granisetron 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
serotonin receptor antagonists (5-HT3) 1329 109889-09-0

Description:

MoleculeDescription

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:

DoseUnitRoute
2 mg O
3 mg P
3.10 mg TD

ADMET properties:

PropertyValueReference
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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,IRAK1,ITK,MET,NTRK2,PDK1,PDK2,PDK4,PRKDC 18
kinase-selectivity-class CAMK2D,EIF2AK3 2
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 High 1

Approvals:

DateAgencyCompanyOrphan
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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Febrile neutropenia 768.28 18.65 485 22474 157864 90447624
Nausea 269.70 18.65 748 22211 1109568 89495920
Neutropenia 249.96 18.65 296 22663 224608 90380880
Drug ineffective 219.53 18.65 43 22916 1384255 89221233
Neutrophil count decreased 204.87 18.65 159 22800 71373 90534115
Anaemia 159.77 18.65 305 22654 352497 90252991
Vomiting 148.66 18.65 487 22472 787806 89817682
Pyrexia 144.71 18.65 430 22529 660055 89945433
Leukopenia 134.52 18.65 146 22813 100564 90504924
Death 130.55 18.65 328 22631 456223 90149265
Platelet count decreased 124.23 18.65 163 22796 136806 90468682
Polyneuropathy 110.61 18.65 66 22893 19275 90586213
Joint swelling 109.99 18.65 4 22955 503296 90102192
Diarrhoea 106.28 18.65 494 22465 938696 89666792
Constipation 95.71 18.65 216 22743 280179 90325309
Mucosal inflammation 90.25 18.65 91 22868 57534 90547954
Dyspnoea 84.28 18.65 442 22517 880513 89724975
White blood cell count decreased 79.82 18.65 148 22811 166961 90438527
Rheumatoid arthritis 78.77 18.65 3 22956 362611 90242877
Disease progression 76.42 18.65 140 22819 156475 90449013
Thrombocytopenia 74.78 18.65 164 22795 208561 90396927
Decreased appetite 74.52 18.65 237 22722 376303 90229185
Flushing 73.59 18.65 101 22858 88390 90517098
Drug intolerance 72.45 18.65 13 22946 447578 90157910
Abdominal pain 71.96 18.65 242 22717 395479 90210009
Malignant neoplasm progression 70.03 18.65 109 22850 106761 90498727
General physical health deterioration 68.88 18.65 222 22737 354893 90250595
Hypokalaemia 66.23 18.65 119 22840 130997 90474491
Swelling 61.99 18.65 15 22944 419043 90186445
Bone pain 56.50 18.65 74 22885 61909 90543579
Chest discomfort 54.46 18.65 113 22846 138252 90467236
Weight increased 54.40 18.65 19 22940 417908 90187580
Pancytopenia 54.27 18.65 104 22855 120159 90485329
Neuropathy peripheral 54.07 18.65 112 22847 136858 90468630
Tooth erosion 51.81 18.65 14 22945 493 90604995
Musculoskeletal stiffness 51.61 18.65 7 22952 296525 90308963
Pharyngeal inflammation 49.67 18.65 16 22943 1044 90604444
Condition aggravated 49.29 18.65 47 22912 595498 90009990
