All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

oxprenolol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
beta-adrenoreceptor antagonists	2027	6452-71-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: oxprenolol hydrochloride oxprenolol (+/-)-Oxprenolol dl-Oxprenolol oxprenolol HCl	A beta-adrenergic antagonist used in the treatment of hypertension, angina pectoris, arrhythmias, and anxiety. Molecular weight: 265.35 Formula: C15H23NO3 CLOGP: 2.09 LIPINSKI: 0 HAC: 4 HDO: 2 TPSA: 50.72 ALOGS: -2.59 ROTB: 9 Status: OFM Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

Dose	Unit	Route
0.16	g	O
0.16	g	P

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	30.86 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	3 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	15.14 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	44 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	0.72 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	7.70 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.19 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.09 hours	Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
azlogd74	LogD at pH 7.4	0.387		High	1
caco2-efflux	Caco-2 efflux ratio (BA/AB)	0.809		High	1
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	24.889	10^-6 cm/s	High	1
dh-clint	Dog hepatocyte intrinsic clearance	39.264	uL/min/10^6 cells	High	1
dppb	Dog plasma protein binding (% unbound)	56.240	%	High	1
fcs-ppb	Fetal calf serum protein binding (% unbound)	64.960	%	High	1
herg	hERG pIC50	4.747	pIC50	High	1
hh-clint	Human hepatocyte intrinsic clearance	15.101	uL/min/10^6 cells	High	1
hlm-clint	Human liver microsomal intrinsic clearance	8.110	uL/min/mg protein	High	1
hppb	Human plasma protein binding (% unbound)	64.110	%	High	1
kinase-safety-class	ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK7,MET,MTOR,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1	40
kinase-selectivity-class	AXL,CDK4,PDK4	3
mdck-mdr1-bcrp-efflux	MDCK-MDR1-BCRP efflux ratio	0.710		High	1
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	0.955		High	1
mh-clint	Mouse hepatocyte intrinsic clearance	262.422		High	1
mppb	Mouse plasma protein binding (% unbound)	68.180		High	1
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	2.143		High	1
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
pld-class	Phospholipidosis risk class (1 = positive, 0 = negative)	0		Moderate	0.66
pppb	Pig plasma protein binding (% unbound)	71.950	%	High	1
rat-kpuu-brain	Rat brain Kpuu	0.178	%	High	1
rh-clint	Rat hepatocyte intrinsic clearance	209.411	uL/min/10^6 cells	High	1
rh-fuinc	Rat hepatocyte fraction unbound in incubation	83.960	%	High	1
rppb	Rat plasma protein binding (% unbound)	67.780	%	High	1
solubility-dd	Solubility at pH 7.4 in DMSO	941.890	uM	High	1

Approvals:

Date	Agency	Company	Orphan
None	FDA	NOVARTIS

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	C07AA02	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Beta blocking agents, non-selective
ATC	C07BA02	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS AND THIAZIDES Beta blocking agents, non-selective, and thiazides
ATC	C07CA02	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS AND OTHER DIURETICS Beta blocking agents, non-selective, and other diuretics
MeSH PA	D000319	Adrenergic beta-Antagonists
MeSH PA	D000889	Anti-Arrhythmia Agents
MeSH PA	D000959	Antihypertensive Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D011619	Psychotropic Drugs
MeSH PA	D013565	Sympatholytics
MeSH PA	D014151	Anti-Anxiety Agents
MeSH PA	D014665	Vasodilator Agents
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018663	Adrenergic Agents
MeSH PA	D018674	Adrenergic Antagonists
CHEBI has role	CHEBI:35530	β-adrenergic antagonist
CHEBI has role	CHEBI:35554	cardiovascular drug

Related Drugs by ATC class:

C07AA Beta blocking agents, non-selective 13 drugs

alprenololbopindololbupranololcarteololcloranololmepindololnadololpenbutololpindololpropranololsotaloltertatolol show all 13 →

C07BA Beta blocking agents, non-selective, and thiazides 5 drugs

metipranololnadololpropranololsotaloltimolol

C07CA Beta blocking agents, non-selective, and other diuretics 3 drugs

bopindololpenbutololpindolol

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

Disease	Relation	SNOMED_ID	DOID
Hypertensive disorder	indication	38341003	DOID:10763
Ventricular arrhythmia	indication	44103008
Anxiety	indication	48694002
Angina pectoris	indication	194828000

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.19	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])	Mechanism action	Bioact source	MoA source
Beta-1 adrenergic receptor	GPCR	P08588	ADRB1_HUMAN	ANTAGONIST	Ki	8.11		WOMBAT-PK	CHEMBL
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN	ANTAGONIST	Ki	8		WOMBAT-PK	CHEMBL
Solute carrier family 22 member 1	Transporter	O15245	S22A1_HUMAN		IC50	4.54		CHEMBL
5-hydroxytryptamine receptor 1A	GPCR		5HT1A_RAT		Ki	7.03		CHEMBL

External reference:

ID	Source
D01806	KEGG_DRUG
6452-73-9	SECONDARY_CAS_RN
C0030040	UMLSCUI
CHEBI:747559	CHEBI
CHEMBL546	ChEMBL_ID
CHEMBL1200745	ChEMBL_ID
DB01580	DRUGBANK_ID
D010096	MESH_DESCRIPTOR_UI
4631	PUBCHEM_CID
7255	IUPHAR_LIGAND_ID
2506	INN_ID
519MXN9YZR	UNII
203131	RXNORM
003463	NDDF
004748	NDDF
387583006	SNOMEDCT_US
395817005	SNOMEDCT_US
96299009	SNOMEDCT_US

Pharmaceutical products:

None