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

Stem definitionDrug idCAS RN
serotonin receptor antagonists (5-HT3) 2046 135729-61-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • palonosetron
  • (-)-Palonosetron
  • palonosetron hydrochloride
  • aloxi
  • RS 25259-197
  • palonosetron HCl
an antiemetic and antinauseant agent, it is a serotonin subtype 3 (5-HT3) receptor antagonist with a strong binding affinity for this receptor and little or no affinity for other receptors
  • Molecular weight: 296.41
  • Formula: C19H24N2O
  • CLOGP: 2.18
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 0
  • TPSA: 23.55
  • ALOGS: -2.81
  • ROTB: 1
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.50 mg O
0.25 mg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 40 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.01 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 97 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 6.30 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 2.60 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.38 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 39 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 0.852 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 4.169 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 7.396 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 3.639 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 57.430 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 62.830 % High 1
herg hERG pIC50 4.795 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 1 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 4.178 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 58.940 % High 1
kinase-safety-class ACVR2B,AXL,BRAF,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAPKAPK2,MET,NTRK2,PDK2,PDK4,PRKDC,TEK,TGFBR1 21
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 1.995 High 1
mh-clint Mouse hepatocyte intrinsic clearance 22.336 High 1
mppb Mouse plasma protein binding (% unbound) 48.160 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 10.209 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 High 1
pppb Pig plasma protein binding (% unbound) 66.200 % High 1
rh-clint Rat hepatocyte intrinsic clearance 30.339 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 82.180 % High 1
rppb Rat plasma protein binding (% unbound) 54.310 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 941.890 uM High 1

Approvals:

DateAgencyCompanyOrphan
May 27, 2021 PMDA TAIHO PHARMACEUTICAL Co., Ltd.
March 22, 2005 EMA
July 25, 2003 FDA HELSINN HLTHCARE