Maternal exposure during pregnancy 49.26 18.65 15 22944 360048 90245440
Lymphoedema 49.26 18.65 35 22924 13718 90591770
Pericarditis 47.92 18.65 6 22953 270145 90335343
Erythema 46.84 18.65 146 22813 229100 90376388
Drug hypersensitivity 46.67 18.65 30 22929 463579 90141909
Product use issue 46.50 18.65 13 22946 329906 90275582
Peripheral swelling 45.45 18.65 24 22935 413082 90192406
Palmar-plantar erythrodysaesthesia syndrome 45.23 18.65 45 22914 27978 90577510
Duodenal ulcer perforation 44.34 18.65 3 22956 221285 90384203
Hepatic enzyme increased 44.26 18.65 18 22941 360718 90244770
Tumour pain 44.20 18.65 17 22942 1870 90603618
Breast cancer metastatic 44.06 18.65 34 22925 15098 90590390
Dysgeusia 43.69 18.65 60 22899 52500 90552988
Sepsis 42.89 18.65 121 22838 179693 90425795
Bone marrow failure 41.73 18.65 46 22913 32175 90573313
Ejection fraction decreased 40.25 18.65 41 22918 26212 90579276
Ileus 39.30 18.65 33 22926 16513 90588975
Abdominal discomfort 39.09 18.65 38 22921 477290 90128198
Wound 39.02 18.65 14 22945 302966 90302522
Nasopharyngitis 38.75 18.65 28 22931 407076 90198412
Discomfort 38.30 18.65 11 22948 274324 90331164
Pulpitis dental 38 18.65 13 22946 1023 90604465
Asthma 37.11 18.65 8 22951 242152 90363336
Epistaxis 36.42 18.65 72 22887 85053 90520435
Serotonin syndrome 35.71 18.65 46 22913 37841 90567647
Cough 35.65 18.65 186 22773 368776 90236712
Interstitial lung disease 35.60 18.65 67 22892 76338 90529150
Tachycardia 35.55 18.65 104 22855 157569 90447919
Disseminated intravascular coagulation 35.53 18.65 35 22924 21503 90583985
Impaired healing 35.36 18.65 8 22951 234191 90371297
Therapeutic product effect incomplete 35.13 18.65 4 22955 193892 90411596
Product dose omission issue 35.05 18.65 15 22944 291672 90313816
Sinusitis 33.43 18.65 23 22936 343065 90262423
Respiratory depth decreased 33.11 18.65 6 22953 29 90605459
Mucosal dryness 32.69 18.65 16 22943 3151 90602337
Periodontitis 32.56 18.65 17 22942 3836 90601652
Exposure during pregnancy 32.47 18.65 10 22949 238400 90367088
Asthenia 32.01 18.65 238 22721 533513 90071975
Systemic infection 31.82 18.65 18 22941 4757 90600731
Hepatic function abnormal 31.41 18.65 48 22911 46240 90559248
Venous thrombosis limb 31.34 18.65 16 22943 3446 90602042
Toxicity to various agents 31.23 18.65 17 22942 287829 90317659
Cachexia 30.56 18.65 20 22939 6858 90598630
Oesophagitis 30.27 18.65 29 22930 17220 90588268
Chills 29.70 18.65 87 22872 131894 90473594
Gastrointestinal disorder 29.58 18.65 14 22945 256673 90348815
Ultrasound foetal abnormal 29.41 18.65 7 22952 146 90605342
Dysphagia 29.18 18.65 78 22881 112200 90493288
Pneumonitis 28.84 18.65 45 22914 44125 90561363
Dehydration 28.52 18.65 111 22848 194336 90411152
Pleural effusion 28.30 18.65 77 22882 111914 90493574
