fosaprepitant 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| neurokinin NK1 (substance P) receptor antagonist | 4470 | 172673-20-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
a pro-drug form of aprepitant
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Hosey CM, Chan R, Benet LZ |
| Vd (Volume of distribution) | 0.07 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 18.60 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.02 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 2.20 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 100 mg/mL | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 27, 2003 | FDA |
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 |
|---|---|---|---|---|---|---|
| Febrile neutropenia | 474.00 | 16.45 | 359 | 20895 | 118090 | 63349678 |
| Flushing | 156.16 | 16.45 | 157 | 21097 | 74930 | 63392838 |
| Erythema | 145.85 | 16.45 | 232 | 21022 | 175519 | 63292249 |
| Febrile bone marrow aplasia | 131.18 | 16.45 | 59 | 21195 | 7266 | 63460502 |
| Mucosal inflammation | 118.05 | 16.45 | 109 | 21145 | 46819 | 63420949 |
| Neutropenia | 117.22 | 16.45 | 210 | 21044 | 174795 | 63292973 |
| Nausea | 110.98 | 16.45 | 570 | 20684 | 853901 | 62613867 |
| Pyrexia | 108.94 | 16.45 | 375 | 20879 | 470103 | 62997665 |
| Computerised tomogram thorax abnormal | 100.40 | 16.45 | 33 | 21221 | 1730 | 63466038 |
| Neutrophil count decreased | 99.41 | 16.45 | 108 | 21146 | 56298 | 63411470 |
| Encephalopathy | 95.76 | 16.45 | 89 | 21165 | 38531 | 63429237 |
| Drug ineffective | 82.62 | 16.45 | 140 | 21114 | 1044625 | 62423143 |
| Bone marrow failure | 77.48 | 16.45 | 70 | 21184 | 29220 | 63438548 |
| Anaphylactic shock | 75.70 | 16.45 | 63 | 21191 | 23570 | 63444198 |
| Hyponatraemia | 70.67 | 16.45 | 131 | 21123 | 111769 | 63355999 |
| Dyspnoea | 69.33 | 16.45 | 417 | 20837 | 660896 | 62806872 |
| Hepatocellular injury | 63.85 | 16.45 | 61 | 21193 | 27320 | 63440448 |
| Injection site phlebitis | 61.44 | 16.45 | 13 | 21241 | 114 | 63467654 |
| Atelectasis | 60.10 | 16.45 | 53 | 21201 | 21430 | 63446338 |
| Computerised tomogram thorax | 58.84 | 16.45 | 16 | 21238 | 433 | 63467335 |
| Feeling hot | 55.39 | 16.45 | 76 | 21178 | 50278 | 63417490 |
| Toxicity to various agents | 53.93 | 16.45 | 9 | 21245 | 247241 | 63220527 |
| Aplasia | 53.85 | 16.45 | 27 | 21227 | 4232 | 63463536 |
| Sense of oppression | 53.79 | 16.45 | 18 | 21236 | 998 | 63466770 |
| Vomiting | 51.15 | 16.45 | 341 | 20913 | 559276 | 62908492 |
| Gastrointestinal disorder | 50.85 | 16.45 | 126 | 21128 | 131113 | 63336655 |
| Fall | 50.27 | 16.45 | 35 | 21219 | 392299 | 63075469 |
| Colony stimulating factor therapy | 49.22 | 16.45 | 13 | 21241 | 314 | 63467454 |
| Stomatitis | 48.37 | 16.45 | 128 | 21126 | 138597 | 63329171 |
| Infusion site streaking | 47.47 | 16.45 | 14 | 21240 | 511 | 63467257 |
| Hypoxia | 46.83 | 16.45 | 77 | 21177 | 59715 | 63408053 |
| Chemotherapy | 46.04 | 16.45 | 18 | 21236 | 1561 | 63466207 |
| Infusion related reaction | 44.31 | 16.45 | 181 | 21073 | 245340 | 63222428 |
| Injection site vasculitis | 44.17 | 16.45 | 7 | 21247 | 7 | 63467761 |
| Palmar-plantar erythrodysaesthesia syndrome | 43.93 | 16.45 | 46 | 21208 | 22969 | 63444799 |
| Tonsillar haemorrhage | 42.28 | 16.45 | 11 | 21243 | 250 | 63467518 |
| Hypersensitivity | 36.72 | 16.45 | 194 | 21060 | 292491 | 63175277 |
