palonosetron 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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

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 396.15 18.85 512 17854 373869 63096787
Febrile neutropenia 314.87 18.85 266 18100 118183 63352473
Neutropenia 259.62 18.85 285 18081 174720 63295936
Nausea 198.38 18.85 617 17749 853854 62616802
Neutrophil count decreased 190.72 18.85 146 18220 56260 63414396
Flushing 150.51 18.85 144 18222 74943 63395713
Drug ineffective 132.81 18.85 69 18297 1044696 62425960
Constipation 130.05 18.85 233 18133 224710 63245946
Decreased appetite 125.13 18.85 244 18122 250808 63219848
Vomiting 124.36 18.85 399 17967 559218 62911438
Neuropathy peripheral 118.62 18.85 155 18211 113512 63357144
Disease progression 110.79 18.85 156 18210 122602 63348054
Palmar-plantar erythrodysaesthesia syndrome 78.65 18.85 60 18306 22955 63447701
Mucosal inflammation 77.38 18.85 81 18285 46847 63423809
Platelet count decreased 75.73 18.85 127 18239 115995 63354661
Off label use 72.79 18.85 385 17981 674077 62796579
Anaemia 70.16 18.85 215 18151 293215 63177441
Dyspnoea 66.92 18.85 371 17995 660942 62809714
Erythema 66.69 18.85 153 18213 175598 63295058
Colony stimulating factor therapy 61.09 18.85 15 18351 312 63470344
Abdominal pain 57.51 18.85 201 18165 293255 63177401
Pyrexia 53.65 18.85 273 18093 470205 63000451
Drug intolerance 51.40 18.85 13 18353 308648 63162008
Chest discomfort 51.15 18.85 104 18262 109865 63360791
Pharyngeal dyskinesia 49.86 18.85 9 18357 36 63470620
Joint swelling 48.74 18.85 17 18349 327649 63143007
Condition aggravated 48.68 18.85 28 18338 402189 63068467
Treatment failure 45.80 18.85 3 18363 199040 63271616
Product dose omission issue 44.99 18.85 7 18359 234306 63236350
Myelosuppression 44.69 18.85 44 18322 23659 63446997
Back pain 44.22 18.85 172 18194 263973 63206683
Alopecia areata 43.88 18.85 17 18349 1668 63468988
Tonsillar haemorrhage 43.88 18.85 11 18355 250 63470406
Dehydration 43.20 18.85 129 18237 173225 63297431
Hypokalaemia 42.27 18.85 93 18273 103711 63366945
Thrombocytopenia 41.04 18.85 116 18250 151041 63319615
Injection site phlebitis 40.55 18.85 9 18357 118 63470538
Maternal exposure during pregnancy 39.15 18.85 8 18358 220054 63250602
Diarrhoea 37.77 18.85 343 18023 715023 62755633
Interstitial lung disease 36.76 18.85 65 18301 61843 63408813
Therapeutic product effect decreased 36.56 18.85 6 18360 193181 63277475
Asthenia 36.49 18.85 212 18154 383392 63087264
Product contamination microbial 35.67 18.85 9 18357 210 63470446
Ascites 35.55 18.85 51 18315 40677 63429979
Epistaxis 35.26 18.85 70 18296 72655 63398001
Glossodynia 35.12 18.85 5 18361 178871 63291785
White blood cell count decreased 35.10 18.85 104 18262 139000 63331656
Infusion related reaction 34.86 18.85 152 18214 245369 63225287
Hair colour changes 33.78 18.85 17 18349 3110 63467546
Madarosis 31.10 18.85 16 18350 3065 63467591
Nasopharyngitis 30.30 18.85 18 18348 254239 63216417
Fatigue 30.21 18.85 390 17976 887638 62583018
Weight increased 28.97 18.85 20 18346 260772 63209884
Hair texture abnormal 28.92 18.85 17 18349 4226 63466430
Fall 28.90 18.85 43 18323 392291 63078365
Dermatitis acneiform 28.85 18.85 18 18348 4978 63465678
Aortitis 28.42 18.85 11 18355 1076 63469580
Product counterfeit 28.27 18.85 7 18359 151 63470505
Wound 26.91 18.85 7 18359 163256 63307400
Leukopenia 26.78 18.85 65 18301 77225 63393431
