palonosetron ๐Ÿถ 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 ยตM/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 366.65 18.64 491 16233 324888 50263512
Febrile neutropenia 267.04 18.64 236 16488 97431 50490969
Neutropenia 226.37 18.64 261 16463 147704 50440696
Nausea 185.45 18.64 580 16144 704818 49883582
Neutrophil count decreased 145.48 18.64 121 16603 45905 50542495
Vomiting 124.15 18.64 383 16341 460375 50128025
Flushing 122.57 18.64 130 16594 66885 50521515
Disease progression 120.05 18.64 153 16571 95713 50492687
Drug ineffective 112.88 18.64 66 16658 819267 49769133
Constipation 112.86 18.64 212 16512 185496 50402904
Decreased appetite 108.25 18.64 218 16506 200705 50387695
Off label use 88.98 18.64 350 16374 474076 50114324
Neuropathy peripheral 84.60 18.64 130 16594 96627 50491773
Mucosal inflammation 75.35 18.64 79 16645 40063 50548337
Palmar-plantar erythrodysaesthesia syndrome 67.98 18.64 55 16669 20043 50568357
Abdominal pain 60.15 18.64 193 16531 236035 50352365
Erythema 59.53 18.64 142 16582 146272 50442128
Colony stimulating factor therapy 59.53 18.64 15 16709 303 50588097
Dyspnoea 55.50 18.64 339 16385 547269 50041131
Platelet count decreased 50.22 18.64 106 16618 100620 50487780
Pyrexia 50.21 18.64 253 16471 379950 50208450
Anaemia 49.32 18.64 189 16535 252267 50336133
Condition aggravated 46.54 18.64 20 16704 297038 50291362
Tonsillar haemorrhage 43.02 18.64 11 16713 236 50588164
Drug intolerance 42.73 18.64 10 16714 219094 50369306
Back pain 39.92 18.64 161 16563 219869 50368531
Injection site phlebitis 39.36 18.64 9 16715 118 50588282
Product dose omission issue 38.72 18.64 7 16717 183831 50404569
Fatigue 38.49 18.64 379 16345 707222 49881178
Dehydration 38.23 18.64 124 16600 152325 50436075
Alopecia areata 37.99 18.64 15 16709 1353 50587047
Chest discomfort 37.72 18.64 90 16634 92632 50495768
Joint swelling 37.63 18.64 17 16707 245269 50343131
Thrombocytopenia 36.78 18.64 109 16615 127564 50460836
Maternal exposure during pregnancy 36.09 18.64 5 16719 159773 50428627
Ascites 35.33 18.64 51 16673 35810 50552590
Product contamination microbial 34.86 18.64 9 16715 201 50588199
Infusion related reaction 34.76 18.64 129 16595 169428 50418972
Treatment failure 34.38 18.64 3 16721 137634 50450766
Epistaxis 33.84 18.64 69 16655 63885 50524515
Diarrhoea 33.31 18.64 318 16406 588158 50000242
Asthenia 32.47 18.64 198 16526 318844 50269556
Fall 32.22 18.64 38 16686 334894 50253506
Dermatitis acneiform 30.10 18.64 18 16706 4039 50584361
Product counterfeit 29.67 18.64 7 16717 106 50588294
Hair colour changes 28.10 18.64 15 16709 2709 50585691
Myelosuppression 27.88 18.64 28 16696 13489 50574911
Oral candidiasis 27.71 18.64 31 16693 16884 50571516
Therapeutic product effect decreased 26.92 18.64 6 16718 136044 50452356
Hypokalaemia 26.16 18.64 76 16648 87916 50500484
Madarosis 26.14 18.64 14 16710 2546 50585854
Interstitial lung disease 25.37 18.64 55 16669 53121 50535279
Toxicity to various agents 25.18 18.64 20 16704 212479 50375921
Stomatitis 24.99 18.64 82 16642 101262 50487138
White blood cell count decreased 24.06 18.64 89 16635 116633 50471767
Hair texture abnormal 24.00 18.64 15 16709 3641 50584759