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
Death 440.50 21.18 501 17949 456050 90153947
Febrile neutropenia 403.40 21.18 300 18150 158049 90451948
Neutropenia 332.53 21.18 311 18139 224593 90385404
Neutrophil count decreased 290.45 21.18 181 18269 71351 90538646
Nausea 233.86 21.18 618 17832 1109698 89500299
Constipation 193.94 21.18 261 18189 280134 90329863
Decreased appetite 172.42 21.18 289 18161 376251 90233746
Neuropathy peripheral 151.42 21.18 162 18288 136808 90473189
Flushing 141.33 21.18 128 18322 88363 90521634
Drug ineffective 136.72 21.18 56 18394 1384242 89225755
Anaemia 129.51 21.18 246 18204 352556 90257441
Disease progression 128.81 21.18 159 18291 156456 90453541
Platelet count decreased 110.90 21.18 138 18312 136831 90473166
Vomiting 107.62 21.18 378 18072 787915 89822082
Myelosuppression 106.79 21.18 88 18362 53503 90556494
Off label use 95.39 21.18 459 17991 1101793 89508204
Palmar-plantar erythrodysaesthesia syndrome 84.62 21.18 59 18391 27964 90582033
Colony stimulating factor therapy 83.59 21.18 19 18431 405 90609592
Mucosal inflammation 79.73 21.18 77 18373 57548 90552449
Hypokalaemia 76.96 21.18 113 18337 131003 90478994
Thrombocytopenia 73.30 21.18 143 18307 208582 90401415
Pyrexia 68.80 21.18 291 18159 660194 89949803
Interstitial lung disease 66.68 21.18 80 18370 76325 90533672
Condition aggravated 60.27 21.18 23 18427 595522 90014475
White blood cell count decreased 59.27 21.18 115 18335 166994 90443003
Cystitis haemorrhagic 56.85 21.18 26 18424 5487 90604510
Dyspnoea 55.60 21.18 337 18113 880618 89729379
Rheumatoid arthritis 55.49 21.18 5 18445 362609 90247388
Joint swelling 55.12 21.18 17 18433 503283 90106714
Diarrhoea 54.74 21.18 352 18098 938838 89671159
Back pain 53.71 21.18 164 18286 317011 90292986
Fatigue 53.52 21.18 409 18041 1153614 89456383
Pharyngeal dyskinesia 53.02 21.18 9 18441 36 90609961
Chest discomfort 50.00 21.18 96 18354 138269 90471728
Treatment failure 49.89 21.18 3 18447 303925 90306072
Epistaxis 49.39 21.18 73 18377 85052 90524945
Drug intolerance 49.22 21.18 15 18435 447576 90162421
Triple negative breast cancer 47.88 21.18 12 18438 392 90609605
Tonsillar haemorrhage 47.55 21.18 11 18439 254 90609743
Asthenia 44.90 21.18 221 18229 533530 90076467
Erythema 44.00 21.18 124 18326 229122 90380875
Abdominal pain 43.93 21.18 178 18272 395543 90214454
Alopecia areata 43.04 21.18 16 18434 1999 90607998
Swelling 41.02 21.18 17 18433 419041 90190956
Weight increased 40.83 21.18 17 18433 417910 90192087
Ascites 40.03 21.18 49 18401 47691 90562306
Wound 39.53 21.18 7 18443 302973 90307024
Hepatic enzyme increased 38.03 21.18 13 18437 360723 90249274
Leukopenia 37.76 21.18 71 18379 100639 90509358
Hair colour changes 37.67 21.18 17 18433 3477 90606520
Product contamination microbial 36.43 21.18 9 18441 277 90609720
Musculoskeletal stiffness 36.27 21.18 8 18442 296524 90313473
Maternal exposure during pregnancy 36.22 21.18 14 18436 360049 90249948
Pneumonitis 34.89 21.18 44 18406 44126 90565871
Drug hypersensitivity 33.71 21.18 27 18423 463582 90146415
Necrotising colitis 33.70 21.18 12 18438 1326 90608671
Aortitis 33.60 21.18 12 18438 1338 90608659
Hair texture abnormal 32.92 21.18 17 18433 4670 90605327
Stridor 32.57 21.18 17 18433 4776 90605221
Product dose omission issue 31.63 21.18 10 18440 291677 90318320
Dehydration 31.43 21.18 99 18351 194348 90415649
Malignant neoplasm progression 31.31 21.18 68 18382 106802 90503195
Madarosis 30.91 21.18 15 18435 3614 90606383
Folliculitis 30.75 21.18 3 18447 204350 90405647
Sinusitis 30.35 21.18 16 18434 343072 90266925
Mobility decreased 30.19 21.18 7 18443 250727 90359270
Oropharyngeal pain 30.06 21.18 70 18380 115117 90494880
Metastases to liver 29.90 21.18 33 18417 28774 90581223
Product counterfeit 29.77 21.18 7 18443 174 90609823
Hypoalbuminaemia 29.36 21.18 25 18425 15872 90594125
Peripheral sensory neuropathy 29.15 21.18 20 18430 9230 90600767
Pancytopenia 29.14 21.18 71 18379 120192 90489805
Intentional product use issue 28.31 21.18 5 18445 216887 90393110
Dysgeusia 27.54 21.18 43 18407 52517 90557480
Polyneuropathy 27.03 21.18 26 18424 19315 90590682
Nasal herpes 26.99 21.18 9 18441 817 90609180
Nasopharyngitis 26.83 21.18 26 18424 407078 90202919
Chemotherapy 26.63 21.18 11 18439 1816 90608181
Palmar erythema 26.15 21.18 11 18439 1900 90608097
Musculoskeletal chest pain 26.03 21.18 28 18422 23722 90586275
Oral candidiasis 25.93 21.18 34 18416 35421 90574576
Transmission of an infectious agent via product 25.88 21.18 6 18444 140 90609857
Hepatic function abnormal 25.84 21.18 39 18411 46249 90563748
Toxicity to various agents 24.61 21.18 14 18436 287832 90322165
Therapeutic product effect incomplete 24.17 21.18 5 18445 193891 90416106
Infection 24.00 21.18 23 18427 362071 90247926
Cytokine release syndrome 23.91 21.18 29 18421 27944 90582053
Blister 23.89 21.18 11 18439 254987 90355010
Hypomagnesaemia 22.80 21.18 32 18418 35556 90574441
Exposure during pregnancy 22.78 21.18 10 18440 238400 90371597
Gastrointestinal disorder 22.65 21.18 12 18438 256675 90353322
Burkholderia cepacia complex sepsis 22.50 21.18 3 18447 0 90609997
Overdose 22.02 21.18 3 18447 157706 90452291
Vascular pain 21.88 21.18 8 18442 954 90609043

