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

Stem definition	Drug id	CAS RN
serotonin receptor antagonists (5-HT3)	1329	109889-09-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: granisetron monohydrochloride BRL-43694 granisetron sancuso kevatril granisetron hydrochloride granisetron HCl kytril	A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients. Molecular weight: 312.42 Formula: C18H24N4O CLOGP: 1.84 LIPINSKI: 0 HAC: 5 HDO: 1 TPSA: 50.16 ALOGS: -2.86 ROTB: 2 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

granisetron monohydrochloride
BRL-43694
granisetron
sancuso
kevatril
granisetron hydrochloride
granisetron HCl
kytril

A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients.

Molecular weight: 312.42
Formula: C18H24N4O
CLOGP: 1.84
LIPINSKI: 0
HAC: 5
HDO: 1
TPSA: 50.16
ALOGS: -2.86
ROTB: 2

Status: OFP

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

Drug dosage:

Dose	Unit	Route
2	mg	O
3	mg	P
3.10	mg	TD

ADMET properties:

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Property	Value	Reference
CL (Clearance)	9.10 mL/min/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	60 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	5.20 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	3.70 L/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	11 %	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	100 mg/mL	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.35 %	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.03 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

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Date	Agency	Company
April 20, 2012	EMA	Kyowa Kirin Holdings B.V.
Dec. 29, 1993	FDA	ROCHE
Feb. 25, 2022	PMDA	Taiyo Pharma Co Ltd

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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
Febrile neutropenia	540.45	18.13	378	19452	118071	63351121
Neutropenia	228.45	18.13	277	19553	174728	63294464
Drug ineffective	217.61	18.13	34	19796	1044731	62424461
Nausea	196.54	18.13	647	19183	853824	62615368
Neutrophil count decreased	157.88	18.13	135	19695	56271	63412921
Vomiting	129.91	18.13	426	19404	559191	62910001
Pyrexia	129.37	18.13	380	19450	470098	62999094
Death	123.20	18.13	323	19507	374058	63095134
Leukopenia	106.60	18.13	126	19704	77164	63392028
General physical health deterioration	95.89	18.13	201	19629	201201	63267991

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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
Febrile neutropenia	329.31	16.65	351	15106	136498	34804976
Drug ineffective	119.63	16.65	28	15429	456723	34484751
Neutrophil count decreased	108.33	16.65	123	15334	50981	34890493
Pyrexia	87.11	16.65	333	15124	332680	34608794
White blood cell count decreased	76.51	16.65	145	15312	95300	34846174
Neutropenia	75.47	16.65	194	15263	156584	34784890
Platelet count decreased	72.52	16.65	162	15295	119555	34821919
Leukopenia	62.55	16.65	105	15352	62751	34878723
Anaemia	55.67	16.65	227	15230	233108	34708366
Vomiting	53.72	16.65	234	15223	247387	34694087

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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
Febrile neutropenia	810.28	15.15	679	29293	230320	79484096
Neutrophil count decreased	250.19	15.15	237	29735	93722	79620694
Drug ineffective	245.38	15.15	54	29918	1080859	78633557
Neutropenia	231.48	15.15	399	29573	287311	79427105
Nausea	187.94	15.15	782	29190	956414	78758002
Pyrexia	185.27	15.15	617	29355	678092	79036324
Platelet count decreased	177.82	15.15	286	29686	194378	79520038
Leukopenia	140.42	15.15	195	29777	116318	79598098
Vomiting	136.47	15.15	552	29420	665276	79049140
White blood cell count decreased	134.29	15.15	248	29724	188040	79526376

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FDA Adverse Event Reporting System (Pediatric)

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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
Small for dates baby	12.13	12.06	5	3	2804	86980

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Pharmacologic Action:

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Source	Code	Description
ATC	A04AA02	ALIMENTARY TRACT AND METABOLISM ANTIEMETICS AND ANTINAUSEANTS ANTIEMETICS AND ANTINAUSEANTS Serotonin (5HT3) antagonists
CHEBI has role	CHEBI:48279	serotonin antagonists
CHEBI has role	CHEBI:50919	antiemetico
FDA EPC	N0000175818	Serotonin-3 Receptor Antagonist
FDA MoA	N0000175817	Serotonin 3 Receptor 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

