palonosetron 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| serotonin receptor antagonists (5-HT3) | 2046 | 135729-61-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.50 | mg | O |
| 0.25 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| 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 term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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:
| Source | Code | Description |
|---|---|---|
| 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|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.52 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| 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:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 |