Gastroenteritis radiation 28.23 18.65 9 22950 568 90604920
Cytomegalovirus test positive 27.95 18.65 15 22944 3576 90601912
Blister 27.75 18.65 15 22944 254983 90350505
Ascites 27.57 18.65 46 22913 47694 90557794
Liver injury 27.46 18.65 5 22954 170562 90434926
Neutropenic sepsis 27.22 18.65 28 22931 18102 90587386
Metastases to liver 27.19 18.65 35 22924 28772 90576716
Chronic hepatitis B 27.09 18.65 8 22951 390 90605098
Folliculitis 27.06 18.65 9 22950 204344 90401144
Psoriasis 26.89 18.65 3 22956 147751 90457737
Tumour lysis syndrome 25.99 18.65 22 22937 11130 90594358
Migraine 25.90 18.65 8 22951 190384 90415104
Mobility decreased 25.51 18.65 16 22943 250718 90354770
Arthralgia 24.97 18.65 107 22852 778415 89827073
Sensation of foreign body 24.66 18.65 17 22942 6349 90599139
Fatigue 24.51 18.65 419 22540 1153604 89451884
Septic shock 24.48 18.65 61 22898 84099 90521389
Lower respiratory tract infection 24.14 18.65 17 22942 250642 90354846
Hepatic failure 23.91 18.65 39 22920 39689 90565799
Renal pain 23.83 18.65 18 22941 7741 90597747
Intestinal perforation 23.72 18.65 23 22936 13858 90591630
Mitral valve disease 23.57 18.65 12 22947 2570 90602918
Anaphylactic shock 23.18 18.65 34 22925 31583 90573905
Sleep disorder 22.51 18.65 11 22948 198019 90407469
Dysaesthesia pharynx 22.46 18.65 6 22953 202 90605286
Subileus 22.31 18.65 13 22946 3631 90601857
Onychalgia 22.14 18.65 9 22950 1145 90604343
Fall 21.75 18.65 57 22902 481753 90123735
Inflammation 21.74 18.65 9 22950 178583 90426905
Contusion 21.72 18.65 19 22940 251197 90354291
Acute interstitial pneumonitis 21.43 18.65 8 22951 811 90604677
Osteochondrosis 21.11 18.65 10 22949 1833 90603655
Enterocolitis 21.04 18.65 19 22940 10471 90595017
Memory impairment 20.88 18.65 12 22947 197232 90408256
Aortitis 20.78 18.65 9 22950 1341 90604147
Flank pain 20.78 18.65 25 22934 19197 90586291
Vertigo 20.72 18.65 51 22908 69760 90535728
Laryngospasm 20.70 18.65 12 22947 3321 90602167
Tachypnoea 20.28 18.65 26 22933 21283 90584205
Gastrointestinal perforation 20.24 18.65 13 22946 4319 90601169
Acute myeloid leukaemia recurrent 20.07 18.65 10 22949 2047 90603441
Mucosal disorder 19.97 18.65 11 22948 2760 90602728
Ill-defined disorder 19.93 18.65 11 22948 184880 90420608
Back pain 19.87 18.65 143 22816 317032 90288456
Gastroenteropancreatic neuroendocrine tumour disease 19.73 18.65 4 22955 38 90605450
Cystitis haemorrhagic 19.67 18.65 14 22945 5499 90599989
Confusional state 19.55 18.65 43 22916 386162 90219326
Cytopenia 19.36 18.65 23 22936 17426 90588062
Bacteraemia 19.35 18.65 26 22933 22274 90583214
Metastases to central nervous system 19.26 18.65 23 22936 17519 90587969
Lymphocyte count decreased 19.21 18.65 33 22926 35017 90570471
Oral candidiasis 18.94 18.65 33 22926 35422 90570066