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
Neutrophil count decreased 182.01 21.39 157 13802 63258 42544118
Nausea 181.17 21.39 399 13560 396400 42210976
Febrile neutropenia 166.93 21.39 251 13708 185452 42421924
Decreased appetite 155.32 21.39 248 13711 192889 42414487
Death 125.10 21.39 387 13572 470798 42136578
Drug ineffective 108.58 21.39 36 13923 630161 41977215
Constipation 86.03 21.39 174 13785 162117 42445259
Vomiting 75.56 21.39 237 13722 289486 42317890
Platelet count decreased 75.09 21.39 150 13809 138431 42468945
Neutropenia 70.32 21.39 182 13777 199249 42408127
Anaemia 70.07 21.39 226 13733 280052 42327324
Diarrhoea 69.42 21.39 316 13643 460533 42146843
Hiccups 68.12 21.39 45 13914 12126 42595250
Stomatitis 67.81 21.39 83 13876 50246 42557130
Pyrexia 66.76 21.39 280 13679 393762 42213614
White blood cell count decreased 62.80 21.39 122 13837 110274 42497102
Off label use 62.16 21.39 388 13571 637947 41969429
Fatigue 58.44 21.39 289 13670 435352 42172024
Toxicity to various agents 54.06 21.39 6 13953 229130 42378246
Myelosuppression 48.56 21.39 63 13896 40398 42566978
Neuropathy peripheral 43.31 21.39 100 13859 101753 42505623
Interstitial lung disease 42.51 21.39 85 13874 78377 42528999
Disease progression 40.54 21.39 121 13838 143535 42463841
Malignant neoplasm progression 35.13 21.39 96 13863 108304 42499072
Thrombocytopenia 32.65 21.39 136 13823 190143 42417233
Hypoalbuminaemia 31.83 21.39 32 13927 15578 42591798
Cytokine release syndrome 31.33 21.39 54 13905 44473 42562903
Intravascular haemolysis 30.21 21.39 10 13949 548 42606828
Leukopenia 29.16 21.39 71 13888 74675 42532701
Pneumonia acinetobacter 28.90 21.39 8 13951 237 42607139
Condition aggravated 28.61 21.39 26 13933 260728 42346648
Hypokalaemia 27.84 21.39 68 13891 71653 42535723
Device related infection 26.57 21.39 33 13926 20246 42587130
Microangiopathic haemolytic anaemia 26.53 21.39 11 13948 1136 42606240
Infusion related reaction 26.15 21.39 60 13899 60746 42546630
Product dose omission issue 24.41 21.39 10 13949 154355 42453021
Subclavian artery occlusion 23.92 21.39 6 13953 120 42607256
Enterocolitis 23.32 21.39 22 13937 9907 42597469
Anaemia of malignant disease 22.66 21.39 8 13951 533 42606843
Lymphocyte count decreased 22.61 21.39 36 13923 27773 42579603
Renal ischaemia 22.57 21.39 11 13948 1659 42605717