Musculoskeletal stiffness 26.70 18.85 10 18356 184608 63286048
Toxicity to various agents 26.11 18.85 20 18346 247230 63223426
Oral candidiasis 25.15 18.85 32 18334 22766 63447890
Bone pain 24.58 18.85 51 18315 54590 63416066
Hepatic enzyme increased 24.56 18.85 14 18352 202314 63268342
Product use issue 24.37 18.85 17 18349 220503 63250153
Sinusitis 24.36 18.85 18 18348 226635 63244021
Anaphylactic shock 24.24 18.85 32 18334 23601 63447055
Intentional product use issue 24.13 18.85 4 18362 127888 63342768
Tachycardia 24.00 18.85 82 18284 118074 63352582
Drug hypersensitivity 23.90 18.85 33 18333 310654 63160002
Gastrointestinal perforation 23.82 18.85 14 18352 3477 63467179
Stridor 23.75 18.85 14 18352 3496 63467160
Transmission of an infectious agent via product 23.58 18.85 6 18360 145 63470511
Therapeutic product effect incomplete 23.40 18.85 4 18362 125052 63345604
Mobility decreased 22.39 18.85 4 18362 121155 63349501
Musculoskeletal chest pain 22.33 18.85 29 18337 21054 63449602
Throat tightness 21.48 18.85 31 18335 24856 63445800
Burkholderia cepacia complex sepsis 21.45 18.85 3 18363 0 63470656
Swelling 21.43 18.85 29 18337 275349 63195307
Chemotherapy 21.32 18.85 10 18356 1569 63469087
Infection 21.21 18.85 21 18345 229152 63241504
Vascular pain 20.73 18.85 8 18358 776 63469880
Stomatitis 20.51 18.85 87 18279 138638 63332018
Bone marrow failure 20.36 18.85 33 18333 29257 63441399
Laryngospasm 20.29 18.85 12 18354 3016 63467640
Palmar erythema 20.25 18.85 10 18356 1757 63468899
Infusion site vesicles 19.76 18.85 7 18359 534 63470122
Metastases to liver 19.75 18.85 29 18337 23610 63447046
Malignant neoplasm progression 19.38 18.85 60 18306 82061 63388595
Exposure to unspecified agent 19.37 18.85 3 18363 3 63470653

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
Death 146.16 19.73 410 13207 397639 34545675
Neutrophil count decreased 138.08 19.73 132 13485 50972 34892342
Febrile neutropenia 133.52 19.73 211 13406 136638 34806676
Nausea 127.37 19.73 353 13264 339555 34603759
Decreased appetite 115.80 19.73 221 13396 166171 34777143
Constipation 99.01 19.73 185 13432 136797 34806517
Neutropenia 89.63 19.73 192 13425 156586 34786728
Drug ineffective 77.44 19.73 41 13576 456710 34486604
Stomatitis 77.42 19.73 89 13528 42425 34900889
Off label use 67.09 19.73 331 13286 419193 34524121
White blood cell count decreased 66.49 19.73 127 13490 95318 34847996
Vomiting 62.65 19.73 225 13392 247396 34695918
Interstitial lung disease 62.56 19.73 100 13517 65182 34878132
Platelet count decreased 56.49 19.73 136 13481 119581 34823733
Dermatitis acneiform 55.79 19.73 33 13584 6156 34937158
Diarrhoea 54.16 19.73 296 13321 389616 34553698
Fatigue 50.52 19.73 280 13337 370373 34572941
Toxicity to various agents 43.74 19.73 12 13605 200350 34742964
Neuropathy peripheral 42.96 19.73 98 13519 83165 34860149
Pyrexia 41.65 19.73 246 13371 332767 34610547
Hiccups 37.00 19.73 31 13586 10051 34933263
Leukopenia 36.97 19.73 78 13539 62778 34880536
Disease progression 35.06 19.73 107 13510 107970 34835344
Anaemia 34.87 19.73 181 13436 233154 34710160
Flushing 34.28 19.73 52 13565 32368 34910946
Drug interaction 31.70 19.73 25 13592 225921 34717393
Device related infection 31.20 19.73 36 13581 17201 34926113
Myelosuppression 31.18 19.73 38 13579 19227 34924087
Intravascular haemolysis 30.28 19.73 10 13607 456 34942858
Condition aggravated 29.93 19.73 19 13598 192177 34751137
Thrombocytopenia 29.70 19.73 130 13487 156117 34787197
