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
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

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 450.96 17.58 326 17078 97341 50490379
Neutropenia 217.87 17.58 261 17143 147704 50440016
Drug ineffective 188.70 17.58 29 17375 819304 49768416
Nausea 168.81 17.58 577 16827 704821 49882899
Neutrophil count decreased 137.19 17.58 119 17285 45907 50541813
Death 119.94 17.58 311 17093 325068 50262652
Vomiting 111.37 17.58 379 17025 460379 50127341
Pyrexia 111.18 17.58 334 17070 379869 50207851
Leukopenia 102.22 17.58 121 17283 67407 50520313
General physical health deterioration 82.32 17.58 163 17241 142271 50445449
Decreased appetite 80.02 17.58 198 17206 200725 50386995
Platelet count decreased 79.50 17.58 132 17272 100594 50487126
Constipation 70.76 17.58 180 17224 185528 50402192
Joint swelling 68.35 17.58 4 17400 245282 50342438
Anaemia 66.34 17.58 214 17190 252242 50335478
Thrombocytopenia 63.05 17.58 137 17267 127536 50460184
Disease progression 59.35 17.58 113 17291 95753 50491967
Polyneuropathy 59.20 17.58 42 17362 12089 50575631
White blood cell count decreased 58.48 17.58 126 17278 116596 50471124
Diarrhoea 55.82 17.58 369 17035 588107 49999613
Dyspnoea 50.45 17.58 341 17063 547267 50040453
Tooth erosion 49.20 17.58 14 17390 437 50587283
Drug intolerance 47.36 17.58 9 17395 219095 50368625
Mucosal inflammation 45 17.58 62 17342 40080 50547640
Condition aggravated 43.58 17.58 24 17380 297034 50290686
Abdominal pain 42.34 17.58 177 17227 236051 50351669
Malignant neoplasm progression 41.77 17.58 80 17324 68044 50519676
Stomatitis 41.44 17.58 101 17303 101243 50486477
Pancytopenia 40.11 17.58 89 17315 83941 50503779
Erythema 37.36 17.58 123 17281 146291 50441429
Pulpitis dental 36.89 17.58 13 17391 820 50586900
Flushing 36.62 17.58 75 17329 66940 50520780
Weight increased 36.46 17.58 12 17392 201879 50385841
Treatment failure 36.12 17.58 3 17401 137634 50450086
Toxicity to various agents 36.05 17.58 14 17390 212485 50375235
Drug hypersensitivity 35.76 17.58 21 17383 250989 50336731
Breast cancer metastatic 35.38 17.58 29 17375 10335 50577385
Neuropathy peripheral 34.93 17.58 92 17312 96665 50491055
Bone marrow failure 34.53 17.58 45 17359 27579 50560141
Maternal exposure during pregnancy 33.59 17.58 7 17397 159771 50427949
Swelling 32.82 17.58 14 17390 200858 50386862
Product dose omission issue 31.36 17.58 12 17392 183826 50403894
Periodontitis 31.31 17.58 17 17387 3052 50584668
Respiratory depth decreased 31.28 17.58 6 17398 29 50587691
Palmar-plantar erythrodysaesthesia syndrome 30.35 17.58 36 17368 20062 50567658
Ileus 29.28 17.58 29 17375 13200 50574520
Cytomegalovirus test positive 28.24 17.58 15 17389 2577 50585143
Venous thrombosis limb 28.08 17.58 15 17389 2607 50585113
Sinusitis 27.68 17.58 12 17392 170546 50417174
Hypokalaemia 27.14 17.58 79 17325 87913 50499807
Fall 27.10 17.58 46 17358 334886 50252834
Peripheral swelling 26.90 17.58 19 17385 205917 50381803
Musculoskeletal stiffness 26.25 17.58 6 17398 128475 50459245
Lymphoedema 25.97 17.58 23 17381 9099 50578621
Chronic hepatitis B 25.82 17.58 7 17397 182 50587538
Chest discomfort 25.54 17.58 80 17324 92642 50495078
Product use issue 25.09 17.58 10 17394 149465 50438255
Sepsis 24.87 17.58 101 17303 132824 50454896