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 583.89 18.62 539 26747 316228 110245785
Neutrophil count decreased 501.83 18.62 333 26953 120608 110441405
Neutropenia 349.09 18.62 445 26841 374175 110187838
Nausea 275.32 18.62 794 26492 1234896 109327117
Decreased appetite 259.30 18.62 439 26847 475407 110086606
Platelet count decreased 214.61 18.62 274 27012 230169 110331844
Constipation 195.82 18.62 331 26955 357455 110204558
Anaemia 189.80 18.62 417 26869 546669 110015344
Triple negative breast cancer 183.23 18.62 39 27247 493 110561520
Drug ineffective 170.07 18.62 82 27204 1520458 109041555
Myelosuppression 158.68 18.62 153 27133 94187 110467826
Flushing 157.88 18.62 160 27126 104576 110457437
Neuropathy peripheral 154.08 18.62 205 27081 179072 110382941
Pyrexia 138.21 18.62 510 26776 897755 109664258
White blood cell count decreased 135.77 18.62 220 27066 229170 110332843
Interstitial lung disease 120.71 18.62 160 27126 139174 110422839
Thrombocytopenia 108.53 18.62 255 27031 348630 110213383
Vomiting 104.92 18.62 473 26813 910202 109651811
Hypokalaemia 102.53 18.62 171 27115 182277 110379736
Diarrhoea 100.88 18.62 549 26737 1138956 109423057
Mucosal inflammation 82.61 18.62 110 27176 96031 110465982
Colony stimulating factor therapy 81.80 18.62 21 27265 621 110561392
Malignant neoplasm progression 81.70 18.62 151 27135 174416 110387597
Leukopenia 75.09 18.62 133 27153 148658 110413355
Death 73.67 18.62 354 26932 698515 109863498
Hiccups 72.26 18.62 43 27243 12826 110549187
Condition aggravated 69.84 18.62 48 27238 734788 109827225
Hypoalbuminaemia 68.53 18.62 57 27229 28917 110533096
Toxicity to various agents 66.82 18.62 18 27268 480537 110081476
Joint swelling 64.64 18.62 15 27271 442830 110119183
Cytokine release syndrome 64.36 18.62 83 27203 70223 110491790
Drug intolerance 62.96 18.62 12 27274 406500 110155513
Pneumonitis 55.91 18.62 81 27205 76450 110485563
Disease progression 55.79 18.62 159 27127 243875 110318138
Rheumatoid arthritis 52.94 18.62 6 27280 299607 110262406
Peripheral sensory neuropathy 50.60 18.62 38 27248 16642 110545371
Infusion related reaction 50.59 18.62 207 27079 380955 110181058
Enterocolitis 48.43 18.62 39 27247 18910 110543103
Aspartate aminotransferase increased 46.50 18.62 114 27172 159822 110402191
Weight increased 44.57 18.62 24 27262 419620 110142393
Chest discomfort 44.41 18.62 118 27168 173730 110388283
Cystitis haemorrhagic 44.30 18.62 31 27255 12178 110549835
Hypomagnesaemia 44.24 18.62 64 27222 60306 110501707
Palmar-plantar erythrodysaesthesia syndrome 43.25 18.62 52 27234 40973 110521040
Polyneuropathy 42.98 18.62 46 27240 31966 110530047
Lower respiratory tract infection 42.62 18.62 5 27281 243101 110318912
Musculoskeletal stiffness 41.77 18.62 9 27277 279813 110282200
Pharyngeal dyskinesia 41.59 18.62 8 27278 58 110561955
Wound 40.65 18.62 5 27281 234432 110327581
Arthralgia 38.98 18.62 84 27202 779548 109782465
Alopecia areata 38.78 18.62 16 27270 2171 110559842
Dysgeusia 38.47 18.62 65 27221 69920 110492093
Product dose omission issue 37.84 18.62 16 27270 321766 110240247
Peritonitis 37.14 18.62 43 27243 32564 110529449
Lymphocyte count decreased 36.68 18.62 57 27229 57186 110504827
Sinusitis 36.11 18.62 14 27272 296674 110265339
Erythema 36.08 18.62 155 27131 291292 110270721
Overdose 35.97 18.62 7 27279 233787 110328226
Therapeutic product effect incomplete 35.95 18.62 6 27280 223799 110338214
Stomatitis 35.22 18.62 146 27140 270096 110291917
Disseminated intravascular coagulation 35.08 18.62 47 27239 41239 110520774
Epistaxis 34.83 18.62 90 27196 130282 110431731
Hepatic enzyme increased 34.58 18.62 18 27268 320874 110241139
Gastrointestinal perforation 34.44 18.62 22 27264 7434 110554579
Drug hypersensitivity 34.15 18.62 37 27249 454053 110107960
Oral candidiasis 33.60 18.62 48 27238 44712 110517301
Swelling 33.19 18.62 23 27263 351018 110210995
Alanine aminotransferase increased 32.91 18.62 110 27176 183663 110378350
Maternal exposure during pregnancy 32.76 18.62 11 27275 254872 110307141
