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

Stem definition	Drug id	CAS RN
serotonin receptor antagonists (5-HT3)	129	122852-42-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: alosetron alosetron hydrochloride alosetron HCl alosetron monohydrochloride GR68755	Molecular weight: 294.36 Formula: C17H18N4O CLOGP: 1.74 LIPINSKI: 0 HAC: 5 HDO: 1 TPSA: 53.92 ALOGS: -2.83 ROTB: 2 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

alosetron
alosetron hydrochloride
alosetron HCl
alosetron monohydrochloride
GR68755

Molecular weight: 294.36
Formula: C17H18N4O
CLOGP: 1.74
LIPINSKI: 0
HAC: 5
HDO: 1
TPSA: 53.92
ALOGS: -2.83
ROTB: 2

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
1	mg	O

ADMET properties:

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Property	Value	Reference
CL (Clearance)	8.70 mL/min/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	61 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	6 %	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	55 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	1.60 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	1.10 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.18 %	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.10 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
Feb. 9, 2000	FDA	PROMETHEUS LABS

FDA Adverse Event Reporting System (Female)

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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
Colitis ischaemic	156.78	43.75	29	270	10679	63478044
Constipation	59.35	43.75	26	273	224917	63263806

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FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

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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
Colitis ischaemic	122.67	45.37	24	265	15335	79728764
Constipation	56.89	45.37	25	264	283025	79461074

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	A03AE01	ALIMENTARY TRACT AND METABOLISM DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS Serotonin receptor antagonists
CHEBI has role	CHEBI:48279	serotonin antagonists
CHEBI has role	CHEBI:50919	antiemetico
CHEBI has role	CHEBI:55324	gastrointestinal drugs
FDA EPC	N0000175818	Serotonin-3 Receptor Antagonist
FDA MoA	N0000175817	Serotonin 3 Receptor Antagonists
MeSH PA	D005765	Gastrointestinal Agents
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018490	Serotonin Agents
MeSH PA	D012702	Serotonin Antagonists

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

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Disease	Relation	SNOMED_ID	DOID
Irritable bowel syndrome with diarrhea	indication	197125005
Rectal hemorrhage	contraindication	12063002
Constipation	contraindication	14760008	DOID:2089
Acute gastric ulcer with perforation	contraindication	19850005
Toxic megacolon	contraindication	28536002	DOID:1770
Crohn's disease	contraindication	34000006
Hepatic failure	contraindication	59927004
Thrombophlebitis	contraindication	64156001	DOID:3875
Colitis	contraindication	64226004	DOID:0060180
Ulcerative colitis	contraindication	64766004	DOID:8577

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	12.33	acidic
pKa2	6.11	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
5-hydroxytryptamine receptor 3A	Ion channel	P46098	5HT3A_HUMAN	ANTAGONIST	Ki	9.30	CHEMBL	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	5.64	CHEMBL
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	7.19	DRUG MATRIX
Cytochrome P450 1A2	Enzyme	P05177	CP1A2_HUMAN		IC50	6.22	DRUG MATRIX

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External reference:

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ID	Source
S7Y	PDB_CHEM_ID
008063	NDDF
008064	NDDF
116509006	SNOMEDCT_US
122852-69-1	SECONDARY_CAS_RN
13Z9HTH115	UNII
2099	PUBCHEM_CID
2296	IUPHAR_LIGAND_ID
234172	MMSL
4021194	VUID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Alosetron	HUMAN PRESCRIPTION DRUG LABEL	1	63629-2517	TABLET	0.50 mg	ORAL	ANDA	26 sections
Alosetron	HUMAN PRESCRIPTION DRUG LABEL	1	63629-2517	TABLET	0.50 mg	ORAL	ANDA	26 sections
Alosetron	HUMAN PRESCRIPTION DRUG LABEL	1	63629-2518	TABLET	1 mg	ORAL	ANDA	26 sections
Alosetron	HUMAN PRESCRIPTION DRUG LABEL	1	63629-2518	TABLET	1 mg	ORAL	ANDA	26 sections
Alosetron	HUMAN PRESCRIPTION DRUG LABEL	1	70756-701	TABLET	1 mg	ORAL	ANDA	26 sections
Alosetron	HUMAN PRESCRIPTION DRUG LABEL	1	70756-701	TABLET	1 mg	ORAL	ANDA	26 sections
Alosetron	HUMAN PRESCRIPTION DRUG LABEL	1	70756-702	TABLET	0.50 mg	ORAL	ANDA	26 sections
Alosetron	HUMAN PRESCRIPTION DRUG LABEL	1	70756-702	TABLET	0.50 mg	ORAL	ANDA	26 sections
Alosetron Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0295	TABLET	0.50 mg	ORAL	ANDA	27 sections
Alosetron Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0296	TABLET	1 mg	ORAL	ANDA	27 sections

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