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

Stem definition	Drug id	CAS RN
serotonin receptor antagonists (5-HT3)	3931	115956-12-2

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: MDL 73,147EF dolasetron methanesulfonate hydrate dolasetron mesylate hydrate anzemet hydrate anzemet dolasetron anemet dolasetron mesylate dolasetron mesilate	Dolasetron mesylate is an antinauseant and antiemetic agent. Dolasetron mesylate and its active metabolite, hydrodolasetron (MDL 74,156), are selective serotonin 5-HT3 receptor antagonists not shown to have activity at other known serotonin receptors and with low affinity for dopamine receptors. The serotonin 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery and centrally in the chemoreceptor trigger zone of the area postrema. Molecular weight: 324.38 Formula: C19H20N2O3 CLOGP: 1.92 LIPINSKI: 0 HAC: 5 HDO: 1 TPSA: 62.40 ALOGS: -3.09 ROTB: 3 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

MDL 73,147EF
dolasetron methanesulfonate hydrate
dolasetron mesylate hydrate
anzemet hydrate
anzemet
dolasetron
anemet
dolasetron mesylate
dolasetron mesilate

Dolasetron mesylate is an antinauseant and antiemetic agent. Dolasetron mesylate and its active metabolite, hydrodolasetron (MDL 74,156), are selective serotonin 5-HT3 receptor antagonists not shown to have activity at other known serotonin receptors and with low affinity for dopamine receptors. The serotonin 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery and centrally in the chemoreceptor trigger zone of the area postrema.

Molecular weight: 324.38
Formula: C19H20N2O3
CLOGP: 1.92
LIPINSKI: 0
HAC: 5
HDO: 1
TPSA: 62.40
ALOGS: -3.09
ROTB: 3

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.20	g	O
0.10	g	P

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	4.11 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	75 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	2 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	180 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.49 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	0.13 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Sept. 11, 1997	FDA	SANOFI AVENTIS US

FDA Adverse Event Reporting System (Female)

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
Death	180.37	23.16	146	2906	374235	63111735
Disease progression	54.63	23.16	46	3006	122712	63363258
Nausea	38.23	23.16	108	2944	854363	62631607
Drug ineffective	36.46	23.16	4	3048	1044761	62441209
Neuropathy peripheral	26.65	23.16	30	3022	113637	63372333
Off label use	25.98	23.16	81	2971	674381	62811589
Flushing	25.15	23.16	24	3028	75063	63410907
Fatigue	24.14	23.16	95	2957	887933	62598037

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
Death	84.48	27.73	95	1456	397954	34557426
Off label use	29.40	27.73	60	1491	419464	34535916

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
Flushing	38.36	25.20	29	2848	88239	79653272
Death	34.58	25.20	68	2809	566446	79175065
Drug ineffective	28.53	25.20	3	2874	1080910	78660601

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	A04AA04	ALIMENTARY TRACT AND METABOLISM ANTIEMETICS AND ANTINAUSEANTS ANTIEMETICS AND ANTINAUSEANTS Serotonin (5HT3) antagonists
MeSH PA	D000932	Antiemetics
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D005765	Gastrointestinal Agents
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D058831	Serotonin 5-HT3 Receptor Antagonists
MeSH PA	D018490	Serotonin Agents
MeSH PA	D012702	Serotonin Antagonists
FDA MoA	N0000175817	Serotonin 3 Receptor Antagonists
FDA EPC	N0000175818	Serotonin-3 Receptor Antagonist

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

Disease	Relation	SNOMED_ID	DOID
Post-Operative Nausea and Vomiting	indication	1488000
Prevention of Post-Operative Nausea and Vomiting	indication
Torsades de pointes	contraindication	31722008
Hypokalemia	contraindication	43339004
Chronic heart failure	contraindication	48447003
Bradycardia	contraindication	48867003
Kidney disease	contraindication	90708001	DOID:557
Prolonged QT interval	contraindication	111975006
Hypomagnesemia	contraindication	190855004
Heart block	contraindication	233916004
Chemotherapy-induced nausea and vomiting	contraindication	236084000
Congenital long QT syndrome	contraindication	442917000
Doxorubicin Induced Cardiomyopathy	contraindication
Atrioventricular Conduction Defect	contraindication

🐶 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	7.74	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	7.70		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	5.23		WOMBAT-PK

External reference:

ID	Source
D00725	KEGG_DRUG
878143-33-0	SECONDARY_CAS_RN
4021059	VANDF
4024082	VANDF
C0209210	UMLSCUI
CHEBI:4682	CHEBI
CHEMBL2368925	ChEMBL_ID
CHEMBL2368924	ChEMBL_ID
DB00757	DRUGBANK_ID
C060344	MESH_SUPPLEMENTAL_RECORD_UI
3033818	PUBCHEM_CID
6780	INN_ID
82WI2L7Q6E	UNII
215357	RXNORM
11370	MMSL
4630	MMSL
d04214	MMSL
006880	NDDF
006881	NDDF
108421009	SNOMEDCT_US
108422002	SNOMEDCT_US
372488002	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
ANZEMET	HUMAN PRESCRIPTION DRUG LABEL	1	30698-220	TABLET, FILM COATED	50 mg	ORAL	NDA	20 sections