aprepitant 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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 µM/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
S (Water solubility) 0.02 mg/mL Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 4.047 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 2.710 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 46.345 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 4.064 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 0.640 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 2.330 % High 1
herg hERG pIC50 4.860 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 6.808 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 17.258 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 0.970 % High 1
kinase-safety-class ACVR2B,AXL,EIF2AK3,ERBB2,GRK2,PDK1,PDK2,PDK4,PRKDC 9
kinase-selectivity-class AXL,EIF2AK3,GRK2 3
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 8.222 High 1
mh-clint Mouse hepatocyte intrinsic clearance 17.418 High 1
mppb Mouse plasma protein binding (% unbound) 0.970 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 36.308 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 1
pppb Pig plasma protein binding (% unbound) 1.660 % High 1
rh-clint Rat hepatocyte intrinsic clearance 9.817 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 5.760 % High 1
rppb Rat plasma protein binding (% unbound) 0.810 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 42.073 uM High 1

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
Sleep disorder due to general medical condition, insomnia type 417.69 18.17 569 87812 128125 90411941
Drug ineffective 362.53 18.17 495 87886 1383803 89156263
Folliculitis 355.20 18.17 680 87701 203673 90336393
Febrile neutropenia 345.65 18.17 582 87799 157767 90382299
Muscle injury 325.79 18.17 603 87778 176051 90364015
Impaired healing 304.71 18.17 692 87689 233507 90306559
Fall 304.39 18.17 52 88329 481758 90058308
Ill-defined disorder 300.26 18.17 598 87783 184293 90355773
Helicobacter infection 293.68 18.17 669 87712 226181 90313885
Gastrointestinal disorder 285.91 18.17 714 87667 255973 90284093
Irritable bowel syndrome 282.18 18.17 624 87757 206824 90333242
Duodenal ulcer perforation 272.58 18.17 640 87741 220648 90319418
Stomatitis 252.02 18.17 711 87670 273987 90266079
Porphyria acute 249.95 18.17 177 88204 17798 90522268
Sleep disorder 219.48 18.17 550 87831 197480 90342586
Lower respiratory tract infection 210.78 18.17 629 87752 250030 90290036
Injury 200.00 18.17 530 87851 196819 90343247
Hand deformity 196.89 18.17 686 87695 295676 90244390
Medication error 195.08 18.17 319 88062 84333 90455733
Contusion 190.39 18.17 608 87773 250608 90289458
Facet joint syndrome 190.25 18.17 343 88038 98046 90442020
X-ray abnormal 186.78 18.17 226 88155 45198 90494868
Liver disorder 182.21 18.17 380 88001 120889 90419177
Blister 180.51 18.17 603 87778 254395 90285671
Toxicity to various agents 171.11 18.17 36 88345 287810 90252256
Feeling hot 170.40 18.17 287 88094 77721 90462345
Glossodynia 169.87 18.17 692 87689 321087 90218979
Product dose omission issue 168.30 18.17 39 88342 291648 90248418
