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:

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

Approvals:

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

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
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
Platelet count decreased	91.12	18.13	144	19686	115978	63353214
Anaemia	89.15	18.13	246	19584	293184	63176008
Decreased appetite	87.97	18.13	222	19608	250830	63218362
Joint swelling	85.62	18.13	4	19826	327662	63141530
Constipation	80.97	18.13	201	19629	224742	63244450
Polyneuropathy	67.28	18.13	47	19783	14542	63454650
Drug intolerance	66.26	18.13	9	19821	308652	63160540
Thrombocytopenia	64.03	18.13	144	19686	151013	63318179
Mucosal inflammation	63.83	18.13	76	19754	46852	63422340
Disease progression	63.64	18.13	127	19703	122631	63346561
Abdominal pain	61.21	18.13	216	19614	293240	63175952
Diarrhoea	60.76	18.13	406	19424	714960	62754232
White blood cell count decreased	56.12	18.13	130	19700	138974	63330218
Dyspnoea	52.34	18.13	369	19461	660944	62808248
Treatment failure	50.16	18.13	3	19827	199040	63270152
Tooth erosion	49.87	18.13	14	19816	459	63468733
Malignant neoplasm progression	46.24	18.13	88	19742	82033	63387159
Pancytopenia	45.17	18.13	96	19734	96837	63372355
Swelling	44.94	18.13	15	19815	275363	63193829
Hypokalaemia	44.05	18.13	99	19731	103705	63365487
Maternal exposure during pregnancy	43.62	18.13	8	19822	220054	63249138
Condition aggravated	41.20	18.13	39	19791	402178	63067014
Drug hypersensitivity	41.07	18.13	23	19807	310664	63158528
Flushing	40.47	18.13	79	19751	75008	63394184
Product dose omission issue	39.58	18.13	12	19818	234301	63234891
Musculoskeletal stiffness	38.15	18.13	6	19824	184612	63284580
Product use issue	37.78	18.13	11	19819	220509	63248683
Respiratory depth decreased	37.31	18.13	7	19823	33	63469159
Chest discomfort	37.11	18.13	96	19734	109873	63359319
Pulpitis dental	36.74	18.13	13	19817	915	63468277
Breast cancer metastatic	36.13	18.13	30	19800	11988	63457204
Neuropathy peripheral	36.09	18.13	97	19733	113570	63355622
Bone marrow failure	35.87	18.13	45	19785	29245	63439947
Weight increased	34.90	18.13	19	19811	260773	63208419
Lymphoedema	34.76	18.13	29	19801	11663	63457529
Bone pain	33.82	18.13	61	19769	54580	63414612
Erythema	33.71	18.13	126	19704	175625	63293567
Stomatitis	33.16	18.13	107	19723	138618	63330574
Toxicity to various agents	33.10	18.13	18	19812	247232	63221960
Asthenia	31.94	18.13	217	19613	383387	63085805
Periodontitis	31.67	18.13	17	19813	3286	63465906
Ileus	30.88	18.13	30	19800	14695	63454497
Abdominal discomfort	30.68	18.13	33	19797	320852	63148340
Sepsis	29.54	18.13	110	19720	153013	63316179