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Febrile neutropenia 382.82 17.19 427 17352 185276 42418280
Drug ineffective 156.77 17.19 36 17743 630161 41973395
Neutrophil count decreased 105.34 17.19 131 17648 63284 42540272
Pyrexia 99.10 17.19 374 17405 393668 42209888
White blood cell count decreased 84.44 17.19 159 17620 110237 42493319
Platelet count decreased 81.54 17.19 179 17600 138402 42465154
Neutropenia 75.72 17.19 218 17561 199213 42404343
Leukopenia 69.11 17.19 117 17662 74629 42528927
Anaemia 67.74 17.19 263 17516 280015 42323541
Nausea 66.10 17.19 333 17446 396466 42207090
Vomiting 59.05 17.19 258 17521 289465 42314091
Thrombocytopenia 58.23 17.19 193 17586 190086 42413470
General physical health deterioration 55.09 17.19 163 17616 151083 42452473
Stomatitis 54.97 17.19 85 17694 50244 42553312
Mucosal inflammation 50.62 17.19 81 17698 49293 42554263
Decreased appetite 50.50 17.19 186 17593 192951 42410605
Mucosal disorder 49.07 17.19 22 17757 2152 42601404
Constipation 49.07 17.19 164 17615 162127 42441429
Diarrhoea 47.31 17.19 341 17438 460508 42143048
Disseminated intravascular coagulation 45.64 17.19 54 17725 24740 42578816
Polyneuropathy 43.55 17.19 46 17733 18615 42584941
Interstitial lung disease 40.15 17.19 96 17683 78366 42525190
Product dose omission issue 39.80 17.19 8 17771 154357 42449199
Sepsis 39.37 17.19 176 17603 199158 42404398
Fall 38.87 17.19 25 17754 234495 42369061
Oesophagitis 38.12 17.19 39 17740 15208 42588348
Toxicity to various agents 33.33 17.19 28 17751 229108 42374448
Pneumonitis 30.49 17.19 59 17720 41659 42561897
Arthralgia 29.94 17.19 25 17754 205213 42398343
Systemic infection 28.84 17.19 21 17758 5184 42598372
Anaphylactic reaction 28.29 17.19 58 17721 42685 42560871
Pneumonia 28.17 17.19 284 17495 421865 42181691
Drug therapeutic incompatibility 27.58 17.19 7 17772 114 42603442
Blast cell count increased 26.77 17.19 12 17767 1173 42602383
Hypokalaemia 26.73 17.19 78 17701 71643 42531913
Aortitis 26.26 17.19 10 17769 646 42602910
Hypoalbuminaemia 25.48 17.19 32 17747 15578 42587978
Radiation oesophagitis 25.31 17.19 9 17770 479 42603077
Nail bed inflammation 24.75 17.19 7 17772 175 42603381
Insulin autoimmune syndrome 24.53 17.19 9 17770 524 42603032
Palmar-plantar erythrodysaesthesia syndrome 24.21 17.19 36 17743 20546 42583010
Antithrombin III decreased 23.88 17.19 9 17770 565 42602991
Fluid imbalance 23.80 17.19 8 17771 359 42603197
Non-small cell lung cancer 22.97 17.19 18 17761 4956 42598600
Subclavian artery occlusion 22.48 17.19 6 17773 120 42603436
Pancytopenia 22.48 17.19 103 17676 117640 42485916
Myocardial infarction 22.24 17.19 12 17767 123997 42479559
Dehydration 22.06 17.19 117 17662 141650 42461906
Laryngeal leukoplakia 21.51 17.19 5 17774 55 42603501
Hepatic infection 21.32 17.19 9 17770 761 42602795
Tumour perforation 21.10 17.19 8 17771 511 42603045
Paronychia 20.96 17.19 16 17763 4239 42599317
Autoimmune colitis 20.93 17.19 10 17769 1131 42602425
Blood lactate dehydrogenase increased 20.43 17.19 38 17741 26043 42577513
Ileus 20.43 17.19 32 17747 19107 42584449
Dermatitis acneiform 19.71 17.19 20 17759 7719 42595837
Staphylococcal sepsis 19.59 17.19 24 17755 11390 42592166
Cytokine release syndrome 19.12 17.19 51 17728 44476 42559080
Drug intolerance 19.05 17.19 5 17774 80419 42523137
Hospitalisation 18.84 17.19 4 17775 74326 42529230
Joint swelling 18.65 17.19 3 17776 68019 42535537
Alopecia 18.52 17.19 39 17740 29237 42574319
Taste disorder 18.40 17.19 22 17757 10185 42593371
Hepatic function abnormal 18.18 17.19 55 17724 51512 42552044
Peripheral sensory neuropathy 17.66 17.19 20 17759 8742 42594814
Flushing 17.53 17.19 44 17735 36984 42566572

