGONIST	EC50	5.89	WOMBAT-PK	CHEMBL
Adenosine receptor A1	GPCR	P30542	AA1R_HUMAN		EC50	4.40	WOMBAT-PK
Adenosine receptor A2b	GPCR	P29275	AA2BR_HUMAN		EC50	5	CHEMBL
Adenosine receptor A3	GPCR	P0DMS8	AA3R_HUMAN		Ki	5	CHEMBL
Adenosine receptor A2a	GPCR		AA2AR_RAT		Ki	6.54	CHEMBL

External reference:

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
365575	MMSL
d07131	MMSL
012689	NDDF
430242005	SNOMEDCT_US
433327005	SNOMEDCT_US
875148-45-1	SECONDARY_CAS_RN

Pharmaceutical products:

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
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
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	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	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