Palmar-plantar erythrodysaesthesia syndrome	29.21	18.13	36	19794	22979	63446213
Therapeutic product effect incomplete	28.39	18.13	3	19827	125053	63344139
Arthralgia	28.19	18.13	88	19742	569622	62899570
Peripheral swelling	28.13	18.13	25	19805	265917	63203275
Tumour pain	27.88	18.13	12	19818	1425	63467767
Disseminated intravascular coagulation	27.80	18.13	32	19798	19019	63450173
Hepatic function abnormal	27.63	18.13	45	19785	37097	63432095
Venous thrombosis limb	27.50	18.13	15	19815	2993	63466199
Cytomegalovirus test positive	27.46	18.13	15	19815	3003	63466189
Fall	26.96	18.13	51	19779	392283	63076909
Sinusitis	26.87	18.13	19	19811	226634	63242558
Chronic hepatitis B	26.30	18.13	8	19822	349	63468843
Systemic infection	26.25	18.13	17	19813	4643	63464549
Tumour lysis syndrome	26.11	18.13	22	19808	8968	63460224
Mucosal dryness	25.97	18.13	14	19816	2730	63466462
Tachycardia	25.44	18.13	88	19742	118068	63351124
Ejection fraction decreased	25.28	18.13	33	19797	22299	63446893
Interstitial lung disease	25.09	18.13	58	19772	61850	63407342
Oral candidiasis	24.74	18.13	33	19797	22765	63446427
Serotonin syndrome	24.46	18.13	37	19793	28645	63440547
Nasopharyngitis	24.46	18.13	26	19804	254231	63214961
Hepatic enzyme increased	23.93	18.13	17	19813	202311	63266881
Metastases to liver	23.81	18.13	33	19797	23606	63445586
Dysgeusia	23.78	18.13	48	19782	46662	63422530
Pericarditis	23.58	18.13	6	19824	131573	63337619
Cachexia	23.08	18.13	17	19813	5709	63463483
Exposure during pregnancy	22.81	18.13	10	19820	155537	63313655
Cough	22.80	18.13	163	19667	292580	63176612
Dysphagia	22.69	18.13	70	19760	88515	63380677
Discomfort	22.66	18.13	12	19818	167362	63301830
Onychalgia	21.82	18.13	9	19821	962	63468230
Mitral valve disease	21.66	18.13	12	19818	2468	63466724
Oesophagitis	21.55	18.13	25	19805	14983	63454209
Subileus	21.43	18.13	13	19817	3166	63466026
Sensation of foreign body	21.21	18.13	15	19815	4730	63464462
Acute interstitial pneumonitis	20.97	18.13	8	19822	696	63468496
Aortitis	20.84	18.13	9	19821	1078	63468114
Asthma	20.70	18.13	7	19823	127554	63341638
Gastrointestinal submucosal tumour	20.66	18.13	4	19826	23	63469169
Mucosal disorder	20.34	18.13	11	19819	2158	63467034
Acute myeloid leukaemia recurrent	20.33	18.13	10	19820	1613	63467579
Wound	20.26	18.13	13	19817	163250	63305942
Epistaxis	20.07	18.13	59	19771	72666	63396526
Neutropenic sepsis	19.72	18.13	25	19805	16413	63452779
Gastroenteropancreatic neuroendocrine tumour disease	19.62	18.13	4	19826	31	63469161
Cytopenia	19.53	18.13	21	19809	11580	63457612
Pleural effusion	18.84	18.13	68	19762	93142	63376050
Tachypnoea	18.71	18.13	25	19805	17277	63451915
Ascites	18.57	18.13	40	19790	40688	63428504

