nefazodone

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Ask DrugCentral helps you explore drug properties, biological targets, and indications using natural language. Sample questions offer starting points, and linked drug cards let you check the underlying records.

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.10 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	18.24 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	20 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	0.51 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	7.50 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.01 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.20 hours	Lombardo F, Berellini G, Obach RS

Property	Description	Value	Unit	Confidence	Similarity
azlogd74	LogD at pH 7.4	4.082		High	1
caco2-efflux	Caco-2 efflux ratio (BA/AB)	1.409		High	1
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	24.946	10^-6 cm/s	High	1
dh-clint	Dog hepatocyte intrinsic clearance	46.881	uL/min/10^6 cells	High	1
dppb	Dog plasma protein binding (% unbound)	0.970	%	High	1
fcs-ppb	Fetal calf serum protein binding (% unbound)	1.560	%	High	1
herg	hERG pIC50	5.536	pIC50	High	1
hh-clint	Human hepatocyte intrinsic clearance	138.357	uL/min/10^6 cells	High	1
hlm-clint	Human liver microsomal intrinsic clearance	300.608	uL/min/mg protein	High	1
hppb	Human plasma protein binding (% unbound)	0.870	%	High	1
kinase-safety-class	ACVR2B,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPKAPK2,MET,NTRK2,PDK2,PDK4,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1,TTK	38
kinase-selectivity-class	AXL,EIF2AK3,GRK2,PDK4,SIK2	5
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	0.741		High	1
mh-clint	Mouse hepatocyte intrinsic clearance	253.513		High	1
mppb	Mouse plasma protein binding (% unbound)	1.230		High	1
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	3.381		High	1
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
pld-class	Phospholipidosis risk class (1 = positive, 0 = negative)	1		High	1
pppb	Pig plasma protein binding (% unbound)	1.840	%	High	1
rh-clint	Rat hepatocyte intrinsic clearance	341.979	uL/min/10^6 cells	High	1
rh-fuinc	Rat hepatocyte fraction unbound in incubation	13.170	%	High	1
rppb	Rat plasma protein binding (% unbound)	1.130	%	High	1
solubility-dd	Solubility at pH 7.4 in DMSO	35.481	uM	High	1

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
Intentional overdose	46.50	36.22	19	512	132482	110456286
Drug hypersensitivity	41.17	36.22	26	505	454064	110134704

Source	Code	Description
ATC	N06AX06	NERVOUS SYSTEM PSYCHOANALEPTICS ANTIDEPRESSANTS Other antidepressants
MeSH PA	D000068760	Serotonin and Noradrenaline Reuptake Inhibitors
MeSH PA	D000928	Antidepressive Agents
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D011619	Psychotropic Drugs
MeSH PA	D012702	Serotonin Antagonists
MeSH PA	D014179	Neurotransmitter Uptake Inhibitors
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018490	Serotonin Agents
MeSH PA	D018687	Antidepressive Agents, Second-Generation
MeSH PA	D049990	Membrane Transport Modulators
MeSH PA	D058830	Serotonin 5-HT2 Receptor Antagonists
FDA EPC	N0000175696	Serotonin Reuptake Inhibitor
CHEBI has role	CHEBI:35469	antidepressant
CHEBI has role	CHEBI:35480	analgesic
CHEBI has role	CHEBI:37890	α-adrenergic antagonist
CHEBI has role	CHEBI:48279	serotonergic antagonist
CHEBI has role	CHEBI:50949	serotonin uptake inhibitor

Disease	Relation	SNOMED_ID	DOID
Major depressive disorder	indication	370143000
Bipolar affective disorder, current episode depression	off-label use	191627008	DOID:3312
Suicidal thoughts	contraindication	6471006
Myocardial infarction	contraindication	22298006	DOID:5844
Hypovolemia	contraindication	28560003
Dehydration	contraindication	34095006
Upper gastrointestinal hemorrhage	contraindication	37372002
Low blood pressure	contraindication	45007003
Disorder of cardiovascular system	contraindication	49601007	DOID:1287
Cerebrovascular disease	contraindication	62914000	DOID:6713
Substance abuse	contraindication	66214007
Epilepsy	contraindication	84757009	DOID:1826
Liver function tests abnormal	contraindication	166603001
Angina pectoris	contraindication	194828000
Cerebrovascular accident	contraindication	230690007
Mania	contraindication	231494001
Disease of liver	contraindication	235856003	DOID:409

Ask DrugCentral

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General architecture

Using the assistant

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

Description:

Drug dosage:

ADMET properties:

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Approvals:

FDA Adverse Event Reporting System (Female)

FDA Adverse Event Reporting System (Male)

FDA Adverse Event Reporting System (Geriatric)

FDA Adverse Event Reporting System (Pediatric)

Pharmacologic Action:

Related Drugs by ATC class:

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

🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

Orange Book patent data (new drug applications)

Orange Book exclusivity data (new drug applications)

Bioactivity Summary:

External reference:

Pharmaceutical products:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN	INHIBITOR	Kd	6.70	WOMBAT-PK	CHEMBL
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	ANTAGONIST	Ki	8	WOMBAT-PK	CHEMBL
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN	INHIBITOR	Kd	6.44	WOMBAT-PK	CHEMBL
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	5.86	CHEMBL
Cytochrome P450 3A4	Enzyme	P08684	CP3A4_HUMAN	INHIBITOR	Ki	6	IUPHAR
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	7.10	WOMBAT-PK
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	7.14	PDSP
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	5.95	CHEMBL
5-hydroxytryptamine receptor 7	GPCR	P34969	5HT7R_HUMAN		Ki	7.15	CHEMBL
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	7.79	WOMBAT-PK
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	6.64	WOMBAT-PK
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	6.42	CHEMBL
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN		Ki	6.43	WOMBAT-PK
5-hydroxytryptamine receptor 1B	GPCR	P28222	5HT1B_HUMAN		Ki	6.58	CHEMBL
5-hydroxytryptamine receptor 1D	GPCR	P28221	5HT1D_HUMAN		Ki	6.92	CHEMBL
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	6.45	CHEMBL
Sodium-dependent dopamine transporter	Transporter	Q01959	SC6A3_HUMAN		Kd	6.44	WOMBAT-PK
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN		Ki	6.49	CHEMBL
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN		Ki	6.35	CHEMBL
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN		Ki	6.24	CHEMBL
Acetylcholinesterase	Enzyme	P22303	ACES_HUMAN		IC50	5.98	CHEMBL
Bile salt export pump	Transporter	O95342	ABCBB_HUMAN		IC50	5.38	CHEMBL
5-hydroxytryptamine receptor 5A	GPCR	P47898	5HT5A_HUMAN		Ki	5.96	CHEMBL
Translocator protein	Transporter	P30536	TSPO_HUMAN		Ki	5.70	CHEMBL
Transmembrane protein 97	Enzyme	Q5BJF2	TMM97_HUMAN		Ki	6.65	CHEMBL
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	6.15	CHEMBL
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN		Ki	6.75	WOMBAT-PK
5-hydroxytryptamine receptor 1A	GPCR		5HT1A_RAT		Ki	7.28	CHEMBL
Sodium-dependent serotonin transporter	Transporter		SC6A4_RAT		Ki	6.86	CHEMBL
Sodium-dependent dopamine transporter	Transporter		SC6A3_RAT		Ki	5.62	CHEMBL
5-hydroxytryptamine receptor 2A	GPCR		5HT2A_RAT		Ki	8.15	CHEMBL
Transporter	Transporter		Q9WTR4_RAT		Ki	6.24	CHEMBL
Transporter	Transporter		Q63380_RAT		Ki	6.26	CHEMBL
Bile salt export pump	Transporter		ABCBB_RAT		IC50	4.76	CHEMBL

ID	Source
4020893	VUID
N0000148387	NUI
D00819	KEGG_DRUG
82752-99-6	SECONDARY_CAS_RN
4020893	VANDF
C0068485	UMLSCUI
CHEBI:7494	CHEBI
CHEMBL623	ChEMBL_ID
CHEMBL1200492	ChEMBL_ID
DB01149	DRUGBANK_ID
C051752	MESH_SUPPLEMENTAL_RECORD_UI
7247	IUPHAR_LIGAND_ID
5432	INN_ID
59H4FCV1TF	UNII
4449	PUBCHEM_CID
151679	RXNORM
1633	MMSL
47455	MMSL
5160	MMSL
d03808	MMSL
005051	NDDF
005052	NDDF
108435006	SNOMEDCT_US
108436007	SNOMEDCT_US
372491002	SNOMEDCT_US
A1EAZ	PDB_CHEM_ID
59H4FCV1TF	INXIGHT DRUGS

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Nefazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-1024	TABLET	100 mg	ORAL	ANDA	32 sections
Nefazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-1024	TABLET	100 mg	ORAL	ANDA	32 sections
Nefazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-1025	TABLET	200 mg	ORAL	ANDA	32 sections
Nefazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-1025	TABLET	200 mg	ORAL	ANDA	32 sections
Nefazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-1026	TABLET	250 mg	ORAL	ANDA	32 sections
Nefazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-1026	TABLET	250 mg	ORAL	ANDA	32 sections
Nefazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-7113	TABLET	150 mg	ORAL	ANDA	32 sections
Nefazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-7113	TABLET	150 mg	ORAL	ANDA	32 sections
Nefazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-7178	TABLET	50 mg	ORAL	ANDA	32 sections
Nefazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-7178	TABLET	50 mg	ORAL	ANDA	32 sections
NEFAZODONE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	16590-166	TABLET	100 mg	ORAL	ANDA	33 sections
Nefazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	21695-174	TABLET	100 mg	ORAL	ANDA	30 sections
Nefazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	21695-175	TABLET	150 mg	ORAL	ANDA	30 sections
Nefazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	21695-176	TABLET	200 mg	ORAL	ANDA	30 sections
Nefazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	21695-177	TABLET	250 mg	ORAL	ANDA	30 sections
Nefazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	63629-7046	TABLET	150 mg	ORAL	ANDA	32 sections