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

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

Stem definition	Drug id	CAS RN
serotonin receptor antagonists (5-HT3)	2357	132036-88-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: YM-060 ramosetron ibsetron hydrochloride ibsetron ramosetron hydrochloride irribow ibsetron HCl ramosetron HCl	Molecular weight: 279.34 Formula: C17H17N3O CLOGP: 2.13 LIPINSKI: 0 HAC: 4 HDO: 1 TPSA: 50.68 ALOGS: -3.61 ROTB: 2

Drug dosage:

None

ADMET properties:

Property	Value	Reference
Vd (Volume of distribution)	2.65 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	7.03 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	4.94 hours	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	0.56 %	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
azlogd74	LogD at pH 7.4	1.891		High	0.84
caco2-efflux	Caco-2 efflux ratio (BA/AB)	2.729		High	0.84
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	23.933	10^-6 cm/s	High	0.84
dh-clint	Dog hepatocyte intrinsic clearance	4.036	uL/min/10^6 cells	High	0.84
dppb	Dog plasma protein binding (% unbound)	26.950	%	High	0.84
fcs-ppb	Fetal calf serum protein binding (% unbound)	44.780	%	High	0.84
herg	hERG pIC50	5.121	pIC50	High	0.84
hh-clint	Human hepatocyte intrinsic clearance	1.102	uL/min/10^6 cells	High	0.84
hlm-clint	Human liver microsomal intrinsic clearance	4.083	uL/min/mg protein	High	0.84
hppb	Human plasma protein binding (% unbound)	23.360	%	High	0.84
kinase-safety-class	ACVR2B,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,DYRK1B,EGFR,EIF2AK3,ERBB2,GRK2,ITK,MAP3K21,MAPK10,MAPK7,MET,PDK1,PDK2,PDK4,PRKDC,TTK	22
kinase-selectivity-class	AXL,EIF2AK3	2
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	8.710		High	0.84
mh-clint	Mouse hepatocyte intrinsic clearance	35.156		High	0.84
mppb	Mouse plasma protein binding (% unbound)	25.010		High	0.84
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	14.223		High	0.84
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
pppb	Pig plasma protein binding (% unbound)	39.780	%	High	0.84
rh-clint	Rat hepatocyte intrinsic clearance	18.155	uL/min/10^6 cells	High	0.84
rh-fuinc	Rat hepatocyte fraction unbound in incubation	74.560	%	High	0.84
rppb	Rat plasma protein binding (% unbound)	19.460	%	High	0.84
solubility-dd	Solubility at pH 7.4 in DMSO	672.977	uM	High	0.84

Approvals:

Date	Agency	Company	Orphan
July 10, 1996	PMDA	Astellas

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
White blood cell count decreased	38.78	37.03	22	562	110374	42510377
Neutrophil count decreased	37.68	37.03	18	566	63397	42557354

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
Platelet count decreased	69.07	37.26	40	1326	230403	110357530
White blood cell count decreased	63.94	37.26	38	1328	229352	110358581
Neutrophil count decreased	58.79	37.26	29	1337	120912	110467021

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
MeSH PA	D000932	Antiemetics
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D005765	Gastrointestinal Agents
MeSH PA	D012702	Serotonin Antagonists
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018490	Serotonin Agents
CHEBI has role	CHEBI:53784	antispasmodic drug
CHEBI has role	CHEBI:35610	antineoplastic agent
CHEBI has role	CHEBI:50919	antiemetic

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

Disease	Relation	SNOMED_ID	DOID
Irritable bowel syndrome with diarrhea	indication	197125005

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.88	acidic
pKa2	5.69	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
5-hydroxytryptamine receptor 3A	Ion channel	P46098	5HT3A_HUMAN	ANTAGONIST	Ki	10.22		CHEMBL	SCIENTIFIC LITERATURE

External reference:

ID	Source
D02016	KEGG_DRUG
C0526950	UMLSCUI
CHEBI:135156	CHEBI
CHEMBL1643895	ChEMBL_ID
CHEMBL3181841	ChEMBL_ID
DB09290	DRUGBANK_ID
C071315	MESH_SUPPLEMENTAL_RECORD_UI
108000	PUBCHEM_CID
2301	IUPHAR_LIGAND_ID
7161	INN_ID
132907-72-3	SECONDARY_CAS_RN
7ZRO0SC54Y	UNII
010967	NDDF
010968	NDDF
7ZRO0SC54Y	INXIGHT DRUGS

Pharmaceutical products:

None