Anti-cyclic citrullinated peptide antibody positive 164.57 18.17 556 87825 235877 90304189
Lip dry 164.28 18.17 327 88054 100628 90439438
Lupus vulgaris 162.59 18.17 210 88171 44849 90495217
Grip strength 159.84 18.17 103 88278 8862 90531204
Computerised tomogram thorax abnormal 138.34 18.17 58 88323 2029 90538037
C-reactive protein abnormal 138.02 18.17 351 88030 127078 90412988
Road traffic accident 136.40 18.17 315 88066 107311 90432755
Bone erosion 133.37 18.17 208 88173 52813 90487253
Retinitis 132.17 18.17 175 88206 38283 90501783
Lower limb fracture 131.90 18.17 270 88111 84743 90455323
Pericarditis 130.81 18.17 566 87815 269585 90270481
Joint range of motion decreased 130.00 18.17 357 88024 135286 90404780
Deep vein thrombosis postoperative 129.45 18.17 241 88140 70568 90469498
Infusion related reaction 127.90 18.17 768 87613 416012 90124054
Hypersensitivity 127.13 18.17 818 87563 453859 90086207
Dislocation of vertebra 126.33 18.17 209 88172 55759 90484307
Infection 121.97 18.17 684 87697 361410 90178656
Discomfort 120.21 18.17 558 87823 273777 90266289
Frequent bowel movements 117.12 18.17 204 88177 56731 90483335
Adjustment disorder with depressed mood 114.99 18.17 202 88179 56551 90483515
Pyrexia 112.64 18.17 1059 87322 659426 89880640
Autoimmune disorder 112.34 18.17 238 88143 76506 90463560
Wound 111.22 18.17 586 87795 302394 90237672
Swollen joint count 110.66 18.17 81 88300 8572 90531494
Sinusitis 109.56 18.17 639 87742 342449 90197617
Hepatic enzyme increased 108.87 18.17 662 87719 360074 90179992
Sciatica 107.42 18.17 277 88104 101105 90438961
Confusional state 106.16 18.17 692 87689 385513 90154553
Maternal exposure timing unspecified 105.96 18.17 120 88261 22363 90517703
Lupus-like syndrome 105.70 18.17 179 88202 48667 90491399
Computerised tomogram thorax 105.00 18.17 33 88348 492 90539574
Synovitis 104.53 18.17 613 87768 329139 90210927
Insomnia 104.47 18.17 618 87763 332856 90207210
Injection site pain 98.61 18.17 24 88357 173675 90366391
Breast cancer stage III 96.01 18.17 237 88144 84210 90455856
Systemic lupus erythematosus 94.93 18.17 641 87740 361255 90178811
General physical health deterioration 94.35 18.17 631 87750 354484 90185582
Urinary tract infection 93.52 18.17 96 88285 305536 90234530
Colitis ulcerative 92.99 18.17 191 88190 60075 90479991
Laryngitis 90.58 18.17 171 88210 50582 90489484
Swollen joint count increased 90.43 18.17 276 88105 110930 90429136
Exostosis 89.89 18.17 175 88206 52959 90487107
Influenza 87.85 18.17 15 88366 139249 90400817
Bursitis 86.60 18.17 304 88077 131350 90408716
Overdose 83.47 18.17 25 88356 157684 90382382
Somnolence 82.36 18.17 51 88330 209033 90331033
Atelectasis 82.22 18.17 110 88271 24299 90515767
C-reactive protein 81.60 18.17 125 88256 31242 90508824
Rheumatic fever 78.82 18.17 327 88054 152794 90387272
Pregnancy 77.92 18.17 181 88200 61866 90478200
Blood pressure increased 77.82 18.17 48 88333 197169 90342897
Rheumatoid factor positive 75.74 18.17 350 88031 171300 90368766
Mucosal inflammation 75.56 18.17 171 88210 57454 90482612
Night sweats 74.30 18.17 285 88096 128481 90411585
Hepatic cirrhosis 73.46 18.17 179 88202 63074 90476992
Myocardial infarction 72.43 18.17 9 88372 105963 90434103