Hair texture abnormal 32.57 18.62 17 27269 3937 110558076
Hepatic function abnormal 31.84 18.62 69 27217 89226 110472787
Injection site pain 30.35 18.62 4 27282 177918 110384095
Fall 30.15 18.62 65 27221 603417 109958596
Back pain 30.07 18.62 175 27111 370821 110191192
Abdominal pain 30.04 18.62 223 27063 512766 110049247
Hair colour changes 29.81 18.62 17 27269 4684 110557329
Dehydration 29.62 18.62 142 27144 279369 110282644
Tonsillar haemorrhage 29.59 18.62 8 27278 290 110561723
Madarosis 28.84 18.62 15 27271 3448 110558565
Bone marrow failure 28.24 18.62 51 27235 57797 110504216
Necrotising colitis 28.23 18.62 12 27274 1753 110560260
Peripheral swelling 28.13 18.62 35 27251 403999 110158014
Intentional product use issue 28.08 18.62 13 27273 247893 110314120
Folliculitis 28.05 18.62 4 27282 167649 110394364
Dyspnoea 28.01 18.62 405 26881 1106467 109455546
Type 2 diabetes mellitus 27.91 18.62 5 27281 177227 110384786
Ileus 27.68 18.62 36 27250 30693 110531320
Pneumonia acinetobacter 27.40 18.62 8 27278 385 110561628
Anaemia of malignant disease 27.31 18.62 10 27276 986 110561027
Anaphylactic shock 27.17 18.62 47 27239 51499 110510514
Intravascular haemolysis 27.01 18.62 10 27276 1017 110560996
Arteritis 26.09 18.62 10 27276 1119 110560894
Enterocolitis infectious 26.08 18.62 14 27272 3430 110558583
Dermatitis acneiform 26.00 18.62 23 27263 12672 110549341
Nasal herpes 25.99 18.62 9 27277 754 110561259
Vascular pain 25.72 18.62 10 27276 1163 110560850
Pain 25.62 18.62 135 27151 954820 109607193
Bacteraemia 25.49 18.62 41 27245 42349 110519664
Burkholderia cepacia complex sepsis 25.19 18.62 4 27282 7 110562006
Oropharyngeal pain 25.13 18.62 82 27204 135194 110426819
Hospitalisation 24.79 18.62 3 27283 142490 110419523
Asthenia 24.63 18.62 269 27017 688730 109873283
Fatigue 24.38 18.62 428 26858 1215530 109346483
Product counterfeit 24.32 18.62 7 27279 320 110561693
Microangiopathic haemolytic anaemia 23.95 18.62 11 27275 1932 110560081
Stridor 23.84 18.62 17 27269 6878 110555135
Metastases to liver 23.74 18.62 36 27250 35350 110526663
Subclavian artery occlusion 23.72 18.62 6 27280 167 110561846
Sepsis 23.72 18.62 150 27136 327196 110234817
Embolism venous 23.65 18.62 15 27271 5008 110557005
Therapy non-responder 23.59 18.62 5 27281 157302 110404711
Aortitis 23.56 18.62 11 27275 2004 110560009
Exposure to unspecified agent 23.45 18.62 4 27282 13 110562000
Osteoarthritis 23.26 18.62 8 27278 182615 110379398
Mobility decreased 23.18 18.62 15 27271 237407 110324606
Chemotherapy 22.90 18.62 11 27275 2135 110559878
Night sweats 22.88 18.62 3 27283 133980 110428033
Product contamination microbial 22.83 18.62 9 27277 1085 110560928
Nasopharyngitis 22.71 18.62 39 27247 394322 110167691
Inappropriate antidiuretic hormone secretion 22.10 18.62 34 27252 33817 110528196
Renal ischaemia 22.07 18.62 11 27275 2312 110559701
Loss of personal independence in daily activities 22.02 18.62 5 27281 150015 110411998
Psoriasis 21.94 18.62 4 27282 139989 110422024
Ultrasound foetal abnormal 21.73 18.62 5 27281 92 110561921
Oxygen saturation decreased 21.37 18.62 86 27200 156896 110405117
Hypoproteinaemia 21.34 18.62 15 27271 5930 110556083
Memory impairment 21.28 18.62 11 27275 196933 110365080
Embolism 21.15 18.62 23 27263 16266 110545747
Cholinergic syndrome 21.12 18.62 9 27277 1323 110560690
Ascites 20.72 18.62 60 27226 92748 110469265
Confusional state 20.59 18.62 54 27232 468626 110093387
Immune-mediated enterocolitis 19.96 18.62 18 27268 10167 110551846
Off label use 19.91 18.62 497 26789 1499688 109062325
Impaired healing 19.79 18.62 12 27274 196705 110365308
Infusion site vesicles 19.75 18.62 7 27279 628 110561385
Non-small cell lung cancer 19.57 18.62 16 27270 7919 110554094
Hypophagia 19.14 18.62 41 27245 52585 110509428
Palmar erythema 19.11 18.62 10 27276 2328 110559685
Blister 18.83 18.62 17 27269 227359 110334654
Tumour necrosis 18.72 18.62 10 27276 2426 110559587
Eye movement disorder 18.68 18.62 17 27269 9711 110552302
Arthritis 18.65 18.62 9 27277 167577 110394436