Bone pain 24.79 17.58 52 17352 47177 50540543
Hepatic function abnormal 24.63 17.58 42 17362 32639 50555081
Arthralgia 22.92 17.58 76 17328 438626 50149094
Ejection fraction decreased 22.88 17.58 30 17374 18490 50569230
Interstitial lung disease 22.79 17.58 54 17350 53122 50534598
Cytopenia 22.77 17.58 21 17383 8754 50578966
Onychalgia 22.72 17.58 9 17395 786 50586934
Mitral valve disease 22.63 17.58 12 17392 2054 50585666
Asthenia 22.59 17.58 187 17217 318855 50268865
Metastases to liver 22.44 17.58 31 17373 20073 50567647
Tumour pain 22.06 17.58 10 17394 1220 50586500
Subileus 21.98 17.58 13 17391 2746 50584974
Tumour lysis syndrome 21.70 17.58 19 17385 7402 50580318
Therapeutic product effect incomplete 21.45 17.58 3 17401 91512 50496208
Abdominal discomfort 21.43 17.58 29 17375 231612 50356108
Off label use 21.37 17.58 253 17151 474173 50113547
Nasopharyngitis 21.25 17.58 21 17383 192906 50394814
Acute interstitial pneumonitis 21.18 17.58 8 17396 615 50587105
Acute myeloid leukaemia recurrent 20.89 17.58 10 17394 1380 50586340
Mucosal dryness 20.87 17.58 12 17392 2405 50585315
Mucosal disorder 20.74 17.58 11 17393 1884 50585836
Gastrointestinal submucosal tumour 20.27 17.58 4 17400 23 50587697
Oesophagitis 20.25 17.58 24 17380 13359 50574361
Gastroenteropancreatic neuroendocrine tumour disease 19.72 17.58 4 17400 27 50587693
Epistaxis 19.31 17.58 57 17347 63897 50523823
Paraesthesia 19.12 17.58 87 17317 120156 50467564
Exposure during pregnancy 18.87 17.58 9 17395 121006 50466714
Metastases to bone marrow 18.81 17.58 6 17398 278 50587442
Fatigue 18.72 17.58 344 17060 707257 49880463
Pleural effusion 18.62 17.58 66 17338 81388 50506332
Aortitis 18.57 17.58 8 17396 864 50586856
Acute graft versus host disease in skin 18.41 17.58 12 17392 3006 50584714
Gastrointestinal perforation 18.26 17.58 12 17392 3049 50584671
Ascites 18.25 17.58 39 17365 35822 50551898

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 270.87 17.58 297 13620 111943 29448667
Neutrophil count decreased 104.13 17.58 115 13802 43452 29517158
Drug ineffective 102.56 17.58 23 13894 363147 29197463
Pyrexia 81.69 17.58 308 13609 287314 29273296
Neutropenia 73.32 17.58 179 13738 131532 29429078
White blood cell count decreased 72.65 17.58 136 13781 83226 29477384
Leukopenia 63.70 17.58 102 13815 55101 29505509
Platelet count decreased 62.23 17.58 146 13771 104526 29456084
Stomatitis 53.35 17.58 76 13841 37037 29523573
Vomiting 51.75 17.58 217 13700 212043 29348567
Nausea 48.27 17.58 265 13652 288990 29271620
Mucosal disorder 47.35 17.58 20 13897 1500 29559110
Decreased appetite 45.54 17.58 161 13756 145181 29415429
Polyneuropathy 41.63 17.58 39 13878 12113 29548497
Interstitial lung disease 41.57 17.58 87 13830 57631 29502979
Disseminated intravascular coagulation 41.35 17.58 49 13868 19931 29540679
Sepsis 41.26 17.58 154 13763 142528 29418082
Thrombocytopenia 41.07 17.58 148 13769 134675 29425935
Anaemia 39.61 17.58 193 13724 200758 29359852
Oesophagitis 38.44 17.58 37 13880 11886 29548724
Diarrhoea 36.42 17.58 274 13643 332424 29228186
Fall 33.56 17.58 21 13896 177157 29383453
Constipation 31.96 17.58 122 13795 114038 29446572
Product dose omission issue 31.70 17.58 4 13913 96379 29464231
General physical health deterioration 28.84 17.58 110 13807 102747 29457863
Antithrombin III decreased 28.25 17.58 9 13908 301 29560309