Pemphigus 71.84 18.17 555 87826 326309 90213757
Pancreatitis 71.10 18.17 188 88193 69638 90470428
Injection site reaction 70.40 18.17 5 88376 92075 90447991
Febrile bone marrow aplasia 69.54 18.17 65 88316 9673 90530393
Balance disorder 69.48 18.17 7 88374 97073 90442993
Nasopharyngitis 69.33 18.17 653 87728 406451 90133615
Peripheral venous disease 68.88 18.17 209 88172 83712 90456354
Cardiac failure congestive 68.39 18.17 8 88373 98686 90441380
Lung disorder 67.88 18.17 308 88073 149575 90390491
Wound infection 67.65 18.17 243 88138 106159 90433907
Anti-cyclic citrullinated peptide antibody 67.35 18.17 106 88275 27115 90512951
Fibromyalgia 66.93 18.17 386 87995 205883 90334183
Death 65.58 18.17 227 88154 456324 90083742
Delirium 63.53 18.17 235 88146 104124 90435942
Stress 63.46 18.17 4 88377 81391 90458675
Rectal haemorrhage 63.22 18.17 201 88180 82543 90457523
Weight increased 61.77 18.17 651 87730 417276 90122790
Drug tolerance decreased 60.77 18.17 111 88270 32019 90508047
Chronic obstructive pulmonary disease 59.49 18.17 3 88378 73826 90466240
Headache 58.90 18.17 548 87833 862198 89677868
Pneumonia 58.71 18.17 373 88008 637686 89902380
Neutrophil count decreased 57.63 18.17 177 88204 71355 90468711
Influenza like illness 57.21 18.17 6 88375 80605 90459461
Suicidal ideation 56.49 18.17 4 88377 73851 90466215
COVID-19 56.34 18.17 49 88332 168794 90371272
Weight fluctuation 56.08 18.17 82 88299 19667 90520399
Obesity 55.60 18.17 227 88154 105280 90434786
Nasal congestion 54.82 18.17 8 88373 83406 90456660
Prescribed overdose 54.61 18.17 214 88167 97411 90442655
Dry mouth 54.29 18.17 336 88045 183723 90356343
Pulmonary fibrosis 54.07 18.17 228 88153 107275 90432791
Pain 53.87 18.17 668 87713 995673 89544393
Swelling 53.82 18.17 635 87746 418423 90121643
Aplasia 52.49 18.17 38 88343 3953 90536113
Pruritus 52.28 18.17 779 87602 540746 89999320
Decreased appetite 52.13 18.17 579 87802 375961 90164105
Herpes zoster 51.93 18.17 14 88367 94630 90445436
Laboratory test abnormal 51.35 18.17 121 88260 41733 90498333
Gastrooesophageal reflux disease 51.12 18.17 52 88329 166285 90373781
Alopecia 50.47 18.17 719 87662 494352 90045714
Ear infection 50.14 18.17 166 88215 69609 90470457
Renal impairment 50.10 18.17 20 88361 105401 90434665
Cognitive disorder 49.68 18.17 5 88376 69402 90470664
Injection site erythema 49.66 18.17 17 88364 98485 90441581
Inflammation 48.34 18.17 319 88062 178273 90361793
Rheumatoid arthritis 48.11 18.17 553 87828 362061 90178005
Injection site phlebitis 47.62 18.17 13 88368 114 90539952
Sleep disorder due to a general medical condition 47.12 18.17 122 88259 44616 90495450
Incorrect dose administered 46.59 18.17 10 88371 78920 90461146
White blood cell count increased 46.57 18.17 158 88223 67083 90472983
Cystitis haemorrhagic 45.66 18.17 40 88341 5473 90534593
Haematochezia 43.92 18.17 8 88373 70905 90469161
Cerebrovascular accident 43.50 18.17 34 88347 123499 90416567
Musculoskeletal pain 43.42 18.17 301 88080 170950 90369116
Encephalopathy 43.23 18.17 121 88260 46323 90493743
Myalgia 43.06 18.17 65 88316 175060 90365006
Type 2 diabetes mellitus 42.34 18.17 341 88040 202903 90337163
Cellulitis 42.32 18.17 18 88363 91319 90448747