Weight increased 23.92 18.64 19 16705 201872 50386528
Stridor 23.35 18.64 14 16710 3155 50585245
Transmission of an infectious agent via product 23.07 18.64 6 16718 138 50588262
Glossodynia 23.06 18.64 5 16719 115564 50472836
Nasopharyngitis 23.06 18.64 18 16706 192909 50395491
Bone pain 22.70 18.64 49 16675 47180 50541220
Musculoskeletal chest pain 22.29 18.64 29 16695 18457 50569943
Aortitis 22.26 18.64 9 16715 863 50587537
Leukopenia 21.70 18.64 60 16664 67468 50520932
Chemotherapy 21.41 18.64 10 16714 1359 50587041
Gastrointestinal perforation 21.21 18.64 13 16711 3048 50585352
Burkholderia cepacia complex sepsis 21.05 18.64 3 16721 0 50588400
Infusion site vesicles 20.95 18.64 7 16717 391 50588009
Vascular pain 20.77 18.64 8 16716 675 50587725
Therapeutic product effect incomplete 20.33 18.64 3 16721 91512 50496888
Palmar erythema 20.15 18.64 10 16714 1553 50586847
Laryngospasm 20.13 18.64 12 16712 2676 50585724
Drug interaction 19.87 18.64 22 16702 199599 50388801
Tachycardia 19.67 18.64 75 16649 99688 50488712
Drug hypersensitivity 19.61 18.64 33 16691 250977 50337423
Exposure to unspecified agent 18.97 18.64 3 16721 3 50588397
Anaphylactic shock 18.88 18.64 28 16696 20127 50568273

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 149.80 19.98 393 11974 341691 29220469
Nausea 126.01 19.98 332 12035 288923 29273237
Febrile neutropenia 117.84 19.98 186 12181 112054 29450106
Neutrophil count decreased 117.34 19.98 116 12251 43451 29518709
Decreased appetite 102.20 19.98 202 12165 145140 29417020
Off label use 91.36 19.98 304 12063 300496 29261664
Constipation 90.45 19.98 167 12200 113993 29448167
Neutropenia 85.32 19.98 177 12190 131534 29430626
Stomatitis 70.20 19.98 82 12285 37031 29525129
Vomiting 59.34 19.98 209 12158 212051 29350109
Drug ineffective 59.01 19.98 40 12327 363130 29199030
White blood cell count decreased 58.59 19.98 116 12251 83246 29478914
Interstitial lung disease 56.78 19.98 93 12274 57625 29504535
Fatigue 50.52 19.98 263 12104 316558 29245602
Dermatitis acneiform 46.87 19.98 29 12338 5462 29556698
Diarrhoea 46.19 19.98 266 12101 332432 29229728
Platelet count decreased 45.03 19.98 120 12247 104552 29457608
Toxicity to various agents 39.16 19.98 12 12355 173649 29388511
Pyrexia 38.57 19.98 228 12139 287394 29274766
Disease progression 38.38 19.98 97 12270 81819 29480341
Hiccups 36.50 19.98 30 12337 8823 29553337
Neuropathy peripheral 36.34 19.98 87 12280 70940 29491220
Drug interaction 34.35 19.98 20 12347 197365 29364795
Leukopenia 33.08 19.98 72 12295 55131 29507029
Intravascular haemolysis 30.79 19.98 10 12357 402 29561758
Thrombocytopenia 30.30 19.98 124 12243 134699 29427461
Device related infection 30.29 19.98 35 12332 15601 29546559
Flushing 30.23 19.98 48 12319 28944 29533216
Alopecia 27.77 19.98 37 12330 19047 29543113
Microangiopathic haemolytic anaemia 27.05 19.98 11 12356 844 29561316
Anaemia 26.66 19.98 159 12208 200792 29361368
Condition aggravated 25.18 19.98 15 12352 146280 29415880
Overdose 23.19 19.98 3 12364 79816 29482344
Subclavian artery occlusion 22.33 19.98 6 12361 123 29562037
Disseminated intravascular coagulation 22.10 19.98 34 12333 19946 29542214
Cholinergic syndrome 21.59 19.98 8 12359 478 29561682