Blast cell count increased 27.38 17.58 12 13905 985 29559625
Toxicity to various agents 27.23 17.58 25 13892 173636 29386974
Drug therapeutic incompatibility 26.86 17.58 7 13910 112 29560498
Disease progression 26.68 17.58 92 13825 81824 29478786
Fluid imbalance 26.13 17.58 8 13909 234 29560376
Radiation oesophagitis 25.87 17.58 9 13908 397 29560213
Tumour perforation 25.54 17.58 8 13909 253 29560357
Nail bed inflammation 24.38 17.58 7 13910 163 29560447
Mucosal inflammation 24.35 17.58 49 13868 31546 29529064
Myocardial infarction 23.90 17.58 11 13906 110285 29450325
Autoimmune colitis 22.12 17.58 10 13907 883 29559727
Non-small cell lung cancer 21.95 17.58 15 13902 2966 29557644
Subclavian artery occlusion 21.62 17.58 6 13911 123 29560487
Systemic infection 21.49 17.58 13 13904 2088 29558522
Blood lactate dehydrogenase increased 21.45 17.58 35 13882 19174 29541436
Pneumonia 21.30 17.58 237 13680 319935 29240675
Laryngeal leukoplakia 20.91 17.58 5 13912 55 29560555
Arthralgia 20.82 17.58 21 13896 139596 29421014
Colorectal cancer 20.26 17.58 12 13905 1855 29558755
Engraftment syndrome 19.50 17.58 9 13908 834 29559776
Hepatic function abnormal 19.30 17.58 51 13866 39208 29521402
Proteinuria 19.30 17.58 30 13887 15774 29544836
Pulpitis dental 18.76 17.58 7 13910 378 29560232
Palmar-plantar erythrodysaesthesia syndrome 18.00 17.58 28 13889 14731 29545879
Acute graft versus host disease in skin 17.99 17.58 16 13901 4648 29555962
Flushing 17.78 17.58 41 13876 28951 29531659
Alopecia 17.66 17.58 32 13885 19052 29541558
Dermatitis acneiform 17.62 17.58 17 13900 5474 29555136

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 662.57 15.33 576 26008 187081 64285067
Neutrophil count decreased 226.32 15.33 214 26370 76982 64395166
Neutropenia 217.51 15.33 369 26215 239255 64232893
Drug ineffective 213.27 15.33 44 26540 840203 63631945
Nausea 159.08 15.33 691 25893 785109 63687039
Pyrexia 158.47 15.33 547 26037 558097 63914051
Platelet count decreased 151.60 15.33 258 26326 167453 64304695
Leukopenia 134.11 15.33 186 26398 101056 64371092
White blood cell count decreased 132.43 15.33 235 26349 157602 64314546
Vomiting 117.52 15.33 493 26091 550624 63921524
Polyneuropathy 101.51 15.33 76 26508 19818 64452330
Thrombocytopenia 88.98 15.33 247 26337 223554 64248594
Anaemia 84.61 15.33 344 26240 378336 64093812
Decreased appetite 80.69 15.33 277 26307 281012 64191136
Completed suicide 79.36 15.33 3 26581 224411 64247737
Diarrhoea 74.29 15.33 530 26054 722174 63749974
Sepsis 69.69 15.33 231 26353 230110 64242038
Joint swelling 69.52 15.33 5 26579 215377 64256771
Constipation 66.73 15.33 227 26357 229110 64243038
Oesophagitis 65.28 15.33 61 26523 21569 64450579
Stomatitis 62.57 15.33 139 26445 109466 64362682
General physical health deterioration 61.81 15.33 205 26379 204220 64267928
Mucosal inflammation 60.05 15.33 99 26485 62485 64409663
Toxicity to various agents 59.93 15.33 38 26546 363475 64108673
Drug intolerance 58.88 15.33 5 26579 187987 64284161
Pulpitis dental 57.69 15.33 20 26564 999 64471149
Interstitial lung disease 55.84 15.33 124 26460 97608 64374540
Arthralgia 54.79 15.33 61 26523 442199 64029949
Fall 54.41 15.33 55 26529 416771 64055377
Product dose omission issue 53.92 15.33 8 26576 194739 64277409
Flushing 53.30 15.33 107 26477 78541 64393607