Blood glucose increased 42.20 18.17 20 88361 95226 90444840
Palpitations 41.72 18.17 43 88338 136685 90403381
Acute kidney injury 41.58 18.17 166 88215 320221 90219845
Depressed level of consciousness 41.40 18.17 10 88371 72774 90467292
Ulcer haemorrhage 41.28 18.17 84 88297 26237 90513829
Foot deformity 41.16 18.17 140 88241 59511 90480555
Arthropathy 41.00 18.17 541 87840 365701 90174365
Cardiac disorder 40.96 18.17 4 88377 56868 90483198
Neck pain 40.59 18.17 31 88350 113932 90426134
Wheezing 40.01 18.17 381 88000 237699 90302367
Abdominal distension 39.93 18.17 41 88340 130560 90409506
Dry eye 39.39 18.17 5 88376 57926 90482140
Therapy non-responder 39.33 18.17 248 88133 136456 90403610
Amnesia 39.13 18.17 209 88172 108296 90431770
Unevaluable event 39.13 18.17 4 88377 54844 90485222
Hypoglycaemia 38.95 18.17 10 88371 69838 90470228
Therapeutic product effect incomplete 38.64 18.17 82 88299 193814 90346252
Wrong technique in product usage process 38.49 18.17 11 88370 71560 90468506
Rhinorrhoea 38.44 18.17 19 88362 88297 90451769
Hypotension 38.29 18.17 175 88206 325222 90214844
Psoriasis 38.13 18.17 53 88328 147701 90392365
Hepatocellular injury 38.03 18.17 86 88295 28872 90511194
Alveolitis 38.00 18.17 28 88353 2993 90537073
Heart rate decreased 37.92 18.17 4 88377 53501 90486565
Lactic acidosis 37.83 18.17 3 88378 50460 90489606
Feeling abnormal 37.44 18.17 66 88315 167169 90372897
Blood pressure systolic increased 37.42 18.17 6 88375 58339 90481727
Bronchitis 37.36 18.17 57 88324 152870 90387196
Gastrointestinal haemorrhage 36.94 18.17 21 88360 90227 90449839
Prescribed underdose 36.85 18.17 158 88223 74861 90465205
Injection site vasculitis 36.69 18.17 7 88374 7 90540059
Walking aid user 35.53 18.17 95 88286 35411 90504655
Renal failure 34.81 18.17 46 88335 130961 90409105
Anaphylactic shock 34.10 18.17 87 88294 31530 90508536
Tremor 33.79 18.17 61 88320 153112 90386954
Hypoxia 33.67 18.17 150 88231 72249 90467817
Flushing 33.66 18.17 173 88208 88318 90451748
Vascular pain 33.19 18.17 17 88364 945 90539121
Diabetes mellitus 33.04 18.17 11 88370 64864 90475202
Cystitis 32.79 18.17 12 88369 66706 90473360
Off label use 32.24 18.17 824 87557 1101428 89438638
Haemoglobin decreased 31.85 18.17 69 88312 161887 90378179
Hyperkalaemia 31.40 18.17 12 88369 64952 90475114
Infusion site streaking 31.33 18.17 14 88367 573 90539493
Sense of oppression 31.05 18.17 17 88364 1083 90538983
Anaemia 30.98 18.17 209 88172 352593 90187473
Electrocardiogram QT prolonged 30.91 18.17 16 88365 72440 90467626
Pulmonary oedema 30.80 18.17 11 88370 62069 90477997
Tonsillar haemorrhage 30.52 18.17 11 88370 254 90539812
Nail bed inflammation 30.41 18.17 20 88361 1781 90538285
Cholelithiasis 30.29 18.17 7 88374 52499 90487567
Skin ulcer 30.26 18.17 6 88375 50069 90489997
Thrombocytopenia 30.24 18.17 324 88057 208401 90331665
Chemotherapy 30.15 18.17 20 88361 1807 90538259
Coeliac disease 29.97 18.17 4 88377 44606 90495460
Heart rate increased 29.63 18.17 40 88341 112862 90427204
Cardiac failure 29.55 18.17 38 88343 109458 90430608
Cataract 29.19 18.17 17 88364 72075 90467991
Grip strength decreased 29.19 18.17 172 88209 92404 90447662
Peripheral swelling 29.11 18.17 565 87816 412541 90127525