Deep vein thrombosis 20.90 19.98 62 12305 57337 29504823

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 403.86 16.49 405 21916 187252 64289159
Neutropenia 263.63 16.49 367 21954 239257 64237154
Neutrophil count decreased 256.70 16.49 213 22108 76983 64399428
Nausea 204.20 16.49 664 21657 785136 63691275
Decreased appetite 147.44 16.49 310 22011 280979 64195432
Flushing 143.97 16.49 156 22165 78492 64397919
Constipation 123.87 16.49 256 22065 229081 64247330
Vomiting 110.77 16.49 429 21892 550688 63925723
Platelet count decreased 107.18 16.49 201 22120 167510 64308901
Neuropathy peripheral 101.51 16.49 161 22160 117364 64359047
Drug ineffective 100.96 16.49 86 22235 840161 63636250
Interstitial lung disease 87.31 16.49 136 22185 97596 64378815
Pyrexia 84.39 16.49 399 21922 558245 63918166
White blood cell count decreased 82.54 16.49 174 22147 157663 64318748
Thrombocytopenia 71.38 16.49 204 22117 223597 64252814
Infusion related reaction 71.03 16.49 168 22153 164299 64312112
Stomatitis 70.74 16.49 132 22189 109473 64366938
Dermatitis acneiform 70.25 16.49 41 22280 8402 64468009
Anaemia 67.22 16.49 284 22037 378396 64098015
Leukopenia 62.93 16.49 120 22201 101122 64375289
Death 60.27 16.49 327 21994 482378 63994033
Toxicity to various agents 59.03 16.49 26 22295 363487 64112924
Mucosal inflammation 58.54 16.49 89 22232 62495 64413916
Diarrhoea 57.20 16.49 436 21885 722268 63754143
Colony stimulating factor therapy 56.14 16.49 16 22305 499 64475912
Myelosuppression 53.90 16.49 53 22268 23777 64452634
Drug intolerance 52.92 16.49 3 22318 187989 64288422
Condition aggravated 52.51 16.49 32 22289 372394 64104017
Erythema 47.91 16.49 158 22163 186912 64289499
Abdominal pain 41.18 16.49 215 22106 312160 64164251
Fall 40.42 16.49 51 22270 416775 64059636
Enterocolitis 39.53 16.49 33 22288 11985 64464426
Drug interaction 38.66 16.49 41 22280 362042 64114369
Disease progression 36.55 16.49 120 22201 141560 64334851
Product dose omission issue 36.53 16.49 11 22310 194736 64281675
Bone marrow failure 36.36 16.49 62 22259 47890 64428521
Palmar-plantar erythrodysaesthesia syndrome 35.87 16.49 47 22274 28772 64447639
Alopecia areata 35.71 16.49 15 22306 1513 64474898
Joint swelling 35.57 16.49 15 22306 215367 64261044
Anaphylactic shock 35.50 16.49 48 22273 30280 64446131
Dehydration 34.87 16.49 158 22163 216605 64259806
Hiccups 33.95 16.49 26 22295 8350 64468061
Disseminated intravascular coagulation 33.10 16.49 48 22273 32300 64444111
Dyspnoea 32.36 16.49 385 21936 718289 63758122
Overdose 31.82 16.49 8 22313 159558 64316853
Injection site phlebitis 31.69 16.49 8 22313 155 64476256
Intravascular haemolysis 30.91 16.49 11 22310 709 64475702
Oral candidiasis 30.68 16.49 39 22282 23173 64453238
Polyneuropathy 30.46 16.49 36 22285 19858 64456553
Hypokalaemia 30.32 16.49 102 22219 121801 64354610
Tonsillar haemorrhage 28.15 16.49 8 22313 247 64476164
Epistaxis 27.00 16.49 85 22236 98046 64378365
Gastrointestinal perforation 26.86 16.49 19 22302 5405 64471006
Madarosis 26.77 16.49 14 22307 2316 64474095
Chest discomfort 26.14 16.49 94 22227 116012 64360399
Hair texture abnormal 26.08 16.49 15 22306 2989 64473422
Vascular pain 25.84 16.49 10 22311 816 64475595
Anaphylactic reaction 25.23 16.49 66 22255 68598 64407813
