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

Stem definition	Drug id	CAS RN
serotonin receptor antagonists (5-HT3)	2775	89565-68-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: tropisetron navoban tropisetron hydrochloride tropisetron HCl	An indole derivative and 5-HT3 RECEPTOR antagonist that is used for the prevention of nausea and vomiting. Molecular weight: 284.36 Formula: C17H20N2O2 CLOGP: 2.88 LIPINSKI: 0 HAC: 4 HDO: 1 TPSA: 45.33 ALOGS: -2.33 ROTB: 3

Molecule

Description

Molfile Inchi Smiles

Synonyms:

tropisetron
navoban
tropisetron hydrochloride
tropisetron HCl

An indole derivative and 5-HT3 RECEPTOR antagonist that is used for the prevention of nausea and vomiting.

Molecular weight: 284.36
Formula: C17H20N2O2
CLOGP: 2.88
LIPINSKI: 0
HAC: 4
HDO: 1
TPSA: 45.33
ALOGS: -2.33
ROTB: 3

Drug dosage:

Dose	Unit	Route
5	mg	O
5	mg	P

ADMET properties:

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Property	Value	Reference
Vd (Volume of distribution)	9.70 L/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	8 %	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	66 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	5.60 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	26 mL/min/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	11 mg/mL	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.25 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1992	YEAR INTRODUCED

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
Myelosuppression	112.92	48.67	31	792	23672	63464527
Bone marrow failure	106.43	48.67	31	792	29259	63458940
Neutrophil count decreased	53.90	48.67	22	801	56384	63431815
White blood cell count decreased	51.02	48.67	28	795	139076	63349123

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FDA Adverse Event Reporting System (Male)

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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
Myelosuppression	87.47	44.19	27	703	19238	34936963
White blood cell count decreased	59.45	44.19	32	698	95413	34860788
Platelet count decreased	57.93	44.19	34	696	119683	34836518

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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
Myelosuppression	182.78	39.16	57	1677	40239	79702415
Bone marrow failure	134.50	39.16	48	1686	51059	79691595
White blood cell count decreased	106.09	39.16	60	1674	188228	79554426
Platelet count decreased	96.26	39.16	57	1677	194607	79548047
Neutrophil count decreased	87.48	39.16	42	1692	93917	79648737
Hypoproteinaemia	47.12	39.16	12	1722	4034	79738620
Pneumonia	40.78	39.16	60	1674	660186	79082468

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	A04AA03	ALIMENTARY TRACT AND METABOLISM ANTIEMETICS AND ANTINAUSEANTS ANTIEMETICS AND ANTINAUSEANTS Serotonin (5HT3) antagonists
CHEBI has role	CHEBI:36335	trypanocidal drugs
CHEBI has role	CHEBI:47958	muscarinic agonists
CHEBI has role	CHEBI:48279	serotonin antagonists
CHEBI has role	CHEBI:50846	Immunologic factor
CHEBI has role	CHEBI:50919	antiemetico
CHEBI has role	CHEBI:63726	neuroprotective agents
CHEBI has role	CHEBI:67079	anti-inflammatory agents
CHEBI has role	CHEBI:68494	apoptosis inhibitors
MeSH PA	D000932	Antiemetics

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

Disease	Relation	SNOMED_ID	DOID
Chemotherapy-induced nausea and vomiting	indication	236084000

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	12.91	acidic
pKa2	9.49	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	8.80	IUPHAR	IUPHAR
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	6.59	DRUG MATRIX
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	8.28	CHEMBL
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN		Ki	5.61	DRUG MATRIX
Glycine receptor subunit alpha-1	Ion channel	P23415	GLRA1_HUMAN	ANTAGONIST	Ki	4.10	IUPHAR
Glycine receptor subunit alpha-2	Ion channel	P23416	GLRA2_HUMAN	ANTAGONIST	Ki	4.90	IUPHAR
5-hydroxytryptamine receptor 4	GPCR	Q13639	5HT4R_HUMAN		Ki	6.85	WOMBAT-PK
Neuronal acetylcholine receptor subunit alpha-7	Ion channel	P36544	ACHA7_HUMAN		Ki	8.16	CHEMBL
Glycine receptor subunit beta	Ion channel	P48167	GLRB_HUMAN	ANTAGONIST	Ki	5.30	IUPHAR
Neuronal acetylcholine receptor; alpha4/beta2	Ion channel	P17787 P43681	ACHB2_HUMAN ACHA4_HUMAN		Ki	4.26	CHEMBL

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External reference:

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ID	Source
TKT	PDB_CHEM_ID
004472	NDDF
004473	NDDF
105826-92-4	SECONDARY_CAS_RN
235997	RXNORM
260	IUPHAR_LIGAND_ID
322201005	SNOMEDCT_US
395917006	SNOMEDCT_US
426339000	SNOMEDCT_US
6535	INN_ID

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Pharmaceutical products:

None