aprepitant ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
neurokinin NK1 (substance P) receptor antagonist 230 170729-80-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • emend
  • aprepitant
  • L-754030
Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. Aprepitant has little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting (CINV). Aprepitant has been shown in animal models to inhibit emesis induced by cytotoxic chemotherapeutic agents, such as cisplatin, via central actions.
  • Molecular weight: 534.44
  • Formula: C23H21F7N4O3
  • CLOGP: 4.40
  • LIPINSKI: 1
  • HAC: 7
  • HDO: 2
  • TPSA: 75.19
  • ALOGS: -4.44
  • ROTB: 8

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
165 mg O
150 mg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 3.34 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 62.50 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.94 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.05 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 13 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
March 27, 2003 FDA MERCK

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
Febrile neutropenia 476.88 16.35 371 21712 97296 50485745
Nausea 194.94 16.35 710 21373 704688 49878353
Mucosal inflammation 192.19 16.35 151 21932 39991 50543050
Neutropenia 177.51 16.35 267 21816 147698 50435343
Erythema 158.50 16.35 252 21831 146162 50436879
Encephalopathy 132.32 16.35 113 21970 33598 50549443
Drug ineffective 120.48 16.35 109 21974 819224 49763817
Flushing 107.19 16.35 139 21944 66876 50516165
Atelectasis 105.70 16.35 77 22006 18193 50564848
Pyrexia 104.40 16.35 383 21700 379820 50203221
Febrile bone marrow aplasia 100.66 16.35 51 22032 6260 50576781
Computerised tomogram thorax abnormal 99.68 16.35 33 22050 1350 50581691
Aplasia 82.57 16.35 38 22045 3775 50579266
Neutrophil count decreased 79.15 16.35 99 21984 45927 50537114
Hypoxia 75.49 16.35 102 21981 51021 50532020
Bone marrow failure 68.82 16.35 72 22011 27552 50555489
Hyponatraemia 68.48 16.35 138 21945 96001 50487040
Gastrointestinal disorder 65.39 16.35 134 21949 94322 50488719
Decreased appetite 63.21 16.35 212 21871 200711 50382330
Dyspnoea 61.82 16.35 429 21654 547179 50035862
Fall 61.41 16.35 35 22048 334897 50248144
Hepatocellular injury 59.98 16.35 65 22018 25882 50557159
Injection site phlebitis 58.01 16.35 13 22070 114 50582927
Feeling hot 57.54 16.35 78 22005 39124 50543917
Palmar-plantar erythrodysaesthesia syndrome 54.80 16.35 55 22028 20043 50562998
Vascular pain 52.05 16.35 17 22066 666 50582375
Vomiting 51.34 16.35 360 21723 460398 50122643
Respiratory syncytial virus infection 50.27 16.35 30 22053 5072 50577969
Anaphylactic shock 49.24 16.35 52 22031 20103 50562938
Alveolitis 47.92 16.35 23 22060 2511 50580530
Constipation 47.34 16.35 183 21900 185525 50397516
Neuropathy peripheral 46.66 16.35 119 21964 96638 50486403
Sense of oppression 46.64 16.35 17 22066 928 50582113
Oral pain 46.50 16.35 56 22027 24977 50558064
Infusion site streaking 46.12 16.35 14 22069 430 50582611