Mucosal disorder 47.96 15.33 24 26560 3038 64469110
Disseminated intravascular coagulation 46.67 15.33 62 26522 32286 64439862
Tooth erosion 44.11 15.33 13 26571 382 64471766
Bone marrow failure 43.51 15.33 74 26510 47878 64424270
Hepatic function abnormal 41.79 15.33 86 26498 64227 64407921
Ileus 41.06 15.33 49 26535 22917 64449231
Drug hypersensitivity 40.35 15.33 24 26560 237791 64234357
Pancytopenia 39.14 15.33 139 26445 143170 64328978
Malignant neoplasm progression 38.45 15.33 118 26466 112753 64359395
Palmar-plantar erythrodysaesthesia syndrome 38.18 15.33 53 26531 28766 64443382
Dyspnoea 37.86 15.33 457 26127 718217 63753931
Myocardial infarction 37.31 15.33 11 26573 165810 64306338
Peripheral swelling 37.07 15.33 20 26564 209133 64263015
Hypokalaemia 36.57 15.33 122 26462 121781 64350367
Condition aggravated 34.55 15.33 63 26521 372363 64099785
Tumour lysis syndrome 32.35 15.33 40 26544 19400 64452748
Treatment failure 31.86 15.33 5 26579 116811 64355337
Therapeutic product effect incomplete 31.72 15.33 3 26581 103479 64368669
Weight increased 30.33 15.33 26 26558 213322 64258826
Respiratory depth decreased 30.20 15.33 6 26578 29 64472119
Disease progression 28.61 15.33 125 26459 141555 64330593
Musculoskeletal stiffness 28.03 15.33 8 26576 123198 64348950
Radiation oesophagitis 27.73 15.33 10 26574 561 64471587
Venous thrombosis limb 27.36 15.33 18 26566 3819 64468329
Enterocolitis 27.21 15.33 29 26555 11989 64460159
C-reactive protein increased 26.71 15.33 93 26491 94816 64377332
Antithrombin III decreased 26.30 15.33 9 26575 432 64471716
Large intestine perforation 26.07 15.33 29 26555 12575 64459573
Periodontitis 26.05 15.33 18 26566 4141 64468007
Dermatitis acneiform 25.83 15.33 24 26560 8419 64463729
Drug therapeutic incompatibility 25.81 15.33 7 26577 151 64471997
Sinusitis 25.78 15.33 14 26570 145914 64326234
Non-small cell lung cancer 25.65 15.33 19 26565 4871 64467277
Nasopharyngitis 25.39 15.33 26 26558 196047 64276101
Breast cancer metastatic 25.13 15.33 22 26562 7147 64465001
Colony stimulating factor therapy 24.94 15.33 9 26575 506 64471642
Aortitis 24.52 15.33 11 26573 1090 64471058
Tumour perforation 24.43 15.33 8 26576 335 64471813
Engraftment syndrome 24.41 15.33 11 26573 1102 64471046
Proteinuria 24.12 15.33 42 26542 27681 64444467
Pneumonia 24.01 15.33 343 26241 559233 63912915
Dehydration 23.85 15.33 162 26422 216601 64255547
Blood lactate dehydrogenase increased 23.59 15.33 46 26538 33032 64439116
Blast cell count increased 22.95 15.33 11 26573 1268 64470880
Fluid imbalance 22.58 15.33 8 26576 426 64471722
Chronic hepatitis B 22.31 15.33 7 26577 255 64471893
Product use issue 22.15 15.33 18 26566 151697 64320451
Neuropathy peripheral 21.71 15.33 101 26483 117424 64354724
Peripheral sensory neuropathy 21.54 15.33 25 26559 11353 64460795
Laryngeal leukoplakia 21.49 15.33 5 26579 56 64472092
Pneumonitis 21.36 15.33 57 26527 50308 64421840
Hypoalbuminaemia 21.19 15.33 31 26553 17643 64454505
Onychalgia 21.12 15.33 9 26575 788 64471360
Subileus 21.01 15.33 17 26567 4960 64467188
Subclavian artery occlusion 20.95 15.33 6 26578 159 64471989
Systemic infection 20.91 15.33 16 26568 4305 64467843
Abdominal pain 20.64 15.33 208 26376 312167 64159981
Hepatic infection 20.54 15.33 9 26575 844 64471304
Maternal exposure during pregnancy 20.42 15.33 7 26577 95877 64376271