Syncope 29.11 18.17 53 88328 132610 90407456
Intentional product misuse 28.69 18.17 27 88354 89577 90450489
Blood creatinine increased 28.60 18.17 34 88347 101352 90438714
Angioedema 28.17 18.17 14 88367 64862 90475204
Pulmonary hypertension 28.12 18.17 4 88377 42519 90497547
Dyspnoea exertional 27.94 18.17 18 88363 72270 90467796
Cardiac arrest 27.72 18.17 37 88344 104898 90435168
Streptococcal sepsis 27.69 18.17 25 88356 3559 90536507
Orthostatic hypotension 27.51 18.17 4 88377 41823 90498243
Nasal mucosal disorder 27.47 18.17 19 88362 1838 90538228
Haemorrhage 27.18 18.17 17 88364 69352 90470714
Lip swelling 27.07 18.17 3 88378 38607 90501459
Lymphadenopathy 26.61 18.17 6 88375 45769 90494297
Fluid intake reduced 26.40 18.17 26 88355 4126 90535940
Foetal exposure during pregnancy 26.29 18.17 5 88376 42970 90497096
Disease recurrence 26.21 18.17 3 88378 37650 90502416
Vascular device infection 26.11 18.17 44 88337 11908 90528158
Burning sensation 25.63 18.17 15 88366 63437 90476629
Pseudomonal sepsis 25.63 18.17 26 88355 4276 90535790
Full blood count abnormal 25.27 18.17 3 88378 36594 90503472
Eye pain 25.25 18.17 6 88375 44162 90495904
Neutropenia 25.04 18.17 332 88049 224572 90315494
Adverse event 24.98 18.17 198 88183 117220 90422846
Viral infection 24.95 18.17 5 88376 41409 90498657
Blood pressure fluctuation 24.81 18.17 10 88371 52403 90487663
Inappropriate schedule of product administration 24.69 18.17 70 88311 149863 90390203
Therapy interrupted 24.65 18.17 9 88372 50099 90489967
Breast cancer 24.26 18.17 11 88370 53750 90486316
Vision blurred 24.25 18.17 44 88337 110249 90429817
Dysphonia 23.98 18.17 16 88365 63068 90476998
Oedema 23.69 18.17 299 88082 199996 90340070
Inappropriate antidiuretic hormone secretion 23.50 18.17 56 88325 19449 90520617
Sedation 23.11 18.17 9 88372 48162 90491904
Therapy cessation 22.74 18.17 4 88377 36357 90503709
Loss of consciousness 22.70 18.17 66 88315 140172 90399894
Premature delivery 22.69 18.17 5 88376 38757 90501309
Bone marrow failure 22.56 18.17 76 88305 32145 90507921
International normalised ratio increased 22.44 18.17 9 88372 47307 90492759
Procedural pain 22.39 18.17 3 88378 33357 90506709
Rhabdomyolysis 22.34 18.17 11 88370 51245 90488821
Fluid retention 22.32 18.17 32 88349 88059 90452007
Hallucination 22.17 18.17 19 88362 65940 90474126
Intestinal strangulation 22.05 18.17 7 88374 108 90539958
Finger deformity 21.98 18.17 3 88378 32894 90507172
Cough 21.90 18.17 242 88139 368720 90171346
Joint injury 21.77 18.17 3 88378 32661 90507405
Agitation 21.74 18.17 20 88361 67078 90472988
Onychomycosis 21.52 18.17 5 88376 37371 90502695
Skin lesion 21.51 18.17 5 88376 37360 90502706
Acute polyneuropathy 21.47 18.17 10 88371 451 90539615
Mental disorder 21.47 18.17 3 88378 32315 90507751
Drug ineffective for unapproved indication 21.43 18.17 20 88361 66624 90473442
Hypercholesterolaemia 21.39 18.17 170 88211 100722 90439344
Hiccups 21.23 18.17 20 88361 3006 90537060
Osteoporosis 21.20 18.17 164 88217 96367 90443699
Hemianopia 21.16 18.17 17 88364 2065 90538001
Skin exfoliation 21.12 18.17 21 88360 67892 90472174
Diverticulitis 20.78 18.17 9 88372 45178 90494888