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
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
Stomatitis	53.33	16.65	79	15378	42435	34899039
Mucosal disorder	52.73	16.65	22	15435	1704	34939770
Nausea	52.21	16.65	291	15166	339617	34601857
Thrombocytopenia	49.80	16.65	167	15290	156080	34785394
Decreased appetite	46.25	16.65	170	15287	166222	34775252
General physical health deterioration	45.27	16.65	142	15315	128127	34813347
Sepsis	43.65	16.65	167	15290	166394	34775080
Disseminated intravascular coagulation	41.97	16.65	50	15407	21766	34919708
Diarrhoea	41.97	16.65	305	15152	389607	34551867
Interstitial lung disease	41.33	16.65	90	15367	65192	34876282
Oesophagitis	40.80	16.65	39	15418	13222	34928252
Polyneuropathy	38.78	16.65	40	15417	14856	34926618
Constipation	38.07	16.65	140	15317	136842	34804632
Product dose omission issue	36.21	16.65	5	15452	119706	34821768
Fall	35.55	16.65	23	15434	202862	34738612
Toxicity to various agents	29.64	16.65	27	15430	200335	34741139
Aortitis	29.59	16.65	10	15447	430	34941044
Pneumonia	28.84	16.65	265	15192	362362	34579112
Mucosal inflammation	28.83	16.65	57	15400	38565	34902909
Antithrombin III decreased	28.14	16.65	9	15448	325	34941149
Systemic infection	27.72	16.65	21	15436	5191	34936283
Blast cell count increased	27.19	16.65	12	15445	1066	34940408
Drug therapeutic incompatibility	27.12	16.65	7	15450	115	34941359
Arthralgia	26.24	16.65	22	15435	170019	34771455
Fluid imbalance	25.91	16.65	8	15449	257	34941217
Radiation oesophagitis	25.69	16.65	9	15448	432	34941042
Nail bed inflammation	24.50	16.65	7	15450	171	34941303
Tumour perforation	24.21	16.65	8	15449	321	34941153
Non-small cell lung cancer	23.48	16.65	17	15440	3923	34937551
Myocardial infarction	22.19	16.65	13	15444	121072	34820402
Subclavian artery occlusion	21.90	16.65	6	15451	125	34941349
Autoimmune colitis	21.50	16.65	10	15447	1004	34940470
Laryngeal leukoplakia	21.22	16.65	5	15452	55	34941419
Pseudomonal bacteraemia	20.92	16.65	11	15446	1438	34940036
Palmar-plantar erythrodysaesthesia syndrome	20.74	16.65	31	15426	16764	34924710
Dermatitis acneiform	20.56	16.65	19	15438	6170	34935304
Blood lactate dehydrogenase increased	19.71	16.65	36	15421	22954	34918520
Alopecia	19.46	16.65	37	15420	24318	34917156
Engraftment syndrome	18.59	16.65	9	15448	988	34940486
Urinary tract infection pseudomonal	18.56	16.65	9	15448	992	34940482
Hepatic function abnormal	18.35	16.65	52	15405	44311	34897163
Proteinuria	18.32	16.65	31	15426	18611	34922863
Disease progression	18.13	16.65	95	15362	107982	34833492
COVID-19	17.86	16.65	6	15451	77544	34863930
Flushing	17.51	16.65	42	15415	32378	34909096
Acute graft versus host disease in skin	17.34	16.65	16	15441	5185	34936289
Peripheral sensory neuropathy	17.31	16.65	18	15439	6742	34934732
Large intestine perforation	17.20	16.65	20	15437	8483	34932991
Joint swelling	16.97	16.65	3	15454	59887	34881587