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

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Disease	Relation	SNOMED_ID
Post-Operative Nausea and Vomiting	indication	1488000
Chemotherapy-induced nausea and vomiting	indication	236084000
Prevention of Post-Operative Nausea and Vomiting	indication
Prevention of Radiation-Induced Nausea and Vomiting	indication
Prolonged-Severe Nausea and Vomiting	off-label use
Hypokalemia	contraindication	43339004
Conduction disorder of the heart	contraindication	44808001
Prolonged QT interval	contraindication	111975006
Hypomagnesemia	contraindication	190855004
Congenital long QT syndrome	contraindication	442917000

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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	13.79	acidic
pKa2	9.5	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
10MG/0.4ML (10MG/0.4ML)	SUSTOL	HERON THERAPS INC	N022445	Aug. 9, 2016	RX	INJECTION, EXTENDED RELEASE	SUBCUTANEOUS	10357570	Sept. 28, 2024	PROPHYLACTIC TREATMENT OF NAUSEA AND VOMITING, INCLUDING PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED CHEMOTHERAPY
10MG/0.4ML (10MG/0.4ML)	SUSTOL	HERON THERAPS INC	N022445	Aug. 9, 2016	RX	INJECTION, EXTENDED RELEASE	SUBCUTANEOUS	8252305	Sept. 28, 2024	TREATMENT OR PREVENTION OF NAUSEA AND VOMITING
10MG/0.4ML (10MG/0.4ML)	SUSTOL	HERON THERAPS INC	N022445	Aug. 9, 2016	RX	INJECTION, EXTENDED RELEASE	SUBCUTANEOUS	9913910	Sept. 28, 2024	PROPHYLACTIC TREATMENT OF NAUSEA AND VOMITING, INCLUDING PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED CHEMOTHERAPY
3.1MG/24HR	SANCUSO	KYOWA KIRIN	N022198	Sept. 12, 2008	RX	FILM, EXTENDED RELEASE	TRANSDERMAL	7608282	Jan. 22, 2025	USE OF GRANISETRON TRANSDERMAL SYSTEM TO TREAT/PREVENT CHEMOTHERAPY INDUCED NAUSEA AND VOMITING

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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	8.70	WOMBAT-PK	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	5.43	WOMBAT-PK
Solute carrier family 22 member 2	Transporter	O15244	S22A2_HUMAN		IC50	5.37	CHEMBL
Multidrug and toxin extrusion protein 1	Transporter	Q96FL8	S47A1_HUMAN		IC50	5.30	CHEMBL
Neuronal acetylcholine receptor; alpha4/beta2	Ion channel	P17787 P43681	ACHB2_HUMAN ACHA4_HUMAN		Ki	4.42	CHEMBL
5-hydroxytryptamine receptor 3B	Ion channel	O95264	5HT3B_HUMAN		Ki	8.80	CHEMBL
Neuronal acetylcholine receptor subunit alpha-3	Ion channel	P32297	ACHA3_HUMAN		Ki	4.17	CHEMBL
Serotonin 3 (5-HT3) receptor	Ion channel		5HT3A_RAT 5HT3B_RAT		Ki	9.46	CHEMBL
5-hydroxytryptamine receptor 3A	Ion channel		5HT3A_CAVPO		Ki	8.40	CHEMBL

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External reference:

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ID	Source
CWB	PDB_CHEM_ID
003975	NDDF
003976	NDDF
107007-99-8	SECONDARY_CAS_RN
108424001	SNOMEDCT_US
108425000	SNOMEDCT_US
130105	MMSL
142149	RXNORM
157872	MMSL
2300	IUPHAR_LIGAND_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Granisetron	HUMAN PRESCRIPTION DRUG LABEL	1	63323-317	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	ANDA	25 sections
Granisetron	HUMAN PRESCRIPTION DRUG LABEL	1	63323-317	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	ANDA	25 sections
Granisetron	HUMAN PRESCRIPTION DRUG LABEL	1	63323-318	INJECTION, SOLUTION	1 mg	INTRAVENOUS	ANDA	25 sections
Granisetron Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0143	TABLET	1 mg	ORAL	ANDA	19 sections
Granisetron Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9744	INJECTION	1 mg	INTRAVENOUS	ANDA	25 sections
Granisetron Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9744	INJECTION	1 mg	INTRAVENOUS	ANDA	25 sections
Granisetron Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9745	INJECTION	1 mg	INTRAVENOUS	ANDA	25 sections
Granisetron Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9745	INJECTION	1 mg	INTRAVENOUS	ANDA	25 sections
Granisetron Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	17478-546	INJECTION	1 mg	INTRAVENOUS	ANDA	26 sections
Granisetron Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	17478-546	INJECTION	1 mg	INTRAVENOUS	ANDA	26 sections

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