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A04AA05 ALIMENTARY TRACT AND METABOLISM
ANTIEMETICS AND ANTINAUSEANTS
ANTIEMETICS AND ANTINAUSEANTS
Serotonin (5HT3) antagonists
ATC A04AA55 ALIMENTARY TRACT AND METABOLISM
ANTIEMETICS AND ANTINAUSEANTS
ANTIEMETICS AND ANTINAUSEANTS
Serotonin (5HT3) antagonists
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
FDA MoA N0000175817 Serotonin 3 Receptor Antagonists
FDA EPC N0000175818 Serotonin-3 Receptor Antagonist
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:48279 serotonergic antagonist
CHEBI has role CHEBI:50919 antiemetic
CHEBI has role CHEBI:66981 ophthalmology drug

Related Drugs by ATC class:

A04AA Serotonin (5HT3) antagonists 4 drugs
dolasetrongranisetronondansetrontropisetron

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

DiseaseRelationSNOMED_IDDOID
Chemotherapy-induced nausea and vomiting indication 18846006
Prevention of Post-Operative Nausea and Vomiting indication
Prevention of Glucocorticoid-Induced Osteoporosis off-label use
Lupus anticoagulant disorder contraindication 19267009
Hypertensive disorder contraindication 38341003 DOID:10763
Thrombosis of retinal vein contraindication 46085004
Chronic heart failure contraindication 48447003
Atrial fibrillation contraindication 49436004 DOID:0060224
Thrombophlebitis contraindication 64156001 DOID:3875
Deep venous thrombosis contraindication 128053003
Impaired renal function disorder contraindication 197663003
Cerebrovascular accident contraindication 230690007
Pulmonary thromboembolism contraindication 233935004
Thrombophilia contraindication 234467004 DOID:2452
Disease of liver contraindication 235856003 DOID:409
Transient ischemic attack contraindication 266257000 DOID:224
Pregnancy, function contraindication 289908002
Hypertriglyceridemia contraindication 302870006
Cardiovascular event risk contraindication 395112001
Breastfeeding (mother) contraindication 413712001
Disorder of coronary artery contraindication 414024009
Smokes tobacco daily contraindication 449868002