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Febrile neutropenia 1082.16 17.23 854 34227 315913 110238305
Neutrophil count decreased 295.98 17.23 270 34811 120671 110433547
Drug ineffective 279.68 17.23 70 35011 1520470 109033748
Nausea 258.32 17.23 917 34164 1234773 109319445
Neutropenia 251.03 17.23 436 34645 374184 110180034
Platelet count decreased 224.97 17.23 319 34762 230124 110324094
Pyrexia 212.04 17.23 695 34386 897570 109656648
Anaemia 198.85 17.23 495 34586 546591 110007627
Leukopenia 174.04 17.23 225 34856 148566 110405652
White blood cell count decreased 170.69 17.23 280 34801 229110 110325108
Vomiting 152.56 17.23 631 34450 910044 109644174
Polyneuropathy 148.23 17.23 104 34977 31908 110522310
Mucosal inflammation 134.28 17.23 159 34922 95982 110458236
Thrombocytopenia 131.06 17.23 320 34761 348565 110205653
Diarrhoea 127.77 17.23 703 34378 1138802 109415416
Joint swelling 115.82 17.23 6 35075 442839 110111379
Constipation 105.60 17.23 300 34781 357486 110196732
Drug intolerance 96.20 17.23 9 35072 406503 110147715
Sepsis 96.11 17.23 274 34807 327072 110227146
Flushing 89.05 17.23 136 34945 104600 110449618
Hypokalaemia 88.09 17.23 185 34896 182263 110371955
Decreased appetite 86.73 17.23 339 34742 475507 110078711
General physical health deterioration 85.78 17.23 313 34768 424982 110129236
Oesophagitis 77.86 17.23 68 35013 28647 110525571
Malignant neoplasm progression 75.12 17.23 169 34912 174398 110379820
Treatment failure 74.91 17.23 3 35078 277231 110276987
Interstitial lung disease 74.00 17.23 147 34934 139187 110415031
Disseminated intravascular coagulation 72.56 17.23 77 35004 41209 110513009
Dyspnoea 70.27 17.23 594 34487 1106278 109447940
Pancytopenia 68.95 17.23 183 34898 209430 110344788
Arthralgia 67.71 17.23 89 34992 779543 109774675
Peripheral swelling 65.82 17.23 23 35058 404011 110150207
Completed suicide 64.24 17.23 3 35078 242378 110311840
Systemic infection 62.70 17.23 39 35042 9780 110544438
Product dose omission issue 62.40 17.23 13 35068 321769 110232449
Palmar-plantar erythrodysaesthesia syndrome 60.83 17.23 70 35011 40955 110513263
Drug hypersensitivity 59.70 17.23 35 35046 454055 110100163
Musculoskeletal stiffness 57.02 17.23 10 35071 279812 110274406
Fall 56.45 17.23 65 35016 603417 109950801
Therapeutic product effect incomplete 55.55 17.23 4 35077 223801 110330417
Ileus 55.22 17.23 58 35023 30671 110523547
Pneumonitis 54.91 17.23 92 34989 76439 110477779
Pulpitis dental 54.62 17.23 20 35061 1529 110552689
Weight increased 54.24 17.23 33 35048 419611 110134607
Toxicity to various agents 53.94 17.23 44 35037 480511 110073707
Bone marrow failure 51.83 17.23 77 35004 57771 110496447
Mucosal disorder 51.35 17.23 26 35055 4391 110549827
Condition aggravated 50.45 17.23 98 34983 734738 109819480
Abdominal pain 49.63 17.23 305 34776 512684 110041534
Hepatic function abnormal 49.57 17.23 96 34985 89199 110465019
Pericarditis 48.87 17.23 6 35075 219108 110335110
Nasopharyngitis 48.24 17.23 33 35048 394328 110159890
Blister 46.60 17.23 8 35073 227368 110326850
Tooth erosion 46.20 17.23 13 35068 423 110553795
Aortitis 46.09 17.23 19 35062 1996 110552222
Mobility decreased 45.19 17.23 10 35071 237412 110316806
Swelling 44.80 17.23 28 35053 351013 110203205
Dehydration 44.39 17.23 191 34890 279320 110274898
Pharyngeal inflammation 42.07 17.23 17 35064 1697 110552521
Cytokine release syndrome 42.00 17.23 78 35003 70228 110483990
Injury 41.70 17.23 4 35077 177261 110376957
Type 2 diabetes mellitus 41.69 17.23 4 35077 177228 110376990