Product counterfeit 24.36 16.49 7 22314 225 64476186
Microangiopathic haemolytic anaemia 24.12 16.49 11 22310 1351 64475060
Burkholderia cepacia complex sepsis 23.83 16.49 4 22317 7 64476404
Deep vein thrombosis 23.54 16.49 85 22236 105097 64371314
Ileus 23.38 16.49 34 22287 22932 64453479
Back pain 23.14 16.49 157 22164 250014 64226397
Hair colour changes 23.10 16.49 15 22306 3712 64472699
Therapeutic product effect incomplete 23.07 16.49 4 22317 103478 64372933
Weight increased 22.92 16.49 24 22297 213324 64263087
Exposure to unspecified agent 22.34 16.49 4 22317 12 64476399
Intestinal perforation 22.27 16.49 27 22294 15286 64461125
Cholinergic syndrome 22.16 16.49 9 22312 834 64475577
Haemolysis 22.12 16.49 23 22298 11016 64465395
Subclavian artery occlusion 21.99 16.49 6 22315 159 64476252
Product contamination microbial 21.75 16.49 9 22312 874 64475537
Paronychia 21.71 16.49 18 22303 6474 64469937
Arthralgia 21.27 16.49 80 22241 442180 64034231
Fatigue 21.20 16.49 370 21951 748360 63728051
Myocardial infarction 20.99 16.49 16 22305 165805 64310606
Therapeutic product effect decreased 20.76 16.49 7 22314 115344 64361067
Infusion site vesicles 20.72 16.49 7 22314 386 64476025
Chemotherapy 20.06 16.49 10 22311 1497 64474914
Device related infection 19.87 16.49 37 22284 30589 64445822
Stridor 19.47 16.49 15 22306 4859 64471552
Hypomagnesaemia 19.25 16.49 41 22280 37335 64439076
Hypophagia 18.77 16.49 42 22279 39545 64436866
Malignant neoplasm progression 18.66 16.49 83 22238 112788 64363623
Coma 18.23 16.49 4 22317 87611 64388800
Musculoskeletal stiffness 18.16 16.49 10 22311 123196 64353215
Peripheral sensory neuropathy 18.10 16.49 21 22300 11357 64465054
Paraesthesia 17.96 16.49 93 22228 134429 64341982
Product use issue 17.52 16.49 16 22305 151699 64324712
Drug hypersensitivity 17.43 16.49 35 22286 237780 64238631
Sinusitis 17.32 16.49 15 22306 145913 64330498
Anaemia of malignant disease 16.97 16.49 7 22314 675 64475736
Transmission of an infectious agent via product 16.78 16.49 5 22316 183 64476228
Oropharyngeal pain 16.74 16.49 68 22253 88799 64387612
Aortitis 16.74 16.49 8 22313 1093 64475318

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




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 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) 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) 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 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
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

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 0781-3415 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 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 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 hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 69097-439 INJECTION, SOLUTION 0.25 mg INTRAVENOUS ANDA 24 sections
palonosetron hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 69097-927 INJECTION 0.25 mg INTRAVENOUS NDA authorized generic 26 sections
Palonosetron hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 69543-371 INJECTION, SOLUTION 0.25 mg INTRAVENOUS ANDA 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