Pneumonia aspiration 20.74 18.17 7 88374 40933 90499133
Surgery 20.54 18.17 9 88372 44878 90495188
Fungal infection 20.42 18.17 8 88373 42653 90497413
Dry skin 20.40 18.17 34 88347 88039 90452027
Blood pressure decreased 20.20 18.17 26 88355 74869 90465197
Hip fracture 19.91 18.17 4 88377 33073 90506993
Drug resistance 19.82 18.17 3 88378 30446 90509620
Coma 19.81 18.17 25 88356 72607 90467459
Dizziness 19.79 18.17 431 87950 588853 89951213
Respiratory disorder 19.52 18.17 119 88262 64697 90475369
Liver function test increased 19.43 18.17 33 88348 84822 90455244
Melaena 19.36 18.17 5 88376 34792 90505274
Neutropenic colitis 19.33 18.17 22 88359 4121 90535945
Sneezing 19.31 18.17 3 88378 29866 90510200
Immunodeficiency 19.27 18.17 9 88372 43225 90496841
Abdominal discomfort 19.19 18.17 605 87776 476723 90063343
Pericardial effusion 19.19 18.17 6 88375 36827 90503239
Full blood count decreased 19.16 18.17 3 88378 29686 90510380
Plasma cell myeloma 18.98 18.17 8 88373 40820 90499246
Blood cholesterol increased 18.75 18.17 296 88085 207716 90332350
Nervousness 18.75 18.17 5 88376 34051 90506015
Sepsis 18.67 18.17 101 88280 179713 90360353
Therapeutic product effect decreased 18.64 18.17 377 88004 277194 90262872
Eye pruritus 18.58 18.17 3 88378 29024 90511042
Pain in jaw 18.47 18.17 12 88369 47973 90492093
Psoriatic arthropathy 18.40 18.17 319 88062 228016 90312050
Subacute cutaneous lupus erythematosus 18.39 18.17 20 88361 3562 90536504
Vaginal haemorrhage 18.37 18.17 4 88377 31267 90508799
Hepatotoxicity 18.29 18.17 11 88370 45831 90494235
Renal disorder 18.29 18.17 7 88374 37852 90502214
Blood potassium decreased 18.28 18.17 12 88369 47715 90492351
Joint dislocation 18.25 18.17 89 88292 44493 90495573
Gastric disorder 18.19 18.17 5 88376 33379 90506687

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 311.75 19.30 380 16979 185323 42418653
Drug ineffective 129.46 19.30 48 17311 630149 41973827
Hiccups 125.75 19.30 72 17287 12099 42591877
Hypersensitivity 111.11 19.30 142 17217 72228 42531748
Neutrophil count decreased 107.86 19.30 131 17228 63284 42540692
Nausea 106.17 19.30 378 16981 396421 42207555
Stomatitis 104.09 19.30 115 17244 50214 42553762
Erythema 99.32 19.30 167 17192 108626 42495350
Neutropenia 90.22 19.30 229 17130 199202 42404774
Decreased appetite 83.44 19.30 218 17141 192919 42411057
Hepatic cytolysis 67.31 19.30 68 17291 26776 42577200
Aplasia 61.97 19.30 33 17326 4810 42599166
Encephalopathy 61.64 19.30 80 17279 41253 42562723
Toxicity to various agents 61.19 19.30 10 17349 229126 42374850
Anaphylactic reaction 61.06 19.30 81 17278 42662 42561314
Vomiting 60.82 19.30 256 17103 289467 42314509
Thrombocytopenia 60.07 19.30 192 17167 190087 42413889
Platelet count decreased 57.29 19.30 154 17205 138427 42465549
Interstitial lung disease 56.87 19.30 109 17250 78353 42525623
Hypokalaemia 56.17 19.30 103 17256 71618 42532358
Hepatocellular injury 55.77 19.30 58 17301 23620 42580356
Diarrhoea 55.29 19.30 348 17011 460501 42143475
Stoma site pain 54.48 19.30 18 17341 785 42603191
Mucosal inflammation 53.47 19.30 82 17277 49292 42554684
White blood cell count decreased 53.19 19.30 130 17229 110266 42493710
Change of bowel habit 52.18 19.30 19 17340 1110 42602866
