granisetron ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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 ยตM/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:

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 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 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 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 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 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 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
Small for dates baby 12.13 12.06 5 3 2804 86980

Pharmacologic Action:

SourceCodeDescription
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|

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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ 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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent 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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
5-hydroxytryptamine receptor 3A Ion channel ANTAGONIST Ki 8.70 WOMBAT-PK CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.43 WOMBAT-PK
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
Neuronal acetylcholine receptor subunit alpha-3 Ion channel Ki 4.17 CHEMBL
Serotonin 3 (5-HT3) receptor Ion channel Ki 9.46 CHEMBL
5-hydroxytryptamine receptor 3A Ion channel Ki 8.40 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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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