Injection site vasculitis 42.31 16.35 7 22076 7 50583034
Computerised tomogram thorax 40.03 16.35 10 22073 145 50582896
Tonsillar haemorrhage 39.99 16.35 11 22072 236 50582805
Inappropriate antidiuretic hormone secretion 39.62 16.35 38 22045 13105 50569936
Stomatitis 39.24 16.35 115 21968 101229 50481812
Diarrhoea 39.16 16.35 410 21673 588066 49994975
Depression 35.30 16.35 14 22069 165409 50417632
Chemotherapy 33.95 16.35 15 22068 1354 50581687
Rheumatoid arthritis 31.91 16.35 25 22058 202525 50380516
Hypersensitivity 31.87 16.35 181 21902 214980 50368061
Gait disturbance 31.51 16.35 13 22070 149992 50433049
Cerebellar syndrome 31.40 16.35 19 22064 3292 50579749
Abdominal pain 31.31 16.35 193 21890 236035 50347006
Interstitial lung disease 30.54 16.35 70 22013 53106 50529935
Hiccups 30.52 16.35 15 22068 1724 50581317
Toxicity to various agents 30.11 16.35 29 22054 212470 50370571
Chest discomfort 29.23 16.35 98 21985 92624 50490417
Intestinal strangulation 28.95 16.35 7 22076 88 50582953
Joint swelling 28.77 16.35 39 22044 245247 50337794
Asthma 28.32 16.35 3 22080 89334 50493707
Thrombocytopenia 25.61 16.35 117 21966 127556 50455485
Leukopenia 24.58 16.35 75 22008 67453 50515588
Colony stimulating factor therapy 24.58 16.35 8 22075 310 50582731
Hypokalaemia 24.27 16.35 89 21994 87903 50495138
Intercepted product administration error 24.02 16.35 6 22077 87 50582954
Infusion related reaction 24.01 16.35 141 21942 169416 50413625
Hypomagnesaemia 23.80 16.35 39 22044 23117 50559924
Anorectal disorder 23.78 16.35 12 22071 1460 50581581
Bronchitis 23.59 16.35 8 22075 104151 50478890
Dental fistula 22.97 16.35 9 22074 600 50582441
Musculoskeletal stiffness 22.68 16.35 14 22069 128467 50454574
Gastrointestinal scarring 22.64 16.35 7 22076 229 50582812
Thrombocytopenic purpura 22.63 16.35 11 22072 1235 50581806
Pneumonia 22.52 16.35 87 21996 378314 50204727
Anaphylactic reaction 22.51 16.35 63 22020 53992 50529049
Mobility decreased 22.25 16.35 4 22079 79944 50503097
Condition aggravated 22.01 16.35 62 22021 296996 50286045
Oropharyngeal discomfort 21.72 16.35 16 22067 3842 50579199
Exposure during pregnancy 21.62 16.35 13 22070 121002 50462039
Laryngeal discomfort 21.36 16.35 7 22076 277 50582764
Sputum abnormal 21.32 16.35 8 22075 474 50582567
Pain 21.15 16.35 157 21926 578746 50004295
Antinuclear antibody 20.94 16.35 8 22075 498 50582543
Balance disorder 20.83 16.35 3 22080 70587 50512454
Nail infection 20.43 16.35 12 22071 1969 50581072
Phlebitis 20.06 16.35 18 22065 5702 50577339
Dysgeusia 19.93 16.35 49 22034 38867 50544174
Myocardial infarction 19.88 16.35 7 22076 89020 50494021
Periorbital cellulitis 19.87 16.35 8 22075 573 50582468
Product dose omission issue 19.80 16.35 31 22052 183807 50399234
Tumour pain 19.79 16.35 10 22073 1220 50581821
Chills 19.67 16.35 89 21994 96598 50486443
Hypermagnesaemia 19.64 16.35 9 22074 885 50582156
Body temperature abnormal 19.48 16.35 10 22073 1260 50581781
Infusion site vesicles 19.05 16.35 7 22076 391 50582650
Hallucination, tactile 18.80 16.35 6 22077 218 50582823