Maternal exposure during pregnancy 40.65 17.23 15 35066 254868 110299350
Wound 40.53 17.23 12 35069 234425 110319793
Sinusitis 40.21 17.23 22 35059 296666 110257552
Enterocolitis 39.96 17.23 39 35042 18910 110535308
Duodenal ulcer perforation 39.30 17.23 5 35076 177695 110376523
Tachycardia 39.20 17.23 159 34922 226486 110327732
Tumour pain 39.04 17.23 19 35062 2948 110551270
Product use issue 38.22 17.23 26 35055 311669 110242549
Chills 37.27 17.23 139 34942 190441 110363777
Discomfort 37.10 17.23 11 35070 214696 110339522
Radiation oesophagitis 37.01 17.23 13 35068 881 110553337
Blood cholesterol increased 36.78 17.23 7 35074 184778 110369440
Hypoalbuminaemia 35.69 17.23 45 35036 28929 110525289
Neutropenic sepsis 35.12 17.23 46 35035 30700 110523518
Tumour lysis syndrome 35.06 17.23 46 35035 30755 110523463
Large intestine perforation 34.64 17.23 34 35047 16595 110537623
Neuropathy peripheral 34.43 17.23 130 34951 179147 110375071
Disease progression 33.67 17.23 160 34921 243874 110310344
Stomatitis 33.60 17.23 172 34909 270070 110284148
Pneumonia 32.80 17.23 423 34658 876291 109677927
Epistaxis 32.40 17.23 103 34978 130269 110423949
Bacteraemia 31.80 17.23 52 35029 42338 110511880
Respiratory depth decreased 31.77 17.23 6 35075 29 110554189
Breast cancer metastatic 31.36 17.23 27 35054 11154 110543064
Gastrointestinal disorder 31.27 17.23 19 35062 241933 110312285
Myocardial infarction 31.14 17.23 11 35070 192072 110362146
Abdominal discomfort 31.11 17.23 48 35033 393810 110160408
Ultrasound foetal abnormal 31.02 17.23 7 35074 90 110554128
Hepatic enzyme increased 30.58 17.23 34 35047 320858 110233360
Asthma 30.52 17.23 21 35060 250270 110303948
Tachypnoea 30.47 17.23 49 35032 39346 110514872
Dysgeusia 30.35 17.23 68 35013 69917 110484301
Dermatitis acneiform 30.33 17.23 28 35053 12667 110541551
C-reactive protein abnormal 30.31 17.23 3 35078 129692 110424526
Lymphoedema 30.13 17.23 30 35051 14899 110539319
Neutropenic colitis 30.08 17.23 23 35058 8042 110546176
Liver injury 29.30 17.23 6 35075 150407 110403811
Migraine 29.28 17.23 9 35072 171643 110382575
Memory impairment 29.10 17.23 13 35068 196931 110357287
Venous thrombosis limb 28.87 17.23 19 35062 5246 110548972
Chest discomfort 28.51 17.23 120 34961 173728 110380490
Inflammation 28.17 17.23 13 35068 193225 110360993
Exposure during pregnancy 28.16 17.23 9 35072 167415 110386803
Bursitis 27.90 17.23 4 35077 129914 110424304
Confusional state 27.57 17.23 68 35013 468612 110085606
Impaired healing 27.51 17.23 14 35067 196703 110357515
Blood lactate dehydrogenase increased 27.50 17.23 50 35031 44284 110509934
Drug therapeutic incompatibility 27.37 17.23 7 35074 157 110554061
Peripheral sensory neuropathy 27.35 17.23 30 35051 16650 110537568
Engraftment syndrome 27.32 17.23 13 35068 1919 110552299
Antithrombin III decreased 27.16 17.23 9 35072 511 110553707
Pain 26.90 17.23 185 34896 954770 109599448
Periodontitis 26.65 17.23 18 35063 5190 110549028
Psoriasis 26.42 17.23 6 35075 139987 110414231
Staphylococcal sepsis 26.24 17.23 30 35051 17424 110536794
Non-small cell lung cancer 26.07 17.23 21 35060 7914 110546304
Venoocclusive disease 25.66 17.23 19 35062 6331 110547887
Colitis 25.57 17.23 81 35000 102242 110451976
Hepatic infection 25.54 17.23 11 35070 1288 110552930
Therapy non-responder 25.51 17.23 9 35072 157298 110396920
Cystitis haemorrhagic 25.50 17.23 25 35056 12184 110542034
Erythema 25.48 17.23 169 34912 291278 110262940
Colony stimulating factor therapy 25.30 17.23 9 35072 633 110553585
