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

Stem definition	Drug id	CAS RN
vasodilators	1873	57149-07-2

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

BM-15275
KT-611
naftopidil
avishot
flivas
naftopil
naftopidil hydrochloride
naftopidil dihydrochloride
naftopidil HCl

Molecular weight: 392.50
Formula: C24H28N2O3
CLOGP: 4.24
LIPINSKI: 0
HAC: 5
HDO: 1
TPSA: 45.17
ALOGS: -3.75
ROTB: 7

Drug dosage:

None

ADMET properties:

Property	Value	Reference
CL (Clearance)	11 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)	3.30 hours	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.11 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
BA (Bioavailability)	20 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	ACVR2A,ACVR2B,AKT1,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1,TTK	49
kinase-selectivity-class	AXL,BRAF,ERBB2,GRK2,PDK4,PIK3CB,PIK3CD,SIK2	8
pfas-class	PFAS structural alert (1 = True, 0 = False)	0

Approvals:

Date	Agency	Company	Orphan
Dec. 25, 1998	PMDA	Asahi Kasei

FDA Adverse Event Reporting System (Female)

None

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
Interstitial lung disease	73.44	27.80	42	1542	78420	42541331
Cerebral infarction	50.07	27.80	24	1560	31145	42588606
Urinary retention	45.96	27.80	25	1559	42189	42577562
Hepatic function abnormal	41.30	27.80	25	1559	51542	42568209
Platelet count decreased	30.01	27.80	31	1553	138550	42481201
Osteonecrosis of jaw	28.55	27.80	14	1570	19035	42600716

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
Interstitial lung disease	86.75	31.64	41	1490	139293	110448475
Cerebral infarction	61.13	31.64	24	1507	51814	110535954
Hepatic function abnormal	51.59	31.64	25	1506	89270	110498498
Urinary retention	51.07	31.64	23	1508	69660	110518108
Platelet count decreased	38.42	31.64	29	1502	230414	110357354
Pneumonia aspiration	35.94	31.64	19	1512	81214	110506554

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
MeSH PA	D000077264	Calcium-Regulating Hormones and Agents
MeSH PA	D000317	Adrenergic alpha-Antagonists
MeSH PA	D000959	Antihypertensive Agents
MeSH PA	D002121	Calcium Channel Blockers
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D006401	Hematologic Agents
MeSH PA	D010975	Platelet Aggregation Inhibitors
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018663	Adrenergic Agents
MeSH PA	D018674	Adrenergic Antagonists
MeSH PA	D049990	Membrane Transport Modulators

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

Disease	Relation	SNOMED_ID	DOID
Benign prostatic hyperplasia	indication	266569009

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.57	Basic
pKa2	0.4	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
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN	ANTAGONIST	Ki	8.43		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN	ANTAGONIST	Ki	8.92		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN	ANTAGONIST	Ki	7.70		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Beta-2 adrenergic receptor	GPCR		ADRB2_CANFA		Ki	6		CHEMBL
Adrenergic receptor alpha-2	GPCR		ADA2B_RAT ADA2C_RAT ADA2A_RAT		Ki	5.80		CHEMBL
Adrenergic receptor alpha-1	GPCR		ADA1B_RAT ADA1D_RAT ADA1A_RAT		Ki	7.41		CHEMBL

External reference:

ID	Source
D01674	KEGG_DRUG
C0083701	UMLSCUI
CHEBI:31891	CHEBI
CHEMBL142635	ChEMBL_ID
DB12092	DRUGBANK_ID
C064357	MESH_SUPPLEMENTAL_RECORD_UI
4418	PUBCHEM_CID
5589	INN_ID
R9PHW59SFN	UNII
CHEMBL1257069	ChEMBL_ID
57149-08-3	SECONDARY_CAS_RN
R9PHW59SFN	INXIGHT DRUGS

Pharmaceutical products:

None