Influenza 18.41 16.35 8 22075 89530 50493511
Administration site oedema 18.29 16.35 4 22079 31 50583010
Cough 17.81 16.35 172 21911 241092 50341949
Injection site induration 17.61 16.35 20 22063 8377 50574664
Folliculitis 17.61 16.35 47 22036 39178 50543863
Onychalgia 17.45 16.35 8 22075 787 50582254
Drug hypersensitivity 17.41 16.35 54 22029 250956 50332085
Abdominal operation 17.27 16.35 7 22076 510 50582531
Muscle injury 17.20 16.35 45 22038 37066 50545975
Paraesthesia 17.01 16.35 100 21983 120143 50462898
Cardiotoxicity 16.93 16.35 18 22065 7009 50576032
Aortitis 16.75 16.35 8 22075 864 50582177
Toxic encephalopathy 16.72 16.35 16 22067 5499 50577542
Subacute cutaneous lupus erythematosus 16.72 16.35 11 22072 2204 50580837
Cardiac failure congestive 16.63 16.35 8 22075 84374 50498667
Loss of personal independence in daily activities 16.53 16.35 5 22078 70045 50512996

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
Febrile neutropenia 220.64 19.29 254 12288 111986 29449999
Hiccups 107.40 19.29 59 12483 8794 29553191
Neutropenia 102.92 19.29 193 12349 131518 29430467
Hypersensitivity 99.02 19.29 117 12425 52786 29509199
Erythema 93.01 19.29 136 12406 75470 29486515
Neutrophil count decreased 79.26 19.29 95 12447 43472 29518513
Drug ineffective 78.92 19.29 28 12514 363142 29198843
Nausea 77.29 19.29 283 12259 288972 29273013
Thrombocytopenia 65.39 19.29 163 12379 134660 29427325
Stomatitis 59.55 19.29 76 12466 37037 29524948
Vomiting 56.79 19.29 208 12334 212052 29349933
Decreased appetite 54.65 19.29 160 12382 145182 29416803
Fixed eruption 50.27 19.29 19 12523 1183 29560802
Intestinal ischaemia 48.40 19.29 32 12510 6660 29555325
Hepatocellular injury 46.49 19.29 51 12491 21192 29540793
Encephalopathy 44.26 19.29 60 12482 30983 29531002
Toxicity to various agents 43.84 19.29 10 12532 173651 29388334
Aplasia 43.61 19.29 25 12517 4038 29557947
Diarrhoea 43.11 19.29 264 12278 332434 29229551
Testicular germ cell cancer metastatic 42.99 19.29 9 12533 57 29561928
Oesophagitis 41.74 19.29 37 12505 11886 29550099
Mouth ulceration 40.02 19.29 34 12508 10321 29551664
Anaphylactic reaction 38.86 19.29 53 12489 27520 29534465
White blood cell count decreased 38.46 19.29 99 12443 83263 29478722
Stoma site pain 36.21 19.29 12 12530 507 29561478
Bone marrow failure 34.58 19.29 50 12492 27399 29534586
Platelet count decreased 34.39 19.29 110 12432 104562 29457423
Toxic encephalopathy 33.22 19.29 22 12520 4590 29557395
Sense of oppression 32.85 19.29 11 12531 480 29561505
Oral pain 32.81 19.29 29 12513 9278 29552707
Flushing 32.49 19.29 50 12492 28942 29533043
Febrile bone marrow aplasia 32.29 19.29 26 12516 7325 29554660
Seminoma 32.02 19.29 9 12533 216 29561769
Change of bowel habit 32.00 19.29 13 12529 981 29561004
Mucosal inflammation 31.97 19.29 52 12490 31543 29530442
Emotional disorder 31.88 19.29 22 12520 4909 29557076
Interstitial lung disease 31.34 19.29 73 12469 57645 29504340
Anaphylactic shock 30.89 19.29 33 12509 13303 29548682
Leukopenia 30.17 19.29 70 12472 55133 29506852