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
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
Anaemia	123.16	15.15	407	29565	444608	79269808
Polyneuropathy	105.45	15.15	81	29891	24070	79690346
Thrombocytopenia	102.20	15.15	273	29699	264986	79449430
General physical health deterioration	93.91	15.15	271	29701	274967	79439449
Decreased appetite	90.01	15.15	308	29664	342110	79372306
Joint swelling	85.29	15.15	6	29966	288640	79425776
Mucosal inflammation	82.90	15.15	121	29851	75459	79638957
Constipation	82.75	15.15	264	29708	282786	79431630
Diarrhoea	82.63	15.15	589	29383	879900	78834516
Drug intolerance	79.48	15.15	5	29967	264114	79450302
Sepsis	79.39	15.15	252	29720	269176	79445240
Completed suicide	79.22	15.15	3	29969	245764	79468652
Oesophagitis	69.81	15.15	64	29908	24225	79690191
Arthralgia	66.74	15.15	70	29902	571733	79142683
Product dose omission issue	63.13	15.15	9	29963	247528	79466888
Interstitial lung disease	59.47	15.15	131	29841	112469	79601947
Disseminated intravascular coagulation	58.88	15.15	70	29902	35772	79678644
Fall	58.81	15.15	58	29914	487571	79226845
Toxicity to various agents	58.28	15.15	44	29928	421496	79292920
Flushing	57.55	15.15	112	29860	88156	79626260
Systemic infection	54.56	15.15	38	29934	9714	79704702
Pulpitis dental	54.54	15.15	20	29952	1293	79713123
Hypokalaemia	54.12	15.15	147	29825	143893	79570523
Mucosal disorder	52.71	15.15	26	29946	3502	79710914
Stomatitis	52.39	15.15	147	29825	146610	79567806
Malignant neoplasm progression	51.30	15.15	139	29833	135851	79578565
Pancytopenia	50.57	15.15	157	29815	165588	79548828
Drug hypersensitivity	48.42	15.15	26	29946	298890	79415526
Aortitis	48.32	15.15	19	29953	1488	79712928
Treatment failure	46.38	15.15	5	29967	170481	79543935
Peripheral swelling	45.84	15.15	22	29950	269595	79444821
Dyspnoea	45.67	15.15	507	29465	856518	78857898
Bone marrow failure	45.06	15.15	74	29898	51033	79663383
Tooth erosion	44.88	15.15	13	29959	395	79714021
Hepatic function abnormal	44.32	15.15	90	29882	73017	79641399
Therapeutic product effect incomplete	41.65	15.15	3	29969	141642	79572774
Ileus	41.10	15.15	50	29922	26161	79688255
Abdominal pain	39.47	15.15	266	29706	389303	79325113
Palmar-plantar erythrodysaesthesia syndrome	39.18	15.15	55	29917	33079	79681337
Musculoskeletal stiffness	36.99	15.15	10	29962	174998	79539418
Respiratory depth decreased	36.02	15.15	7	29965	33	79714383
Myocardial infarction	34.52	15.15	13	29959	184116	79530300
Nasopharyngitis	34.41	15.15	27	29945	253854	79460562
Condition aggravated	33.55	15.15	88	29884	501036	79213380
Tumour lysis syndrome	33.28	15.15	43	29929	23896	79690520
Weight increased	32.24	15.15	34	29938	277352	79437064
Pneumonia	32.12	15.15	384	29588	659862	79054554
Product use issue	31.48	15.15	20	29952	209802	79504614
Tachypnoea	30.41	15.15	48	29924	32015	79682401
Sinusitis	30.21	15.15	18	29954	195483	79518933
Enterocolitis	30.08	15.15	32	29940	14480	79699936
Disease progression	29.26	15.15	142	29830	184220	79530196
Maternal exposure during pregnancy	28.48	15.15	8	29964	136530	79577886
Dermatitis acneiform	28.07	15.15	26	29946	9967	79704449
Cytokine release syndrome	27.61	15.15	49	29923	35949	79678467
Dehydration	27.25	15.15	173	29799	248014	79466402
Neutropenic colitis	26.80	15.15	20	29952	5687	79708729
Radiation oesophagitis	26.77	15.15	10	29962	681	79713735
Large intestine perforation	26.52	15.15	30	29942	14537	79699879
Venous thrombosis limb	26.42	15.15	18	29954	4439	79709977
Periodontitis	26.28	15.15	18	29954	4478	79709938
Antithrombin III decreased	26.01	15.15	9	29963	491	79713925
Drug therapeutic incompatibility	25.94	15.15	7	29965	163	79714253
Colony stimulating factor therapy	25.60	15.15	9	29963	515	79713901
Tachycardia	25.45	15.15	133	29839	177635	79536781
Breast cancer metastatic	25.37	15.15	23	29949	8579	79705837
COVID-19	25.10	15.15	14	29958	157660	79556756
Oral candidiasis	24.91	15.15	42	29930	29586	79684830
Non-small cell lung cancer	24.88	15.15	20	29952	6340	79708076
Pneumonitis	24.75	15.15	64	29908	60796	79653620