Oesophagitis 50.38 19.30 45 17314 15202 42588774
Mouth ulceration 49.12 19.30 44 17315 14919 42589057
Neuropathy peripheral 48.06 19.30 119 17240 101734 42502242
Intestinal ischaemia 46.35 19.30 35 17324 9353 42594623
Testicular germ cell cancer metastatic 42.33 19.30 9 17350 65 42603911
Febrile bone marrow aplasia 41.71 19.30 34 17325 10147 42593829
Rash maculo-papular 41.61 19.30 63 17296 37440 42566536
Oral pain 41.26 19.30 37 17322 12559 42591417
Procalcitonin decreased 39.98 19.30 11 17348 254 42603722
Eosinophil percentage decreased 39.50 19.30 11 17348 266 42603710
Blood creatine decreased 39.34 19.30 11 17348 270 42603706
Emotional disorder 39.07 19.30 27 17332 6287 42597689
Pyrexia 39.03 19.30 284 17075 393758 42210218
Bone marrow failure 38.73 19.30 57 17302 33036 42570940
Product dose omission issue 38.46 19.30 8 17351 154357 42449619
Acute kidney injury 38.25 19.30 268 17091 367069 42236907
Fixed eruption 37.96 19.30 19 17340 2435 42601541
Leukopenia 37.02 19.30 89 17270 74657 42529319
Flushing 35.26 19.30 58 17301 36970 42567006
Toxic encephalopathy 34.49 19.30 26 17333 6927 42597049
Pancytopenia 32.80 19.30 114 17245 117629 42486347
Neutropenic colitis 32.18 19.30 21 17338 4449 42599527
Sense of oppression 31.89 19.30 11 17348 548 42603428
Condition aggravated 31.40 19.30 36 17323 260718 42343258
Septic shock 31.15 19.30 95 17264 91577 42512399
Anaphylactic shock 29.69 19.30 42 17317 23475 42580501
Seminoma 29.03 19.30 9 17350 319 42603657
Enteritis 28.21 19.30 28 17331 10788 42593188
Aortic valve calcification 27.95 19.30 10 17349 555 42603421
Infusion related reaction 27.56 19.30 70 17289 60736 42543240
Blood folate decreased 27.01 19.30 11 17348 870 42603106
Anaemia 26.52 19.30 200 17159 280078 42323898
Hyperthermia 26.42 19.30 29 17330 12545 42591431
Constipation 26.22 19.30 133 17226 162158 42441818
Chemotherapeutic drug level increased 25.55 19.30 8 17351 293 42603683
Alopecia 25.40 19.30 44 17315 29232 42574744
Herpes simplex reactivation 24.84 19.30 9 17350 518 42603458
Peritonitis 24.60 19.30 34 17325 18599 42585377
Chills 24.40 19.30 89 17270 93977 42509999
Large intestine perforation 23.61 19.30 24 17335 9512 42594464
Fall 22.59 19.30 38 17321 234482 42369494
Colitis 22.56 19.30 55 17304 46517 42557459
Hyperammonaemic encephalopathy 22.45 19.30 14 17345 2744 42601232
Cardiac failure congestive 22.23 19.30 4 17355 85598 42518378
Blood urea decreased 22.09 19.30 11 17348 1395 42602581
Regurgitation 21.44 19.30 12 17347 1928 42602048
Platelet count increased 21.31 19.30 24 17335 10679 42593297
Paraesthesia 21.20 19.30 72 17287 73387 42530589
Weight increased 20.74 19.30 9 17350 107974 42496002
Dehydration 20.70 19.30 113 17246 141654 42462322
Bicytopenia 20.61 19.30 14 17345 3170 42600806
Cholestasis 20.58 19.30 43 17316 32836 42571140
COVID-19 20.24 19.30 11 17348 115937 42488039
Oxygen saturation decreased 20.09 19.30 65 17294 64622 42539354
Hypochloraemia 19.87 19.30 9 17350 924 42603052
Necrotising ulcerative gingivostomatitis 19.51 19.30 5 17354 87 42603889
Blood chloride decreased 19.48 19.30 15 17344 4124 42599852
Atrioventricular block second degree 19.33 19.30 15 17344 4172 42599804