Enteritis 29.79 19.29 24 12518 6767 29555218
Peritonitis 29.71 19.29 34 12508 14790 29547195
Neuropathy peripheral 29.35 19.29 81 12461 70946 29491039
Pyrexia 28.05 19.29 213 12329 287409 29274576
Alopecia 27.36 19.29 37 12505 19047 29542938
Paraesthesia 25.90 19.29 65 12477 53780 29508205
Regurgitation 25.46 19.29 12 12530 1295 29560690
Rash maculo-papular 24.60 19.29 40 12502 24249 29537736
Hypokalaemia 24.56 19.29 61 12481 50142 29511843
Large intestine perforation 24.11 19.29 22 12520 7334 29554651
Dehydration 23.77 19.29 104 12438 114644 29447341
Chemotherapeutic drug level increased 23.64 19.29 7 12535 203 29561782
Septic shock 23.55 19.29 69 12473 62491 29499494
Incorrect drug administration rate 23.53 19.29 11 12531 1165 29560820
Product dose omission issue 23.41 19.29 6 12536 96377 29465608
Platelet count increased 23.33 19.29 23 12519 8440 29553545
Jaundice 22.85 19.29 43 12499 29253 29532732
Acute kidney injury 20.75 19.29 187 12355 265080 29296905
Oropharyngeal discomfort 20.39 19.29 13 12529 2543 29559442
Necrotising ulcerative gingivostomatitis 20.32 19.29 5 12537 70 29561915
Cardiac failure congestive 20.13 19.29 4 12538 76577 29485408
Hepatic cytolysis 19.94 19.29 21 12521 8326 29553659

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 610.87 15.29 588 30272 187069 64280803
Erythema 231.75 15.29 360 30500 186710 64281162
Nausea 231.41 15.29 860 30000 784940 63682932
Neutropenia 227.24 15.29 409 30451 239215 64228657
Mucosal inflammation 166.01 15.29 176 30684 62408 64405464
Encephalopathy 153.51 15.29 164 30696 58655 64409217
Drug ineffective 150.86 15.29 110 30750 840137 63627735
Neutrophil count decreased 129.83 15.29 172 30688 77024 64390848
Aplasia 122.74 15.29 62 30798 6891 64460981
Hypersensitivity 122.40 15.29 282 30578 196170 64271702
Flushing 118.27 15.29 166 30694 78482 64389390
Febrile bone marrow aplasia 114.99 15.29 70 30790 11185 64456687
Hiccups 114.63 15.29 63 30797 8313 64459559
Pyrexia 103.32 15.29 533 30327 558111 63909761
Hepatocellular injury 93.88 15.29 112 30748 45123 64422749
Decreased appetite 93.18 15.29 321 30539 280968 64186904
Bone marrow failure 90.24 15.29 113 30747 47839 64420033
Stomatitis 87.37 15.29 174 30686 109431 64358441
Toxicity to various agents 86.40 15.29 33 30827 363480 64104392
Computerised tomogram thorax abnormal 85.31 15.29 33 30827 1936 64465936
Neuropathy peripheral 83.58 15.29 178 30682 117347 64350525
Atelectasis 81.86 15.29 82 30778 27184 64440688
Sense of oppression 76.30 15.29 28 30832 1419 64466453
Thrombocytopenia 72.83 15.29 254 30606 223547 64244325
Fall 70.13 15.29 58 30802 416768 64051104
Vomiting 69.58 15.29 476 30384 550641 63917231
Anaphylactic shock 67.76 15.29 78 30782 30250 64437622
Gastrointestinal disorder 63.91 15.29 136 30724 89573 64378299
Diarrhoea 63.55 15.29 574 30286 722130 63745742
Vascular pain 62.83 15.29 21 30839 805 64467067
Oral pain 61.91 15.29 71 30789 27422 64440450
Hyponatraemia 58.68 15.29 180 30680 148159 64319713
Interstitial lung disease 53.96 15.29 134 30726 97598 64370274