Paraesthesia 20.18 15.33 109 26475 134413 64337735
Acute graft versus host disease in skin 20.04 15.33 19 26565 6836 64465312
Gastrointestinal perforation 19.73 15.33 17 26567 5407 64466741
Erythema 19.50 15.33 138 26446 186932 64285216
Febrile infection 19.22 15.33 13 26571 2888 64469260
Autoimmune colitis 19.16 15.33 10 26574 1381 64470767
Pain 18.95 15.33 142 26442 553369 63918779
Oral candidiasis 18.69 15.33 34 26550 23178 64448970
Gastroenteropancreatic neuroendocrine tumour disease 18.63 15.33 4 26580 30 64472118
Neutropenic sepsis 18.63 15.33 34 26550 23238 64448910
Cardiac failure congestive 18.44 15.33 16 26568 130564 64341584
Colorectal cancer 17.99 15.33 13 26571 3208 64468940
Neutropenic colitis 17.98 15.33 15 26569 4566 64467582
Psoriasis 17.57 15.33 4 26580 71699 64400449
Lymphoedema 17.48 15.33 21 26563 9884 64462264
Nail bed inflammation 17.35 15.33 7 26577 534 64471614
Acute myeloid leukaemia recurrent 17.32 15.33 12 26572 2772 64469376
COVID-19 17.28 15.33 3 26581 65137 64407011
Paronychia 17.11 15.33 17 26567 6475 64465673
Colitis ischaemic 16.77 15.33 24 26560 13390 64458758
Radiation skin injury 16.74 15.33 9 26575 1321 64470827
Cytomegalovirus test positive 16.47 15.33 15 26569 5129 64467019
Drug interaction 16.47 15.33 85 26499 361998 64110150
Enterocolitis infectious 16.22 15.33 11 26573 2453 64469695
Tumour pain 16.10 15.33 10 26574 1923 64470225
Colitis 16.08 15.33 57 26527 58617 64413531
Cystitis haemorrhagic 15.93 15.33 18 26566 7938 64464210
Metastases to bone marrow 15.93 15.33 7 26577 661 64471487
Cerebrovascular accident 15.89 15.33 20 26564 137563 64334585
Acute interstitial pneumonitis 15.79 15.33 8 26576 1039 64471109
Confusional state 15.76 15.33 55 26529 261089 64211059
Capillary leak syndrome 15.50 15.33 12 26572 3285 64468863
Tachycardia 15.38 15.33 110 26474 149469 64322679
Incisional hernia 15.38 15.33 10 26574 2080 64470068
Intracranial tumour haemorrhage 15.34 15.33 6 26578 422 64471726

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 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 D018490 Serotonin Agents
MeSH PA D012702 Serotonin Antagonists

Drug Use (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
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
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
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 17478-547 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
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 63323-318 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 25 sections
Granisetron HUMAN PRESCRIPTION DRUG LABEL 1 63323-319 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 25 sections
Granisetron hydrochloride Human Prescription Drug Label 1 63850-0005 TABLET, FILM COATED 1 mg ORAL ANDA 18 sections
GRANISETRON HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 64679-661 INJECTION 1 mg INTRAVENOUS ANDA 23 sections
GRANISETRON HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 64679-662 INJECTION 0.10 mg INTRAVENOUS ANDA 23 sections
GRANISETRON HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 64679-841 INJECTION 1 mg INTRAVENOUS ANDA 23 sections
Granisetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 67457-861 INJECTION, SOLUTION 0.10 mg INTRAVENOUS ANDA 24 sections