Microangiopathic haemolytic anaemia 27.12 19.73 11 13606 901 34942413
Overdose 25.10 19.73 3 13614 91056 34852258
Malignant neoplasm progression 24.74 19.73 83 13534 87963 34855351
Infusion related reaction 24.67 19.73 60 13557 52997 34890317
Product dose omission issue 24.58 19.73 8 13609 119703 34823611
Disseminated intravascular coagulation 24.50 19.73 36 13581 21780 34921534
Colon cancer metastatic 23.79 19.73 12 13605 1635 34941679
Alopecia 22.87 19.73 37 13580 24318 34918996
Malignant ascites 22.74 19.73 8 13609 442 34942872
Subclavian artery occlusion 22.66 19.73 6 13611 125 34943189
Cholinergic syndrome 20.67 19.73 8 13609 579 34942735
Deep vein thrombosis 20.57 19.73 64 13553 65184 34878130
Cytokine release syndrome 20.46 19.73 34 13583 22843 34920471

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 458.68 18.02 457 24647 230542 79488742
Neutrophil count decreased 320.60 18.02 253 24851 93706 79625578
Neutropenia 294.14 18.02 405 24699 287305 79431979
Nausea 208.49 18.02 716 24388 956480 78762804
Decreased appetite 175.94 18.02 354 24750 342064 79377220
Flushing 173.41 18.02 174 24930 88094 79631190
Constipation 145.71 18.02 293 24811 282757 79436527
Platelet count decreased 145.46 18.02 237 24867 194427 79524857
Neuropathy peripheral 136.64 18.02 194 24910 141111 79578173
Drug ineffective 131.84 18.02 90 25014 1080823 78638461
Vomiting 110.05 18.02 457 24647 665371 79053913
Interstitial lung disease 105.01 18.02 152 24952 112448 79606836
White blood cell count decreased 102.90 18.02 200 24904 188088 79531196
Anaemia 93.56 18.02 330 24774 444685 79274599
Pyrexia 89.63 18.02 436 24668 678273 79041011
Myelosuppression 83.82 18.02 82 25022 40214 79679070
Dermatitis acneiform 77.91 18.02 45 25059 9948 79709336
Infusion related reaction 75.81 18.02 200 24904 230037 79489247
Thrombocytopenia 74.10 18.02 217 24887 265042 79454242
Leukopenia 72.62 18.02 131 24973 116382 79602902
Death 71.87 18.02 360 24744 566154 79153130
Stomatitis 66.10 18.02 144 24960 146613 79572671
Toxicity to various agents 64.55 18.02 26 25078 421514 79297770
Diarrhoea 64.40 18.02 485 24619 880004 78839280
Mucosal inflammation 60.42 18.02 95 25009 75485 79643799
Drug intolerance 58.94 18.02 7 25097 264112 79455172
Condition aggravated 57.83 18.02 44 25060 501080 79218204
Colony stimulating factor therapy 57.36 18.02 16 25088 508 79718776
Erythema 51.51 18.02 171 24933 223119 79496165
Joint swelling 48.96 18.02 15 25089 288631 79430653
Product dose omission issue 45.48 18.02 11 25093 247526 79471758
Hypokalaemia 44.21 18.02 122 24982 143918 79575366
Malignant neoplasm progression 42.55 18.02 116 24988 135874 79583410
Palmar-plantar erythrodysaesthesia syndrome 42.00 18.02 52 25052 33082 79686202
Alopecia areata 41.01 18.02 17 25087 1826 79717458
Enterocolitis 40.85 18.02 35 25069 14477 79704807
Fall 40.23 18.02 57 25047 487572 79231712
Anaphylactic shock 40.13 18.02 53 25051 35943 79683341
Pharyngeal dyskinesia 39.65 18.02 8 25096 58 79719226
Abdominal pain 39.42 18.02 233 24871 389336 79329948
Dyspnoea 39.34 18.02 427 24677 856598 78862686
Dehydration 38.91 18.02 168 24936 248019 79471265
Disseminated intravascular coagulation 38.77 18.02 52 25052 35790 79683494
Bone marrow failure 37.77 18.02 62 25042 51045 79668239
Chest discomfort 37.58 18.02 112 24992 137932 79581352
Hiccups 36.28 18.02 28 25076 10003 79709281
Drug interaction 35.77 18.02 47 25057 415136 79304148