| Hypokalaemia | 36.39 | 16.45 | 96 | 21158 | 103708 | 63364060 |
| Chest discomfort | 31.95 | 16.45 | 95 | 21159 | 109874 | 63357894 |
| Medication error | 31.46 | 16.45 | 60 | 21194 | 52224 | 63415544 |
| Muscle injury | 31.05 | 16.45 | 68 | 21186 | 65277 | 63402491 |
| Interstitial lung disease | 30.07 | 16.45 | 65 | 21189 | 61843 | 63405925 |
| Platelet count decreased | 28.84 | 16.45 | 95 | 21159 | 116027 | 63351741 |
| Folliculitis | 28.79 | 16.45 | 69 | 21185 | 70248 | 63397520 |
| Thrombocytopenia | 28.48 | 16.45 | 113 | 21141 | 151044 | 63316724 |
| Abdominal pain | 28.01 | 16.45 | 181 | 21073 | 293275 | 63174493 |
| Diarrhoea | 27.83 | 16.45 | 363 | 20891 | 715003 | 62752765 |
| Leukopenia | 27.61 | 16.45 | 72 | 21182 | 77218 | 63390550 |
| Pain | 26.50 | 16.45 | 143 | 21111 | 740485 | 62727283 |
| Neutropenic colitis | 26.13 | 16.45 | 15 | 21239 | 3080 | 63464688 |
| Dental fistula | 24.86 | 16.45 | 9 | 21245 | 631 | 63467137 |
| Anorectal disorder | 24.83 | 16.45 | 12 | 21242 | 1737 | 63466031 |
| Colitis | 24.77 | 16.45 | 52 | 21202 | 48476 | 63419292 |
| Decreased appetite | 24.66 | 16.45 | 156 | 21098 | 250896 | 63216872 |
| Vascular device infection | 24.47 | 16.45 | 20 | 21234 | 7292 | 63460476 |
| White blood cell count decreased | 23.06 | 16.45 | 100 | 21154 | 139004 | 63328764 |
| Laryngeal discomfort | 22.26 | 16.45 | 7 | 21247 | 318 | 63467450 |
| Cerebellar syndrome | 21.76 | 16.45 | 14 | 21240 | 3525 | 63464243 |
| Irritable bowel syndrome | 20.97 | 16.45 | 68 | 21186 | 82344 | 63385424 |
| Injection site induration | 20.46 | 16.45 | 20 | 21234 | 9206 | 63458562 |
| Pain in extremity | 19.64 | 16.45 | 52 | 21202 | 331434 | 63136334 |
| Craniocerebral injury | 19.41 | 16.45 | 12 | 21242 | 2820 | 63464948 |
| Therapeutic product effect incomplete | 19.06 | 16.45 | 9 | 21245 | 125047 | 63342721 |
| Bronchitis | 19.02 | 16.45 | 9 | 21245 | 124926 | 63342842 |
| Antinuclear antibody | 18.96 | 16.45 | 7 | 21247 | 519 | 63467249 |
| Septic shock | 18.81 | 16.45 | 57 | 21197 | 66572 | 63401196 |
| Thrombocytopenic purpura | 18.12 | 16.45 | 9 | 21245 | 1382 | 63466386 |
| Throat tightness | 18.08 | 16.45 | 31 | 21223 | 24856 | 63442912 |
| Inappropriate antidiuretic hormone secretion | 18 | 16.45 | 24 | 21230 | 15438 | 63452330 |
| Sleep disorder due to general medical condition, insomnia type | 17.99 | 16.45 | 48 | 21206 | 52169 | 63415599 |
| Duodenal ulcer perforation | 17.89 | 16.45 | 67 | 21187 | 87142 | 63380626 |
| Myocardial infarction | 17.15 | 16.45 | 6 | 21248 | 99887 | 63367881 |
| Intercepted product administration error | 17.10 | 16.45 | 6 | 21248 | 384 | 63467384 |
| Product dose omission issue | 16.92 | 16.45 | 33 | 21221 | 234280 | 63233488 |
| Fluid intake reduced | 16.67 | 16.45 | 12 | 21242 | 3629 | 63464139 |
| Balance disorder | 16.46 | 16.45 | 4 | 21250 | 84418 | 63383350 |
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 |
|---|---|---|---|---|---|---|
| Febrile neutropenia | 194.63 | 20 | 231 | 11188 | 136618 | 34808894 |
| Hiccups | 117.58 | 20 | 60 | 11359 | 10022 | 34935490 |
| Erythema | 111.54 | 20 | 141 | 11278 | 88639 | 34856873 |
| Neutropenia | 96.93 | 20 | 179 | 11240 | 156599 | 34788913 |
| Neutrophil count decreased | 83.68 | 20 | 93 | 11326 | 51011 | 34894501 |
| Nausea | 77.61 | 20 | 265 | 11154 | 339643 | 34605869 |
| Anaphylactic reaction | 73.16 | 20 | 70 | 11349 | 32231 | 34913281 |