Colitis	24.75	15.15	72	29900	73235	79641181
Peripheral sensory neuropathy	23.99	15.15	27	29945	13006	79701410
Swelling	23.60	15.15	28	29944	216683	79497733
Tumour perforation	23.54	15.15	8	29964	413	79714003
Proteinuria	23.35	15.15	43	29929	32459	79681957
Gastroenteropancreatic neuroendocrine tumour disease	23.14	15.15	5	29967	43	79714373
Blister	23.13	15.15	8	29964	119468	79594948
Tumour pain	23.11	15.15	13	29959	2286	79712130
Bacteraemia	23.04	15.15	43	29929	32781	79681635
Chronic hepatitis B	23.01	15.15	8	29964	443	79713973
Engraftment syndrome	22.90	15.15	11	29961	1398	79713018
Blast cell count increased	22.89	15.15	11	29961	1399	79713017
Neuropathy peripheral	22.53	15.15	109	29863	141196	79573220
Blood lactate dehydrogenase increased	22.30	15.15	47	29925	39123	79675293
Neutropenic sepsis	22.27	15.15	38	29934	27026	79687390
Laryngeal leukoplakia	21.95	15.15	5	29967	56	79714360
Pericarditis	21.94	15.15	6	29966	104230	79610186
Fluid imbalance	21.66	15.15	8	29964	528	79713888
Subclavian artery occlusion	21.18	15.15	6	29966	168	79714248
Febrile infection	21.00	15.15	14	29958	3332	79711084
Mobility decreased	20.70	15.15	10	29962	122165	79592251
Subileus	20.48	15.15	17	29955	5637	79708779
Pain	20.41	15.15	168	29804	703634	79010782
Onychalgia	20.38	15.15	9	29963	943	79713473
Hypoalbuminaemia	20.36	15.15	32	29940	21265	79693151
Discomfort	20.21	15.15	11	29961	125606	79588810
Dysaesthesia	19.98	15.15	17	29955	5831	79708585
Acute graft versus host disease in skin	19.74	15.15	19	29953	7639	79706777
Hepatic infection	19.62	15.15	9	29963	1031	79713385
Gastrointestinal perforation	19.27	15.15	17	29955	6120	79708296
Confusional state	18.93	15.15	59	29913	317938	79396478
C-reactive protein increased	18.78	15.15	97	29875	128930	79585486
Cystitis haemorrhagic	18.62	15.15	20	29952	9152	79705264
Autoimmune colitis	18.58	15.15	10	29962	1613	79712803
Arthritis	18.57	15.15	10	29962	114870	79599546
Chills	18.38	15.15	113	29859	160121	79554295
Lymphoedema	18.36	15.15	23	29949	12390	79702026
Cardiac failure congestive	18.23	15.15	16	29956	142386	79572030
Chest discomfort	18.20	15.15	101	29871	137943	79576473
Intracranial tumour haemorrhage	18.05	15.15	7	29965	528	79713888
Enterocolitis infectious	17.99	15.15	12	29960	2857	79711559
Stress	17.88	15.15	4	29968	79608	79634808
Nail bed inflammation	17.86	15.15	7	29965	543	79713873
Cytomegalovirus test positive	17.73	15.15	16	29956	5931	79708485
Psoriasis	17.34	15.15	6	29966	89581	79624835
Dysgeusia	17.26	15.15	54	29918	57123	79657293
Injury	17.20	15.15	4	29968	77492	79636924
Hyperaemia	17.12	15.15	12	29960	3098	79711318
Paraesthesia	16.98	15.15	119	29853	176204	79538212
Incorrect dose administered	16.92	15.15	4	29968	76626	79637790
Radiation skin injury	16.88	15.15	9	29963	1425	79712991
Restrictive cardiomyopathy	16.78	15.15	8	29964	1000	79713416
Abdominal discomfort	16.77	15.15	44	29928	250683	79463733
Capillary leak syndrome	16.77	15.15	13	29959	3912	79710504
Sensation of foreign body	16.75	15.15	15	29957	5507	79708909
Intestinal perforation	16.40	15.15	26	29946	17400	79697016
Acute myeloid leukaemia recurrent	16.21	15.15	12	29960	3371	79711045
Intentional product use issue	16.19	15.15	20	29952	152092	79562324
Wound	16.18	15.15	12	29960	116167	79598249
Erythema	16.14	15.15	141	29831	223149	79491267
Influenza	16.06	15.15	15	29957	129591	79584825
Exposure during pregnancy	16.06	15.15	9	29963	101123	79613293
Colitis ischaemic	15.98	15.15	24	29948	15335	79699081
Cerebrovascular accident	15.92	15.15	21	29951	155271	79559145
Paronychia	15.80	15.15	17	29955	7791	79706625
Mucosal dryness	15.67	15.15	12	29960	3547	79710869
Epistaxis	15.65	15.15	83	29889	111432	79602984
Malignant ascites	15.51	15.15	8	29964	1184	79713232
Taste disorder	15.44	15.15	24	29948	15799	79698617
Gastrointestinal disorder	15.32	15.15	14	29958	122191	79592225
Acute interstitial pneumonitis	15.31	15.15	8	29964	1215	79713201
Staphylococcal sepsis	15.30	15.15	23	29949	14703	79699713
Metastases to bone marrow	15.15	15.15	7	29965	815	79713601