Sleep disorder 25.11 17.23 16 35065 198628 110355590
Septic shock 24.49 17.23 107 34974 157421 110396797
Osteoarthritis 24.08 17.23 14 35067 182609 110371609
Insulin autoimmune syndrome 24.03 17.23 9 35072 733 110553485
Dysaesthesia pharynx 23.86 17.23 7 35074 265 110553953
Immune-mediated enterocolitis 23.44 17.23 22 35059 10163 110544055
Intestinal perforation 23.40 17.23 31 35050 20913 110533305
Gastroenteritis radiation 23.29 17.23 9 35072 799 110553419
Blast cell count increased 23.11 17.23 11 35070 1626 110552592
Lower respiratory tract infection 22.89 17.23 26 35055 243080 110311138
Enterocolitis infectious 22.80 17.23 14 35067 3430 110550788
Laryngeal leukoplakia 22.79 17.23 5 35076 56 110554162
Pleural effusion 22.70 17.23 114 34967 177595 110376623
Chronic hepatitis B 22.54 17.23 8 35073 559 110553659
Subclavian artery occlusion 22.22 17.23 6 35075 167 110554051
Ill-defined disorder 22.18 17.23 11 35070 156842 110397376
Proteinuria 22.17 17.23 43 35038 39975 110514243
Arthritis 21.88 17.23 13 35068 167573 110386645
Tumour perforation 21.53 17.23 8 35073 637 110553581
Gastroenteropancreatic neuroendocrine tumour disease 21.44 17.23 5 35076 75 110554143
Wheezing 21.22 17.23 30 35051 255200 110299018
Subileus 21.07 17.23 17 35064 6420 110547798
Stress 20.94 17.23 4 35077 105344 110448874
Gastrointestinal perforation 20.90 17.23 18 35063 7438 110546780
Fluid imbalance 20.88 17.23 8 35073 694 110553524
Serotonin syndrome 20.81 17.23 53 35028 59100 110495118
Intentional product use issue 20.75 17.23 29 35052 247877 110306341
Hepatic failure 20.57 17.23 58 35023 68681 110485537
Onychalgia 20.32 17.23 9 35072 1128 110553090
Drug ineffective for unapproved indication 20.24 17.23 4 35077 102834 110451384
Dysaesthesia 20.15 17.23 17 35064 6830 110547388
Febrile infection 19.54 17.23 14 35067 4434 110549784
Gastrooesophageal reflux disease 19.52 17.23 17 35064 179959 110374259
Hyperglycaemia 19.14 17.23 65 35016 85025 110469193
Anaphylactic shock 18.99 17.23 47 35034 51499 110502719
Cachexia 18.96 17.23 22 35059 12983 110541235
Oral candidiasis 18.86 17.23 43 35038 44717 110509501
Lymphocyte count decreased 18.82 17.23 50 35031 57193 110497025
Acute graft versus host disease in skin 18.81 17.23 20 35061 10720 110543498
Bone pain 18.56 17.23 54 35027 65079 110489139
Aplastic anaemia 18.48 17.23 30 35051 24278 110529940
Incorrect dose administered 18.47 17.23 5 35076 103636 110450582
Vertigo 18.36 17.23 65 35016 86805 110467413
Paronychia 18.29 17.23 20 35061 11061 110543157
Autoimmune colitis 18.28 17.23 10 35071 1975 110552243
Death 18.19 17.23 317 34764 698552 109855666
Night sweats 18.05 17.23 10 35071 133973 110420245
Anaphylactic reaction 18.04 17.23 78 35003 114222 110439996
Intracranial tumour haemorrhage 17.94 17.23 7 35074 637 110553581
Sensation of foreign body 17.92 17.23 17 35064 7958 110546260
Injection site pain 17.89 17.23 18 35063 177904 110376314
Circulatory collapse 17.78 17.23 41 35040 42952 110511266
Mucosal dryness 17.78 17.23 13 35068 4250 110549968
Vulvovaginal dryness 17.76 17.23 11 35070 2736 110551482
Cytomegalovirus test positive 17.75 17.23 16 35065 7020 110547198
Electrocardiogram ST segment elevation 17.74 17.23 18 35063 9142 110545076
Restrictive cardiomyopathy 17.69 17.23 8 35073 1053 110553165
Road traffic accident 17.66 17.23 6 35075 107392 110446826
Hypotension 17.57 17.23 248 34833 523601 110030617
COVID-19 17.36 17.23 32 35049 245028 110309190
Throat tightness 17.36 17.23 35 35046 33454 110520764