| Drug ineffective | 65.51 | 20 | 34 | 11385 | 456717 | 34488795 |
| Hypersensitivity | 64.29 | 20 | 89 | 11330 | 60946 | 34884566 |
| Thrombocytopenia | 61.02 | 20 | 148 | 11271 | 156099 | 34789413 |
| Encephalopathy | 57.31 | 20 | 64 | 11355 | 35255 | 34910257 |
| Pyrexia | 54.72 | 20 | 234 | 11185 | 332779 | 34612733 |
| Vomiting | 51.95 | 20 | 188 | 11231 | 247433 | 34698079 |
| Stomatitis | 50.88 | 20 | 66 | 11353 | 42448 | 34903064 |
| Decreased appetite | 48.09 | 20 | 141 | 11278 | 166251 | 34779261 |
| Febrile bone marrow aplasia | 47.59 | 20 | 31 | 11388 | 8178 | 34937334 |
| White blood cell count decreased | 46.77 | 20 | 99 | 11320 | 95346 | 34850166 |
| Hepatocellular injury | 46.28 | 20 | 46 | 11373 | 22165 | 34923347 |
| Testicular germ cell cancer metastatic | 45.33 | 20 | 9 | 11410 | 57 | 34945455 |
| Flushing | 44.64 | 20 | 54 | 11365 | 32366 | 34913146 |
| Platelet count decreased | 41.03 | 20 | 108 | 11311 | 119609 | 34825903 |
| Toxicity to various agents | 40.78 | 20 | 8 | 11411 | 200354 | 34745158 |
| Bone marrow failure | 40.72 | 20 | 49 | 11370 | 29204 | 34916308 |
| Diarrhoea | 39.34 | 20 | 239 | 11180 | 389673 | 34555839 |
| Fixed eruption | 38.34 | 20 | 16 | 11403 | 1684 | 34943828 |
| Interstitial lung disease | 37.05 | 20 | 72 | 11347 | 65210 | 34880302 |
| Aplasia | 35.95 | 20 | 21 | 11398 | 4567 | 34940945 |
| Seminoma | 33.88 | 20 | 9 | 11410 | 228 | 34945284 |
| Acute kidney injury | 31.35 | 20 | 188 | 11231 | 304800 | 34640712 |
| Anaphylactic shock | 31.34 | 20 | 32 | 11387 | 15909 | 34929603 |
| Sense of oppression | 30.39 | 20 | 10 | 11409 | 539 | 34944973 |
| Septic shock | 30.07 | 20 | 70 | 11349 | 71764 | 34873748 |
| Mucosal inflammation | 28.81 | 20 | 48 | 11371 | 38574 | 34906938 |
| Constipation | 28.61 | 20 | 104 | 11315 | 136878 | 34808634 |
| Chest discomfort | 28.35 | 20 | 58 | 11361 | 54472 | 34891040 |
| Leukopenia | 28.24 | 20 | 63 | 11356 | 62793 | 34882719 |
| Paraesthesia | 27.37 | 20 | 63 | 11356 | 64109 | 34881403 |
| Rash maculo-papular | 26.27 | 20 | 39 | 11380 | 28412 | 34917100 |
| Platelet count increased | 26.14 | 20 | 23 | 11396 | 9503 | 34936009 |
| Enteritis | 25.07 | 20 | 21 | 11398 | 8121 | 34937391 |
| Jaundice | 24.28 | 20 | 40 | 11379 | 31842 | 34913670 |
| Infusion related reaction | 23.63 | 20 | 53 | 11366 | 53004 | 34892508 |
| Product dose omission issue | 21.91 | 20 | 6 | 11413 | 119705 | 34825807 |
| Necrotising ulcerative gingivostomatitis | 21.62 | 20 | 5 | 11414 | 70 | 34945442 |
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 | 592.14 | 15.99 | 563 | 28672 | 230436 | 79484717 |
| Erythema | 244.55 | 15.99 | 352 | 28883 | 222938 | 79492215 |
| Neutropenia | 178.73 | 15.99 | 352 | 28883 | 287358 | 79427795 |
| Flushing | 173.80 | 15.99 | 187 | 29048 | 88081 | 79627072 |
| Neutrophil count decreased | 167.60 | 15.99 | 189 | 29046 | 93770 | 79621383 |
| Febrile bone marrow aplasia | 156.06 | 15.99 | 82 | 29153 | 12938 | 79702215 |
| Nausea | 143.51 | 15.99 | 710 | 28525 | 956486 | 78758667 |
| Pyrexia | 141.50 | 15.99 | 556 | 28679 | 678153 | 79037000 |
| Encephalopathy | 133.01 | 15.99 | 143 | 29092 | 67254 | 79647899 |
| Drug ineffective | 109.66 | 15.99 | 142 | 29093 | 1080771 | 78634382 |
| Toxicity to various agents | 107.26 | 15.99 | 14 | 29221 | 421526 | 79293627 |
| Hiccups | 105.71 | 15.99 | 58 | 29177 | 9973 | 79705180 |