FDA Adverse Event Reporting System (Pediatric)

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

Pharmacologic Action:

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 MoA	N0000175817	Serotonin 3 Receptor Antagonists
FDA EPC	N0000175818	Serotonin-3 Receptor Antagonist
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

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

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
Doxorubicin Induced Cardiomyopathy	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	13.79	acidic
pKa2	9.5	Basic

Orange Book patent data (new drug applications)

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

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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

External reference:

ID	Source
4020855	VUID
N0000179527	NUI
D00677	KEGG_DRUG
107007-99-8	SECONDARY_CAS_RN
4020855	VANDF
4023910	VANDF
C0061863	UMLSCUI
CHEBI:5537	CHEBI
CWB	PDB_CHEM_ID
CHEMBL289469	ChEMBL_ID
DB00889	DRUGBANK_ID
CHEMBL1237080	ChEMBL_ID
D017829	MESH_DESCRIPTOR_UI
5284566	PUBCHEM_CID
2300	IUPHAR_LIGAND_ID
6230	INN_ID
WZG3J2MCOL	UNII
142149	RXNORM
130105	MMSL
157872	MMSL
25895	MMSL
4344	MMSL
4801	MMSL
d03171	MMSL
003975	NDDF
003976	NDDF
108424001	SNOMEDCT_US
108425000	SNOMEDCT_US
372489005	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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
Granisetron Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	17478-546	INJECTION	1 mg	INTRAVENOUS	ANDA	26 sections
Granisetron Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	17478-547	INJECTION	0.10 mg	INTRAVENOUS	ANDA	26 sections
Granisetron Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	42043-390	TABLET, FILM COATED	1 mg	ORAL	ANDA	20 sections
SANCUSO	HUMAN PRESCRIPTION DRUG LABEL	1	42747-726	PATCH	3.10 mg	TRANSDERMAL	NDA	31 sections
SANCUSO	HUMAN PRESCRIPTION DRUG LABEL	1	42747-726	PATCH	3.10 mg	TRANSDERMAL	NDA	31 sections
SANCUSO	HUMAN PRESCRIPTION DRUG LABEL	1	42747-726	PATCH	3.10 mg	TRANSDERMAL	NDA	31 sections
SUSTOL	HUMAN PRESCRIPTION DRUG LABEL	1	47426-101	INJECTION	10 mg	SUBCUTANEOUS	NDA	27 sections
SUSTOL	HUMAN PRESCRIPTION DRUG LABEL	1	47426-101	INJECTION	10 mg	SUBCUTANEOUS	NDA	27 sections
SUSTOL	HUMAN PRESCRIPTION DRUG LABEL	1	47426-101	INJECTION	10 mg	SUBCUTANEOUS	NDA	27 sections
Granisetron Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	51991-735	TABLET	1 mg	ORAL	ANDA	21 sections
Granisetron Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	51991-735	TABLET	1 mg	ORAL	ANDA	21 sections
Sancuso	HUMAN PRESCRIPTION DRUG LABEL	1	54868-5985	PATCH	3.10 mg	TRANSDERMAL	NDA	26 sections
Granisetron Hydrochloride	Human Prescription Drug Label	1	55150-175	INJECTION, SOLUTION	1 mg	INTRAVENOUS	ANDA	24 sections
Granisetron Hydrochloride	Human Prescription Drug Label	1	55150-176	INJECTION, SOLUTION	4 mg	INTRAVENOUS	ANDA	24 sections
GRANISETRON HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	55648-661	INJECTION	1 mg	INTRAVENOUS	ANDA	16 sections
GRANISETRON HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	55648-661	INJECTION	1 mg	INTRAVENOUS	ANDA	16 sections
GRANISETRON HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	55648-662	INJECTION	0.10 mg	INTRAVENOUS	ANDA	16 sections
Granisetron Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	63126-331	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	ANDA	26 sections
Granisetron Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	63126-332	INJECTION, SOLUTION	1 mg	INTRAVENOUS	ANDA	22 sections
Granisetron Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	63126-333	INJECTION, SOLUTION	4 mg	INTRAVENOUS	ANDA	22 sections
Granisetron	HUMAN PRESCRIPTION DRUG LABEL	1	63323-317	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	ANDA	25 sections
Granisetron	HUMAN PRESCRIPTION DRUG LABEL	1	63323-317	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