Anaphylactic reaction 53.47 15.29 108 30752 68556 64399316
Leukopenia 50.91 15.29 134 30726 101108 64366764
Constipation 49.44 15.29 229 30631 229108 64238764
Feeling hot 48.36 15.29 82 30778 45581 64422291
Hypoxia 47.75 15.29 120 30740 88029 64379843
Palmar-plantar erythrodysaesthesia syndrome 46.54 15.29 63 30797 28756 64439116
Toxic encephalopathy 46.17 15.29 38 30822 9777 64458095
Oesophagitis 45.59 15.29 54 30806 21576 64446296
Infusion site streaking 44.76 15.29 14 30846 433 64467439
Intestinal ischaemia 44.72 15.29 40 30820 11509 64456363
Infusion related reaction 44.52 15.29 176 30684 164291 64303581
Oropharyngeal discomfort 44.04 15.29 29 30831 5306 64462566
Testicular germ cell cancer metastatic 42.04 15.29 9 30851 56 64467816
Product dose omission issue 40.97 15.29 21 30839 194726 64273146
Respiratory syncytial virus infection 40.31 15.29 31 30829 7237 64460635
Injection site vasculitis 39.91 15.29 7 30853 11 64467861
Computerised tomogram thorax 39.05 15.29 10 30850 146 64467726
Chest discomfort 38.76 15.29 133 30727 115973 64351899
Alopecia 38.33 15.29 169 30691 165521 64302351
Depression 38.21 15.29 20 30840 183271 64284601
White blood cell count decreased 38.05 15.29 163 30697 157674 64310198
Alveolitis 37.80 15.29 23 30837 3669 64464203
Fixed eruption 37.37 15.29 19 30841 2140 64465732
Paraesthesia 37.24 15.29 145 30715 134377 64333495
Platelet count decreased 35.77 15.29 167 30693 167544 64300328
Rash maculo-papular 35.46 15.29 73 30787 46953 64420919
Dyspnoea 35.35 15.29 510 30350 718164 63749708
Asthma 34.43 15.29 3 30857 95222 64372650
Condition aggravated 34.28 15.29 80 30780 372346 64095526
Cardiac failure congestive 34.20 15.29 10 30850 130570 64337302
Overdose 33.87 15.29 17 30843 159549 64308323
Inappropriate antidiuretic hormone secretion 33.40 15.29 47 30813 22242 64445630
Seminoma 32.22 15.29 9 30851 186 64467686
Hypokalaemia 31.80 15.29 129 30731 121774 64346098
Chemotherapy 31.25 15.29 15 30845 1492 64466380
Colony stimulating factor therapy 31.03 15.29 11 30849 504 64467368
Myocardial infarction 30.48 15.29 21 30839 165800 64302072
Dermatitis acneiform 30.26 15.29 28 30832 8415 64459457
Mobility decreased 30.24 15.29 3 30857 85837 64382035
Balance disorder 29.40 15.29 3 30857 83923 64383949
Injection site phlebitis 29.12 15.29 8 30852 155 64467717
Hepatic cytolysis 27.85 15.29 34 30826 14015 64453857
Rheumatoid arthritis 27.39 15.29 23 30837 164271 64303601
Abdominal pain 27.21 15.29 248 30612 312127 64155745
Enteritis 26.87 15.29 31 30829 12046 64455826
Chills 26.60 15.29 133 30727 137131 64330741
Tonsillar haemorrhage 25.59 15.29 8 30852 247 64467625
Septic shock 25.48 15.29 109 30751 105328 64362544
Cholestasis 25.25 15.29 62 30798 44810 64423062
Musculoskeletal stiffness 24.86 15.29 14 30846 123192 64344680
Arthritis 24.71 15.29 5 30855 83809 64384063
Dysgeusia 24.38 15.29 63 30797 46984 64420888
Intentional product misuse 24.27 15.29 3 30857 72292 64395580
Neutropenic colitis 24.23 15.29 19 30841 4562 64463310
Cardiotoxicity 23.92 15.29 27 30833 10247 64457625