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A04AA02 ALIMENTARY TRACT AND METABOLISM
ANTIEMETICS AND ANTINAUSEANTS
ANTIEMETICS AND ANTINAUSEANTS
Serotonin (5HT3) antagonists
CHEBI has role CHEBI:48279 serotonergic antagonist
CHEBI has role CHEBI:50919 antiemetic
FDA MoA N0000175817 Serotonin 3 Receptor Antagonists
FDA EPC N0000175818 Serotonin-3 Receptor Antagonist
MeSH PA D000932 Antiemetics
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D012702 Serotonin Antagonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018490 Serotonin Agents
MeSH PA D058831 Serotonin 5-HT3 Receptor Antagonists

Related Drugs by ATC class:

A04AA Serotonin (5HT3) antagonists 4 drugs
dolasetronondansetronpalonosetrontropisetron

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

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (acidic/basic)
pKa1 13.79 acidic
pKa2 9.5 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
5-hydroxytryptamine receptor 3A Ion channel ANTAGONIST Ki 8.70 WOMBAT-PK CHEMBL
Solute carrier family 22 member 2 Transporter IC50 5.37 CHEMBL
Multidrug and toxin extrusion protein 1 Transporter IC50 5.30 CHEMBL
Neuronal acetylcholine receptor; alpha4/beta2 Ion channel Ki 4.42 CHEMBL
5-hydroxytryptamine receptor 3B Ion channel Ki 8.80 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.43 WOMBAT-PK
Neuronal acetylcholine receptor subunit alpha-3 Ion channel Ki 4.17 CHEMBL
5-hydroxytryptamine receptor 3A Ion channel Ki 8.40 CHEMBL
Serotonin 3 (5-HT3) receptor Ion channel Ki 9.46 CHEMBL

External reference:

IDSource
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
WZG3J2MCOL INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Granisetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0143-9744 INJECTION 1 mg INTRAVENOUS ANDA 24 sections
Granisetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0143-9745 INJECTION 1 mg INTRAVENOUS ANDA 24 sections
Granisetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 17478-546 INJECTION 1 mg INTRAVENOUS ANDA 26 sections
SUSTOL HUMAN PRESCRIPTION DRUG LABEL 1 47426-101 INJECTION 10 mg SUBCUTANEOUS NDA 28 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 HUMAN PRESCRIPTION DRUG LABEL 1 63323-317 INJECTION, SOLUTION 0.10 mg INTRAVENOUS ANDA 24 sections
Granisetron HUMAN PRESCRIPTION DRUG LABEL 1 63323-318 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 24 sections
Granisetron HUMAN PRESCRIPTION DRUG LABEL 1 63323-319 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 24 sections
Granisetron hydrochloride Human Prescription Drug Label 1 63850-0005 TABLET, FILM COATED 1 mg ORAL ANDA 18 sections
SANCUSO HUMAN PRESCRIPTION DRUG LABEL 1 66220-637 PATCH 3.10 mg TRANSDERMAL NDA 29 sections
Granisetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 67457-861 INJECTION, SOLUTION 0.10 mg INTRAVENOUS ANDA 24 sections
Granisetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 67457-863 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 24 sections
Granisetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 67457-864 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 24 sections
Granisetron Hydrochloride Human Prescription Drug Label 1 67877-184 TABLET 1 mg ORAL ANDA 16 sections
Granisetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 69452-350 TABLET, FILM COATED 1 mg ORAL ANDA 20 sections
Granisol HUMAN PRESCRIPTION DRUG LABEL 1 80056-801 SOLUTION 2 mg ORAL ANDA 19 sections