| Mucosal inflammation | 101.96 | 15.99 | 132 | 29103 | 75448 | 79639705 |
| Bone marrow failure | 101.81 | 15.99 | 109 | 29126 | 50998 | 79664155 |
| Hypersensitivity | 99.30 | 15.99 | 264 | 28971 | 261975 | 79453178 |
| Hepatocellular injury | 97.45 | 15.99 | 103 | 29132 | 47490 | 79667663 |
| Computerised tomogram thorax abnormal | 90.89 | 15.99 | 34 | 29201 | 2385 | 79712768 |
| Anaphylactic shock | 90.37 | 15.99 | 87 | 29148 | 35909 | 79679244 |
| Aplasia | 87.36 | 15.99 | 47 | 29188 | 7773 | 79707380 |
| Stomatitis | 85.46 | 15.99 | 175 | 29060 | 146582 | 79568571 |
| Sense of oppression | 81.43 | 15.99 | 28 | 29207 | 1538 | 79713615 |
| Thrombocytopenia | 69.92 | 15.99 | 235 | 29000 | 265024 | 79450129 |
| Infusion related reaction | 69.79 | 15.99 | 214 | 29021 | 230023 | 79485130 |
| Vomiting | 67.02 | 15.99 | 445 | 28790 | 665383 | 79049770 |
| Platelet count decreased | 66.68 | 15.99 | 189 | 29046 | 194475 | 79520678 |
| Anaphylactic reaction | 66.38 | 15.99 | 114 | 29121 | 83629 | 79631524 |
| Fall | 62.83 | 15.99 | 52 | 29183 | 487577 | 79227576 |
| Hyponatraemia | 61.22 | 15.99 | 173 | 29062 | 177675 | 79537478 |
| Dyspnoea | 60.02 | 15.99 | 526 | 28709 | 856499 | 78858654 |
| Decreased appetite | 59.62 | 15.99 | 266 | 28969 | 342152 | 79373001 |
| Interstitial lung disease | 59.40 | 15.99 | 129 | 29106 | 112471 | 79602682 |
| White blood cell count decreased | 58.90 | 15.99 | 177 | 29058 | 188111 | 79527042 |
| Palmar-plantar erythrodysaesthesia syndrome | 57.91 | 15.99 | 66 | 29169 | 33068 | 79682085 |
| Computerised tomogram thorax | 57.36 | 15.99 | 16 | 29219 | 434 | 79714719 |
| Colony stimulating factor therapy | 54.95 | 15.99 | 16 | 29219 | 508 | 79714645 |
| Leukopenia | 53.13 | 15.99 | 126 | 29109 | 116387 | 79598766 |
| Feeling hot | 52.25 | 15.99 | 85 | 29150 | 59649 | 79655504 |
| Chest discomfort | 51.17 | 15.99 | 138 | 29097 | 137906 | 79577247 |
| Diarrhoea | 49.97 | 15.99 | 517 | 28718 | 879972 | 78835181 |
| Infusion site streaking | 46.13 | 15.99 | 14 | 29221 | 514 | 79714639 |
| Gastrointestinal disorder | 46.13 | 15.99 | 123 | 29112 | 122082 | 79593071 |
| Atelectasis | 46.09 | 15.99 | 58 | 29177 | 32199 | 79682954 |
| Chemotherapy | 45.95 | 15.99 | 19 | 29216 | 1738 | 79713415 |
| Testicular germ cell cancer metastatic | 44.43 | 15.99 | 9 | 29226 | 56 | 79715097 |
| Hypokalaemia | 40.93 | 15.99 | 131 | 29104 | 143909 | 79571244 |
| Injection site vasculitis | 40.70 | 15.99 | 7 | 29228 | 14 | 79715139 |
| Product dose omission issue | 39.10 | 15.99 | 21 | 29214 | 247516 | 79467637 |
| Neutropenic colitis | 36.66 | 15.99 | 24 | 29211 | 5683 | 79709470 |
| Enteritis | 36.13 | 15.99 | 35 | 29200 | 14548 | 79700605 |
| Septic shock | 36.09 | 15.99 | 113 | 29122 | 122688 | 79592465 |
| Hypoxia | 36.05 | 15.99 | 101 | 29134 | 103142 | 79612011 |
| Paraesthesia | 34.49 | 15.99 | 142 | 29093 | 176181 | 79538972 |
| Seminoma | 33.89 | 15.99 | 9 | 29226 | 202 | 79714951 |
| Therapeutic product effect incomplete | 33.02 | 15.99 | 6 | 29229 | 141639 | 79573514 |
| Rash maculo-papular | 32.75 | 15.99 | 67 | 29168 | 56011 | 79659142 |
| Overdose | 31.55 | 15.99 | 14 | 29221 | 184192 | 79530961 |
| Injection site phlebitis | 30.72 | 15.99 | 8 | 29227 | 166 | 79714987 |
| Folliculitis | 29.82 | 15.99 | 64 | 29171 | 55316 | 79659837 |
| Muscle injury | 29.52 | 15.99 | 59 | 29176 | 48502 | 79666651 |