Dental fistula 23.78 15.29 9 30851 497 64467375
Chronic obstructive pulmonary disease 23.73 15.29 3 30857 71045 64396827
Periorbital cellulitis 23.56 15.29 10 30850 746 64467126
Drug clearance decreased 23.49 15.29 15 30845 2604 64465268
Epistaxis 23.37 15.29 101 30759 98030 64369842
Dehydration 23.05 15.29 180 30680 216583 64251289
Folliculitis 23.04 15.29 47 30813 30030 64437842
Ileus 22.68 15.29 40 30820 22926 64444946
Muscle injury 22.28 15.29 43 30817 26394 64441478
Suicidal ideation 21.77 15.29 3 30857 66539 64401333
Joint swelling 21.66 15.29 44 30816 215338 64252534
Influenza 21.64 15.29 12 30848 106519 64361353
Antinuclear antibody 21.14 15.29 8 30852 442 64467430
Bronchitis 21.03 15.29 13 30847 108730 64359142
Hyperthermia 20.69 15.29 31 30829 15519 64452353
Hypomagnesaemia 20.35 15.29 51 30809 37325 64430547
Nail infection 20.19 15.29 12 30848 1835 64466037
Anorectal disorder 19.65 15.29 12 30848 1927 64465945
Intercepted product administration error 19.62 15.29 6 30854 172 64467700
Chemotherapeutic drug level increased 19.26 15.29 7 30853 345 64467527
Peritonitis 19.04 15.29 39 30821 24984 64442888
Malaise 18.90 15.29 280 30580 395967 64071905
Wrong technique in product usage process 18.90 15.29 4 30856 64970 64402902
Drug hypersensitivity 18.86 15.29 55 30805 237760 64230112
Regurgitation 18.72 15.29 12 30848 2097 64465775
Infusion site vesicles 18.51 15.29 7 30853 386 64467486
Thrombocytopenic purpura 18.45 15.29 12 30848 2150 64465722
Keratitis 18.37 15.29 14 30846 3223 64464649
Osteoarthritis 18.22 15.29 4 30856 63332 64404540
Loss of personal independence in daily activities 18.16 15.29 6 30854 72448 64395424
Chronic kidney disease 18.05 15.29 3 30857 57916 64409956
Administration site oedema 18.04 15.29 4 30856 30 64467842
Large intestine perforation 18.03 15.29 26 30834 12578 64455294
Sputum abnormal 18.00 15.29 9 30851 978 64466894
Disseminated intravascular coagulation 17.46 15.29 44 30816 32304 64435568
Gait disturbance 17.45 15.29 35 30825 172120 64295752
Hallucination, tactile 17.11 15.29 7 30853 476 64467396
Hypermagnesaemia 17.10 15.29 9 30851 1088 64466784
Aortitis 17.07 15.29 9 30851 1092 64466780
Hypoglycaemia 17.03 15.29 11 30849 89881 64377991
Skin reaction 16.97 15.29 25 30835 12327 64455545
Laryngeal discomfort 16.89 15.29 7 30853 492 64467380
Heart rate decreased 16.84 15.29 3 30857 55064 64412808
Cerebellar syndrome 16.76 15.29 16 30844 5000 64462872
Onychalgia 16.73 15.29 8 30852 789 64467083
Duodenal ulcer perforation 16.55 15.29 45 30815 34580 64433292
Body temperature abnormal 16.48 15.29 10 30850 1588 64466284
Pain 16.23 15.29 178 30682 553333 63914539
Coombs positive haemolytic anaemia 16.00 15.29 8 30852 870 64467002
Type III immune complex mediated reaction 15.92 15.29 7 30853 569 64467303
Palmar erythema 15.85 15.29 10 30850 1700 64466172
Seizure 15.79 15.29 135 30725 166757 64301115
Cerebrovascular accident 15.70 15.29 26 30834 137557 64330315
Influenza like illness 15.65 15.29 5 30855 61697 64406175
Therapeutic response decreased 15.62 15.29 3 30857 52185 64415687