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.52 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
300MG;EQ 0.5MG BASE AKYNZEO HELSINN HLTHCARE N205718 Oct. 10, 2014 RX CAPSULE ORAL 11559523 Nov. 18, 2030 METHOD OF TREATING EMESIS
300MG;EQ 0.5MG BASE AKYNZEO HELSINN HLTHCARE N205718 Oct. 10, 2014 RX CAPSULE ORAL 12042494 Nov. 18, 2030 METHOD OF TREATING EMESIS
300MG;EQ 0.5MG BASE AKYNZEO HELSINN HLTHCARE N205718 Oct. 10, 2014 RX CAPSULE ORAL 8623826 Nov. 18, 2030 USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF CANCER CHEMOTHERAPY, INCLUDING, BUT NOT LIMITED TO, HIGHLY EMETOGENIC CHEMOTHERAPY
300MG;EQ 0.5MG BASE AKYNZEO HELSINN HLTHCARE N205718 Oct. 10, 2014 RX CAPSULE ORAL 9186357 Nov. 18, 2030 USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF CANCER CHEMOTHERAPY, INCLUDING, BUT NOT LIMITED TO, HIGHLY EMETOGENIC CHEMOTHERAPY
300MG;EQ 0.5MG BASE AKYNZEO HELSINN HLTHCARE N205718 Oct. 10, 2014 RX CAPSULE ORAL 9943515 Nov. 18, 2030 USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF CANCER CHEMOTHERAPY, INCLUDING, BUT NOT LIMITED TO, HIGHLY EMETOGENIC CHEMOTHERAPY
EQ 235MG BASE/20ML (EQ 11.75MG BASE/ML);EQ 0.25MG BASE/20ML (EQ 0.0125MG BASE/ML) AKYNZEO HELSINN HLTHCARE N210493 May 27, 2020 RX SOLUTION INTRAVENOUS 9186357 Nov. 18, 2030 USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY
EQ 235MG BASE/VIAL;EQ 0.25MG BASE/VIAL AKYNZEO HELSINN HLTHCARE N210493 April 19, 2018 DISCN POWDER INTRAVENOUS 9186357 Nov. 18, 2030 USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY
300MG;EQ 0.5MG BASE AKYNZEO HELSINN HLTHCARE N205718 Oct. 10, 2014 RX CAPSULE ORAL 10828297 Dec. 17, 2030 USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF CANCER CHEMOTHERAPY, INCLUDING, BUT NOT LIMITED TO, HIGHLY EMETOGENIC CHEMOTHERAPY
EQ 235MG BASE/20ML (EQ 11.75MG BASE/ML);EQ 0.25MG BASE/20ML (EQ 0.0125MG BASE/ML) AKYNZEO HELSINN HLTHCARE N210493 May 27, 2020 RX SOLUTION INTRAVENOUS 10828297 Dec. 17, 2030 USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY
EQ 235MG BASE/VIAL;EQ 0.25MG BASE/VIAL AKYNZEO HELSINN HLTHCARE N210493 April 19, 2018 DISCN POWDER INTRAVENOUS 10828297 Dec. 17, 2030 USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY
300MG;EQ 0.5MG BASE AKYNZEO HELSINN HLTHCARE N205718 Oct. 10, 2014 RX CAPSULE ORAL 9271975 Sept. 9, 2031 USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF CANCER CHEMOTHERAPY, INCLUDING, BUT NOT LIMITED TO, HIGHLY EMETOGENIC CHEMOTHERAPY
EQ 235MG BASE/20ML (EQ 11.75MG BASE/ML);EQ 0.25MG BASE/20ML (EQ 0.0125MG BASE/ML) AKYNZEO HELSINN HLTHCARE N210493 May 27, 2020 RX SOLUTION INTRAVENOUS 10208073 May 23, 2032 USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY
EQ 235MG BASE/20ML (EQ 11.75MG BASE/ML);EQ 0.25MG BASE/20ML (EQ 0.0125MG BASE/ML) AKYNZEO HELSINN HLTHCARE N210493 May 27, 2020 RX SOLUTION INTRAVENOUS 8895586 May 23, 2032 USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY
EQ 235MG BASE/20ML (EQ 11.75MG BASE/ML);EQ 0.25MG BASE/20ML (EQ 0.0125MG BASE/ML) AKYNZEO HELSINN HLTHCARE N210493 May 27, 2020 RX SOLUTION INTRAVENOUS 9403772 May 23, 2032 USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY
EQ 235MG BASE/VIAL;EQ 0.25MG BASE/VIAL AKYNZEO HELSINN HLTHCARE N210493 April 19, 2018 DISCN POWDER INTRAVENOUS 10208073 May 23, 2032 USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY
EQ 235MG BASE/VIAL;EQ 0.25MG BASE/VIAL AKYNZEO HELSINN HLTHCARE N210493 April 19, 2018 DISCN POWDER INTRAVENOUS 8895586 May 23, 2032 USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY
EQ 235MG BASE/VIAL;EQ 0.25MG BASE/VIAL AKYNZEO HELSINN HLTHCARE N210493 April 19, 2018 DISCN POWDER INTRAVENOUS 9403772 May 23, 2032 USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY

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 10.50 CHEMBL CHEMBL
Serotonin 3 receptor (5HT3) Ion channel Kd 9.74 CHEMBL

External reference:

IDSource
4021398 VUID
N0000148816 NUI
D07175 KEGG_DRUG
135729-62-3 SECONDARY_CAS_RN
4021398 VANDF
C0220578 UMLSCUI
CHEBI:85161 CHEBI
7A9 PDB_CHEM_ID
CHEMBL1189679 ChEMBL_ID
DB00377 DRUGBANK_ID
CHEMBL1720 ChEMBL_ID
D000077924 MESH_DESCRIPTOR_UI
6337614 PUBCHEM_CID
7486 IUPHAR_LIGAND_ID
7407 INN_ID
5D06587D6R UNII
397405 RXNORM
17493 MMSL
272498 MMSL
34848 MMSL
47149 MMSL
d04888 MMSL
002715 NDDF
002719 NDDF
404851001 SNOMEDCT_US
404852008 SNOMEDCT_US
412263008 SNOMEDCT_US
5D06587D6R INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Palonosetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0703-4094 INJECTION, SOLUTION 0.25 mg INTRAVENOUS ANDA 26 sections
Palonosetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0781-3312 INJECTION, SOLUTION 0.25 mg INTRAVENOUS ANDA 26 sections
Palonosetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0781-3415 INJECTION, SOLUTION 0.25 mg INTRAVENOUS ANDA 26 sections
Palonosetron HUMAN PRESCRIPTION DRUG LABEL 1 16714-834 INJECTION, SOLUTION 0.05 mg INTRAVENOUS ANDA 26 sections
palonosetron hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 25021-783 INJECTION, SOLUTION 0.05 mg INTRAVENOUS ANDA 27 sections
Palonosetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 36000-326 INJECTION 0.25 mg INTRAVENOUS ANDA 25 sections
Palonosetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 36000-326 INJECTION 0.25 mg INTRAVENOUS ANDA 25 sections
Palonosetron HUMAN PRESCRIPTION DRUG LABEL 1 55111-694 INJECTION, SOLUTION 0.05 mg INTRAVENOUS ANDA 26 sections
Palonosetron Hydrochloride Human Prescription Drug Label 1 55150-186 INJECTION, SOLUTION 0.25 mg INTRAVENOUS ANDA 26 sections
Palonosetron HUMAN PRESCRIPTION DRUG LABEL 1 60505-6193 INJECTION 0.25 mg INTRAVENOUS ANDA 26 sections
Palonosetron HUMAN PRESCRIPTION DRUG LABEL 1 60505-6439 INJECTION 0.25 mg INTRAVENOUS ANDA 26 sections
PALONOSETRON HUMAN PRESCRIPTION DRUG LABEL 1 63323-673 INJECTION, SOLUTION 0.25 mg INTRAVENOUS ANDA 27 sections
PALONOSETRON HUMAN PRESCRIPTION DRUG LABEL 1 63323-673 INJECTION, SOLUTION 0.25 mg INTRAVENOUS ANDA 27 sections
Palonosetron HUMAN PRESCRIPTION DRUG LABEL 1 67184-0514 INJECTION 0.25 mg INTRAVENOUS ANDA 26 sections
Palonosetron HUMAN PRESCRIPTION DRUG LABEL 1 67184-0515 INJECTION 0.08 mg INTRAVENOUS ANDA 26 sections
Palonosetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 67457-317 INJECTION, SOLUTION 0.25 mg INTRAVENOUS ANDA 27 sections
Palonosetron HUMAN PRESCRIPTION DRUG LABEL 1 68001-355 INJECTION, SOLUTION 0.05 mg INTRAVENOUS ANDA 25 sections
Palonosetron HUMAN PRESCRIPTION DRUG LABEL 1 68001-708 INJECTION 0.25 mg INTRAVENOUS ANDA 26 sections
palonosetron hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 69097-927 INJECTION 0.25 mg INTRAVENOUS NDA authorized generic 26 sections
AKYNZEO HUMAN PRESCRIPTION DRUG LABEL 2 69639-101 CAPSULE 0.50 mg ORAL NDA 26 sections
AKYNZEO HUMAN PRESCRIPTION DRUG LABEL 2 69639-102 INJECTION 0.28 mg INTRAVENOUS NDA 26 sections
AKYNZEO HUMAN PRESCRIPTION DRUG LABEL 2 69639-105 INJECTION 0.28 mg INTRAVENOUS NDA 26 sections
AKYNZEO HUMAN PRESCRIPTION DRUG LABEL 2 69639-106 INJECTION 0.28 mg INTRAVENOUS NDA 26 sections
Palonosetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 71288-409 INJECTION, SOLUTION 0.25 mg INTRAVENOUS ANDA 27 sections
Palonosetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 83634-777 INJECTION, SOLUTION 0.05 mg INTRAVENOUS ANDA 28 sections
posfrea HUMAN PRESCRIPTION DRUG LABEL 1 83831-104 INJECTION, SOLUTION 0.08 mg INTRAVENOUS NDA 25 sections
posfrea HUMAN PRESCRIPTION DRUG LABEL 1 83831-105 INJECTION, SOLUTION 0.25 mg INTRAVENOUS NDA 25 sections