| Condition aggravated | 28.93 | 15.99 | 91 | 29144 | 501033 | 79214120 |
| Arthritis | 28.72 | 15.99 | 4 | 29231 | 114876 | 79600277 |
| Neuropathy peripheral | 28.58 | 15.99 | 115 | 29120 | 141190 | 79573963 |
| Fixed eruption | 28.17 | 15.99 | 16 | 29219 | 2938 | 79712215 |
| Constipation | 27.02 | 15.99 | 187 | 29048 | 282863 | 79432290 |
| Tonsillar haemorrhage | 26.46 | 15.99 | 8 | 29227 | 290 | 79714863 |
| Pain | 26.32 | 15.99 | 151 | 29084 | 703651 | 79011502 |
| Myocardial infarction | 25.75 | 15.99 | 18 | 29217 | 184111 | 79531042 |
| Cardiac failure congestive | 25.71 | 15.99 | 10 | 29225 | 142392 | 79572761 |
| Dental fistula | 25.68 | 15.99 | 9 | 29226 | 523 | 79714630 |
| Colitis | 24.88 | 15.99 | 71 | 29164 | 73236 | 79641917 |
| Pain in extremity | 24.11 | 15.99 | 62 | 29173 | 364476 | 79350677 |
| Inappropriate antidiuretic hormone secretion | 23.76 | 15.99 | 38 | 29197 | 26275 | 79688878 |
| Hyperthermia | 23.52 | 15.99 | 31 | 29204 | 18006 | 79697147 |
| Balance disorder | 23.44 | 15.99 | 4 | 29231 | 98853 | 79616300 |
| Anorectal disorder | 23.44 | 15.99 | 13 | 29222 | 2280 | 79712873 |
| Cholestasis | 23.35 | 15.99 | 56 | 29179 | 52053 | 79663100 |
| Abdominal pain | 23.03 | 15.99 | 231 | 29004 | 389338 | 79325815 |
| Loss of personal independence in daily activities | 22.54 | 15.99 | 5 | 29230 | 102575 | 79612578 |
| Chills | 22.41 | 15.99 | 117 | 29118 | 160117 | 79555036 |
| Toxic encephalopathy | 22.07 | 15.99 | 24 | 29211 | 11416 | 79703737 |
| Asthma | 22.00 | 15.99 | 11 | 29224 | 135084 | 79580069 |
| Transposition of the great vessels | 21.39 | 15.99 | 5 | 29230 | 65 | 79715088 |
| Dermatitis acneiform | 21.11 | 15.99 | 22 | 29213 | 9971 | 79705182 |
| Irritable bowel syndrome | 20.85 | 15.99 | 60 | 29175 | 62181 | 79652972 |
| Pancreatitis acute | 20.84 | 15.99 | 52 | 29183 | 49552 | 79665601 |
| Keratitis | 20.30 | 15.99 | 15 | 29220 | 4307 | 79710846 |
| Depression | 20.29 | 15.99 | 30 | 29205 | 216760 | 79498393 |
| Oxygen saturation decreased | 20.00 | 15.99 | 97 | 29138 | 128950 | 79586203 |
| Duodenal ulcer perforation | 19.51 | 15.99 | 61 | 29174 | 66150 | 79649003 |
| Antinuclear antibody | 19.15 | 15.99 | 7 | 29228 | 460 | 79714693 |
| Ileus | 18.58 | 15.99 | 34 | 29201 | 26177 | 79688976 |
| Hypomagnesaemia | 18.48 | 15.99 | 48 | 29187 | 46863 | 79668290 |
| Injection site induration | 17.90 | 15.99 | 20 | 29215 | 9799 | 79705354 |
| Rash | 17.71 | 15.99 | 304 | 28931 | 578054 | 79137099 |
| Joint swelling | 17.65 | 15.99 | 51 | 29184 | 288595 | 79426558 |
| SARS-CoV-2 test negative | 17.47 | 15.99 | 9 | 29226 | 1362 | 79713791 |
| Laryngeal discomfort | 17.44 | 15.99 | 7 | 29228 | 593 | 79714560 |
| Arthralgia | 17.15 | 15.99 | 131 | 29104 | 571672 | 79143481 |
| Seizure | 16.98 | 15.99 | 123 | 29112 | 188711 | 79526442 |
| Headache | 16.81 | 15.99 | 156 | 29079 | 653616 | 79061537 |
| Suicidal ideation | 16.22 | 15.99 | 4 | 29231 | 76336 | 79638817 |
| Cognitive disorder | 16.21 | 15.99 | 3 | 29232 | 69923 | 79645230 |
| Coombs positive haemolytic anaemia | 16.10 | 15.99 | 8 | 29227 | 1122 | 79714031 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| FDA MoA | N0000010262 | Neurokinin 1 Antagonists |
| MeSH PA | D000932 | Antiemetics |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D005765 | Gastrointestinal Agents |