Hyperammonaemic encephalopathy 15.60 15.29 14 30846 4044 64463828

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A04AD12 ALIMENTARY TRACT AND METABOLISM
ANTIEMETICS AND ANTINAUSEANTS
ANTIEMETICS AND ANTINAUSEANTS
Other antiemetics
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
FDA MoA N0000182141 Cytochrome P450 3A4 Inhibitors
FDA MoA N0000185506 Cytochrome P450 3A4 Inducers
FDA MoA N0000185507 Cytochrome P450 2C9 Inducers
CHEBI has role CHEBI:35469 antidepressants
CHEBI has role CHEBI:49110 peripheral nervous system drugs
CHEBI has role CHEBI:50919 antiemetico
CHEBI has role CHEBI:55350 neurokinin-1 receptor antagonists
CHEBI has role CHEBI:55351 substance P receptor antagonists

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

DiseaseRelationSNOMED_IDDOID
Chemotherapy-induced nausea and vomiting indication 236084000
Prevention of Post-Operative Nausea and Vomiting indication
Hepatic failure contraindication 59927004




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 8.8 acidic
pKa2 13.0 acidic
pKa3 3.22 Basic
pKa4 2.56 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
125MG EMEND MERCK N021549 March 26, 2003 RX CAPSULE ORAL 8258132 Sept. 26, 2027 FOR THE PREVENTION OF NAUSEA AND VOMITING ASSOCIATED WITH CHEMOTHERAPY
125MG EMEND MERCK N021549 March 26, 2003 RX CAPSULE ORAL 8258132 Sept. 26, 2027 PREVENTION OF POSTOPERATIVE NAUSEA AND VOMITING
40MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** EMEND MERCK N021549 June 30, 2006 DISCN CAPSULE ORAL 8258132 Sept. 26, 2027 FOR THE PREVENTION OF NAUSEA AND VOMITING ASSOCIATED WITH CHEMOTHERAPY
40MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** EMEND MERCK N021549 June 30, 2006 DISCN CAPSULE ORAL 8258132 Sept. 26, 2027 PREVENTION OF POSTOPERATIVE NAUSEA AND VOMITING
80MG EMEND MERCK N021549 March 26, 2003 RX CAPSULE ORAL 8258132 Sept. 26, 2027 FOR THE PREVENTION OF NAUSEA AND VOMITING ASSOCIATED WITH CHEMOTHERAPY
80MG EMEND MERCK N021549 March 26, 2003 RX CAPSULE ORAL 8258132 Sept. 26, 2027 PREVENTION OF POSTOPERATIVE NAUSEA AND VOMITING
125MG/KIT EMEND MSD MERCK CO N207865 Dec. 17, 2015 RX FOR SUSPENSION ORAL 8258132 Sept. 26, 2027 PREVENTION OF NAUSEA AND VOMITING ASSOCIATED WITH CHEMOTHERAPY (CINV)
130MG/18ML (7.2MG/ML) CINVANTI HERON THERAPS INC N209296 Nov. 9, 2017 RX EMULSION INTRAVENOUS 10624850 Sept. 18, 2035 TREATMENT OF NAUSEA AND VOMITING, INCLUDING THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY OR MODERATELY EMETOGENIC CANCER CHEMOTHERAPY
130MG/18ML (7.2MG/ML) CINVANTI HERON THERAPS INC N209296 Nov. 9, 2017 RX EMULSION INTRAVENOUS 10953018 Sept. 18, 2035 TREATMENT OF NAUSEA AND VOMITING, INCLUDING THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY OR MODERATELY EMETOGENIC CANCER CHEMOTHERAPY
130MG/18ML (7.2MG/ML) CINVANTI HERON THERAPS INC N209296 Nov. 9, 2017 RX EMULSION INTRAVENOUS 9561229 Sept. 18, 2035 TREATMENT OF NAUSEA AND VOMITING, INCLUDING THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY OR MODERATELY EMETOGENIC CANCER CHEMOTHERAPY