Disease progression 35.44 18.02 133 24971 184229 79535055
Overdose 34.19 18.02 8 25096 184198 79535086
Pneumonitis 33.61 18.02 65 25039 60795 79658489
Injection site phlebitis 31.93 18.02 8 25096 166 79719118
Madarosis 31.26 18.02 16 25088 2786 79716498
Weight increased 31.13 18.02 25 25079 277361 79441923
Gastrointestinal perforation 31.05 18.02 21 25083 6116 79713168
Therapeutic product effect decreased 30.64 18.02 7 25097 163856 79555428
Hair texture abnormal 30.47 18.02 17 25087 3517 79715767
Intravascular haemolysis 30.40 18.02 11 25093 819 79718465
Arthralgia 29.92 18.02 87 25017 571716 79147568
Polyneuropathy 29.17 18.02 37 25067 24114 79695170
Therapeutic product effect incomplete 28.68 18.02 5 25099 141640 79577644
Musculoskeletal stiffness 28.07 18.02 10 25094 174998 79544286
Epistaxis 28.03 18.02 88 25016 111427 79607857
Tonsillar haemorrhage 27.66 18.02 8 25096 290 79718994
Hair colour changes 27.63 18.02 17 25087 4215 79715069
Oral candidiasis 27.58 18.02 40 25064 29588 79689696
Maternal exposure during pregnancy 27.26 18.02 5 25099 136533 79582751
Anaphylactic reaction 26.74 18.02 72 25032 83671 79635613
Back pain 26.40 18.02 175 24929 304005 79415279
Hypomagnesaemia 25.77 18.02 50 25054 46861 79672423
Vascular pain 25.76 18.02 10 25094 905 79718379
Cytokine release syndrome 25.69 18.02 43 25061 35955 79683329
Sinusitis 25.41 18.02 15 25089 195486 79523798
Ileus 25.30 18.02 36 25068 26175 79693109
Peritonitis 24.87 18.02 37 25067 27999 79691285
Burkholderia cepacia complex sepsis 24.21 18.02 4 25100 7 79719277
Microangiopathic haemolytic anaemia 23.92 18.02 11 25093 1516 79717768
Deep vein thrombosis 23.86 18.02 88 25016 120831 79598453
Product counterfeit 23.71 18.02 7 25097 273 79719011
Nasopharyngitis 23.68 18.02 27 25077 253854 79465430
Intestinal perforation 23.14 18.02 28 25076 17398 79701886
Exposure to unspecified agent 22.71 18.02 4 25100 12 79719272
Drug hypersensitivity 22.63 18.02 37 25067 298879 79420405
Paronychia 22.32 18.02 19 25085 7789 79711495
Intentional product use issue 22.25 18.02 10 25094 152102 79567182
Subclavian artery occlusion 22.23 18.02 6 25098 168 79719116
Product use issue 22.20 18.02 20 25084 209802 79509482
Loss of personal independence in daily activities 22.18 18.02 3 25101 102577 79616707
Product contamination microbial 21.98 18.02 9 25095 937 79718347
Device related infection 21.90 18.02 39 25065 34255 79685029
Wound 21.64 18.02 5 25099 116174 79603110
Haemolysis 21.08 18.02 23 25081 12789 79706495
Aortitis 20.96 18.02 10 25094 1497 79717787
Cholinergic syndrome 20.77 18.02 9 25095 1078 79718206
Peripheral sensory neuropathy 20.76 18.02 23 25081 13010 79706274
Infective exacerbation of chronic obstructive airways disease 20.28 18.02 12 25092 2772 79716512
Myocardial infarction 20.15 18.02 17 25087 184112 79535172
Eye movement disorder 19.90 18.02 18 25086 7993 79711291
Peripheral swelling 19.82 18.02 34 25070 269583 79449701
Hypophagia 19.81 18.02 44 25060 45323 79673961
Hepatic function abnormal 19.58 18.02 59 25045 73048 79646236
Chemotherapy 19.50 18.02 10 25094 1747 79717537
Paraesthesia 19.45 18.02 108 24996 176215 79543069
Infusion site vesicles 19.43 18.02 7 25097 515 79718769
Coma 19.42 18.02 4 25100 100645 79618639
Bacteraemia 19.28 18.02 36 25068 32788 79686496
Stridor 19.24 18.02 15 25089 5438 79713846
Aspartate aminotransferase increased 18.82 18.02 90 25014 138551 79580733
Psoriasis 18.49 18.02 3 25101 89584 79629700