| MeSH PA | D064729 | Neurokinin-1 Receptor Antagonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| FDA EPC | N0000175786 | Substance P/Neurokinin-1 Receptor Antagonist |
| CHEBI has role | CHEBI:50266 | Prodrugs |
| CHEBI has role | CHEBI:50919 | antiemetico |
| CHEBI has role | CHEBI:55350 | neurokinin-1 receptor antagonists |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Chemotherapy-induced nausea and vomiting | indication | 236084000 | |
| Hepatic failure | contraindication | 59927004 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 0.87 | acidic |
| pKa2 | 6.2 | acidic |
| pKa3 | 8.25 | acidic |
| pKa4 | 10.36 | acidic |
| pKa5 | 3.99 | Basic |
| pKa6 | 1.47 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 115MG BASE/VIAL **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** | EMEND | MERCK AND CO INC | N022023 | Jan. 25, 2008 | DISCN | POWDER | INTRAVENOUS | May 2, 2025 | ADDITION OF A 3-DAY FOSAPREPITANT FOR INJECTION INTRAVENOUS DOSING REGIMEN IN PEDIATRIC PATIENTS FOR THE CURRENTLY APPROVED PREVENTION OF CHEMOTHERAPY-INDUCED NAUSEA AND VOMITING |
| EQ 150MG BASE/VIAL | EMEND | MERCK AND CO INC | N022023 | Nov. 12, 2010 | RX | POWDER | INTRAVENOUS | May 2, 2025 | ADDITION OF A 3-DAY FOSAPREPITANT FOR INJECTION INTRAVENOUS DOSING REGIMEN IN PEDIATRIC PATIENTS FOR THE CURRENTLY APPROVED PREVENTION OF CHEMOTHERAPY-INDUCED NAUSEA AND VOMITING |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Substance-P receptor | GPCR | ANTAGONIST | IC50 | 8.92 | IUPHAR | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D06597 | KEGG_DRUG |
| 4027247 | VUID |
| N0000176136 | NUI |
| 265121-04-8 | SECONDARY_CAS_RN |
| 4027246 | VANDF |
| 4027247 | VANDF |
| CHEBI:64321 | CHEBI |
| CHEMBL1199324 | ChEMBL_ID |
| CHEMBL1201782 | ChEMBL_ID |
| C579707 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7623 | IUPHAR_LIGAND_ID |
| 8699 | INN_ID |
| DB06717 | DRUGBANK_ID |
| 6L8OF9XRDC | UNII |
| 1731071 | RXNORM |
| 25045 | MMSL |
| 322336 | MMSL |
| d07080 | MMSL |
| 012534 | NDDF |
| 012535 | NDDF |
| 429822007 | SNOMEDCT_US |
| 429825009 | SNOMEDCT_US |
| 434337009 | SNOMEDCT_US |
| C2349941 | UMLSCUI |
| 135413538 | PUBCHEM_CID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| EMEND | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-3061 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | NDA | 29 sections |
| EMEND | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-3061 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | NDA | 29 sections |
| EMEND | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-3061 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | NDA | 29 sections |
| EMEND | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-3061 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | NDA | 29 sections |
| EMEND | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-3884 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 115 mg | INTRAVENOUS | NDA | 29 sections |
| EMEND | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-3941 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | NDA | 29 sections |
| FOSAPREPITANT DIMEGLUMINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9384 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | ANDA | 28 sections |
| FOSAPREPITANT DIMEGLUMINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9384 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | ANDA | 28 sections |