130MG/18ML (7.2MG/ML) CINVANTI HERON THERAPS INC N209296 Nov. 9, 2017 RX EMULSION INTRAVENOUS 9808465 Sept. 18, 2035 TREATMENT OF NAUSEA AND VOMITING, INCLUDING THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY OR MODERATELY EMETOGENIC CANCER CHEMOTHERAPY
130MG/18ML (7.2MG/ML) CINVANTI HERON THERAPS INC N209296 Nov. 9, 2017 RX EMULSION INTRAVENOUS 9974794 Sept. 18, 2035 TREATMENT OF NAUSEA AND VOMITING, INCLUDING THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY OR MODERATELY EMETOGENIC CANCER CHEMOTHERAPY

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Substance-P receptor GPCR ANTAGONIST Ki 10.70 CHEMBL CHEMBL
Cytochrome P450 3A4 Enzyme WOMBAT-PK
Neuromedin-K receptor GPCR Ki 6.34 CHEMBL
Substance-P receptor GPCR IC50 10.05 CHEMBL

External reference:

IDSource
D02968 KEGG_DRUG
357280 RXNORM
C1176306 UMLSCUI
CHEBI:499361 CHEBI
CHEMBL1471 ChEMBL_ID
CHEMBL1201782 ChEMBL_ID
D000077608 MESH_DESCRIPTOR_UI
DB00673 DRUGBANK_ID
3490 IUPHAR_LIGAND_ID
8050 INN_ID
1NF15YR6UY UNII
135413536 PUBCHEM_CID
17180 MMSL
247683 MMSL
46392 MMSL
d04855 MMSL
009926 NDDF
4021391 VANDF
398690007 SNOMEDCT_US
409205009 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
EMEND HUMAN PRESCRIPTION DRUG LABEL 1 0006-0461 CAPSULE 80 mg ORAL NDA 31 sections
EMEND HUMAN PRESCRIPTION DRUG LABEL 1 0006-0461 CAPSULE 80 mg ORAL NDA 31 sections
EMEND HUMAN PRESCRIPTION DRUG LABEL 1 0006-0462 CAPSULE 125 mg ORAL NDA 31 sections
EMEND HUMAN PRESCRIPTION DRUG LABEL 1 0006-0462 CAPSULE 125 mg ORAL NDA 31 sections
EMEND HUMAN PRESCRIPTION DRUG LABEL 1 0006-0464 CAPSULE 40 mg ORAL NDA 31 sections
EMEND HUMAN PRESCRIPTION DRUG LABEL 1 0006-0464 CAPSULE 40 mg ORAL NDA 31 sections
EMEND HUMAN PRESCRIPTION DRUG LABEL 1 0006-3066 POWDER, FOR SUSPENSION 125 mg ORAL NDA 31 sections
EMEND HUMAN PRESCRIPTION DRUG LABEL 1 0006-3066 POWDER, FOR SUSPENSION 125 mg ORAL NDA 31 sections
Aprepitant HUMAN PRESCRIPTION DRUG LABEL 1 0781-2321 CAPSULE 40 mg ORAL ANDA 26 sections
Aprepitant HUMAN PRESCRIPTION DRUG LABEL 1 0781-2322 CAPSULE 80 mg ORAL ANDA 26 sections
Aprepitant HUMAN PRESCRIPTION DRUG LABEL 1 0781-2323 CAPSULE 125 mg ORAL ANDA 26 sections
APREPITANT HUMAN PRESCRIPTION DRUG LABEL 1 13668-591 CAPSULE 40 mg ORAL ANDA 25 sections
APREPITANT HUMAN PRESCRIPTION DRUG LABEL 1 13668-592 CAPSULE 80 mg ORAL ANDA 25 sections
APREPITANT HUMAN PRESCRIPTION DRUG LABEL 1 13668-593 CAPSULE 125 mg ORAL ANDA 25 sections
EMEND HUMAN PRESCRIPTION DRUG LABEL 1 42254-160 CAPSULE 40 mg ORAL NDA 26 sections
CINVANTI HUMAN PRESCRIPTION DRUG LABEL 1 47426-201 INJECTION, EMULSION 130 mg INTRAVENOUS NDA 33 sections
CINVANTI HUMAN PRESCRIPTION DRUG LABEL 1 47426-201 INJECTION, EMULSION 130 mg INTRAVENOUS NDA 33 sections
EMEND HUMAN PRESCRIPTION DRUG LABEL 1 54868-5231 CAPSULE 80 mg ORAL NDA 26 sections
Aprepitant HUMAN PRESCRIPTION DRUG LABEL 1 68462-583 CAPSULE 40 mg ORAL ANDA 25 sections
Aprepitant HUMAN PRESCRIPTION DRUG LABEL 1 68462-584 CAPSULE 80 mg ORAL ANDA 25 sections
Aprepitant HUMAN PRESCRIPTION DRUG LABEL 1 68462-585 CAPSULE 125 mg ORAL ANDA 25 sections