Oxygen saturation decreased 18.42 18.02 85 25019 128962 79590322
Glossodynia 18.18 18.02 5 25099 103332 79615952
Throat tightness 18.16 18.02 32 25072 27875 79691409

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 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
FDA MoA N0000175817 Serotonin 3 Receptor Antagonists
FDA EPC N0000175818 Serotonin-3 Receptor Antagonist
CHEBI has role CHEBI:48279 serotonin antagonists
CHEBI has role CHEBI:50919 antiemetico

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
EQ 0.25MG BASE/5ML (EQ 0.05MG BASE/ML) **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** ALOXI HELSINN HLTHCARE N021372 July 25, 2003 DISCN INJECTABLE INTRAVENOUS 8729094 Jan. 30, 2024 PREVENTION OF CHEMOTHERAPY-INDUCED NAUSEA AND VOMITING
EQ 0.25MG BASE/5ML (EQ 0.05MG BASE/ML) **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** ALOXI HELSINN HLTHCARE N021372 July 25, 2003 DISCN INJECTABLE INTRAVENOUS 9066980 Jan. 30, 2024 PREVENTION OF CHEMOTHERAPY-INDUCED NAUSEA AND VOMITING
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 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 RX 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 RX 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 RX 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 RX 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 RX 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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
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 April 19, 2023 NEW CHEMICAL ENTITY
EQ 235MG BASE/VIAL;EQ 0.25MG BASE/VIAL AKYNZEO HELSINN HLTHCARE N210493 April 19, 2018 RX POWDER INTRAVENOUS April 19, 2023 NEW CHEMICAL ENTITY

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
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
CHEMBL1720 ChEMBL_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Palonosetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0143-9513 INJECTION 0.25 mg INTRAVENOUS NDA 27 sections
Palonosetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0409-2503 INJECTION, SOLUTION 0.08 mg INTRAVENOUS ANDA 29 sections
Palonosetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0409-2504 INJECTION, SOLUTION 0.25 mg INTRAVENOUS ANDA 29 sections
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 0781-3312 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 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 HUMAN PRESCRIPTION DRUG LABEL 1 16714-834 INJECTION, SOLUTION 0.05 mg INTRAVENOUS ANDA 26 sections
palonosetron hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 16729-365 INJECTION 0.25 mg INTRAVENOUS NDA authorized generic 27 sections
Palonosetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 23155-356 INJECTION 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 25021-788 INJECTION, SOLUTION 0.05 mg INTRAVENOUS ANDA 28 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 Hydrochloride Human Prescription Drug Label 1 50742-485 INJECTION 0.25 mg INTRAVENOUS ANDA 26 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
Aloxi HUMAN PRESCRIPTION DRUG LABEL 1 62856-797 INJECTION 0.25 mg INTRAVENOUS NDA 28 sections
Aloxi HUMAN PRESCRIPTION DRUG LABEL 1 62856-798 INJECTION 0.08 mg INTRAVENOUS NDA 28 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 68001-482 INJECTION 0.25 mg INTRAVENOUS ANDA 26 sections
Palonosetron HUMAN PRESCRIPTION DRUG LABEL 1 68001-482 INJECTION 0.25 mg INTRAVENOUS ANDA 26 sections