| FOSAPREPITANT DIMEGLUMINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9428 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | ANDA | 28 sections |
| FOSAPREPITANT DIMEGLUMINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9428 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | ANDA | 28 sections |
| Fosaprepitant | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0338-0008 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | ANDA | 29 sections |
| Fosaprepitant | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0338-0008 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | ANDA | 29 sections |
| Fosaprepitant | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-4385 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | NDA | 27 sections |
| Fosaprepitant | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-4385 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | NDA | 27 sections |
| Fosaprepitant | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-4385 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | NDA | 27 sections |
| fosaprepitant dimeglumine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-3484 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | ANDA | 27 sections |
| Fosaprepitant | Human Prescription Drug Label | 1 | 0781-3497 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | ANDA | 27 sections |
| Fosaprepitant | Human Prescription Drug Label | 1 | 0781-3497 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | ANDA | 27 sections |
| Fosaprepitant | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-120 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | ANDA | 27 sections |
| Fosaprepitant | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-248 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | ANDA | 28 sections |
| Fosaprepitant | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-248 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | ANDA | 28 sections |
| Fosaprepitant | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-248 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | ANDA | 28 sections |
| Fosaprepitant | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-929 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | ANDA | 27 sections |
| Fosaprepitant | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-929 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | ANDA | 27 sections |
| Fosaprepitant | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16729-240 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | ANDA | 27 sections |
| Fosaprepitant | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16729-240 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | ANDA | 27 sections |
| Fosaprepitant | HUMAN PRESCRIPTION DRUG LABEL | 1 | 31722-165 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | ANDA | 27 sections |
| Fosaprepitant | HUMAN PRESCRIPTION DRUG LABEL | 1 | 31722-165 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | ANDA | 27 sections |
| Fosaprepitant | HUMAN PRESCRIPTION DRUG LABEL | 1 | 31722-165 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | ANDA | 27 sections |
| Fosaprepitant | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43598-859 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 150 mg | INTRAVENOUS | ANDA | 28 sections |