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 467.42 17.66 917 94663 315850 110177869
Sleep disorder due to general medical condition, insomnia type 377.47 17.66 461 95119 105182 110388537
Drug ineffective 371.99 17.66 463 95117 1520077 108973642
Folliculitis 362.03 17.66 574 95006 167079 110326640
Muscle injury 346.13 17.66 512 95068 140295 110353424
Irritable bowel syndrome 315.00 17.66 533 95047 163682 110330037
Helicobacter infection 309.51 17.66 560 95020 181317 110312402
Stomatitis 307.46 17.66 704 94876 269538 110224181
Impaired healing 303.86 17.66 581 94999 196136 110297583
Ill-defined disorder 296.73 17.66 506 95074 156347 110337372
Fall 290.74 17.66 81 95499 603401 109890318
Toxicity to various agents 280.13 17.66 41 95539 480514 110013205
Duodenal ulcer perforation 277.09 17.66 527 95053 177173 110316546
Porphyria acute 271.87 17.66 181 95399 18599 110475120
Hand deformity 258.21 17.66 578 95002 217928 110275791
Glossodynia 250.93 17.66 577 95003 221427 110272292
X-ray abnormal 248.16 17.66 229 95351 37888 110455831
Gastrointestinal disorder 246.59 17.66 604 94976 241348 110252371
Hypersensitivity 242.55 17.66 834 94746 403164 110090555
Facet joint syndrome 233.43 17.66 349 95231 96479 110397240
Lupus vulgaris 231.20 17.66 209 95371 33674 110460045
Lip dry 202.70 17.66 333 95247 99750 110393969
Liver disorder 194.07 17.66 399 95181 141844 110351875
Joint range of motion decreased 188.19 17.66 360 95220 121472 110372247
Product dose omission issue 186.16 17.66 28 95552 321754 110171965
Dislocation of vertebra 184.70 17.66 208 95372 43513 110450206
Deep vein thrombosis postoperative 183.55 17.66 241 95339 59050 110434669
Retinitis 183.39 17.66 180 95400 32147 110461572
Lower respiratory tract infection 183.26 17.66 543 95037 242563 110251156
Bone erosion 181.38 17.66 212 95368 46159 110447560
Sleep disorder 177.50 17.66 472 95108 198172 110295547
Anti-cyclic citrullinated peptide antibody positive 175.53 17.66 445 95135 181539 110312180
Feeling hot 174.95 17.66 296 95284 90810 110402909
Grip strength 174.59 17.66 105 95475 9036 110484683
Lower limb fracture 173.66 17.66 266 95314 75082 110418637
Adjustment disorder with depressed mood 172.26 17.66 201 95379 43682 110450037
Infusion related reaction 170.84 17.66 717 94863 380445 110113274
C-reactive protein abnormal 167.80 17.66 356 95224 129339 110364380
Road traffic accident 166.66 17.66 318 95262 107080 110386639
Blister 163.93 17.66 500 95080 226876 110266843
Autoimmune disorder 163.50 17.66 240 95340 65243 110428476
Swollen joint count increased 160.89 17.66 272 95308 83389 110410330
Lupus-like syndrome 155.40 17.66 184 95396 40608 110453111
Injury 155.12 17.66 418 95162 176847 110316872
Rheumatoid factor positive 154.00 17.66 347 95233 131293 110362426
Sciatica 153.86 17.66 282 95298 92117 110401602
Contusion 153.37 17.66 497 95083 232864 110260855
Rheumatic fever 144.37 17.66 324 95256 122255 110371464
Systemic lupus erythematosus 143.73 17.66 515 95065 253823 110239896
Wound 136.14 17.66 479 95101 233958 110259761
Laryngitis 132.20 17.66 173 95407 42238 110451481
Discomfort 131.02 17.66 446 95134 214261 110279458
Medication error 129.14 17.66 283 95297 105083 110388636
Exostosis 128.81 17.66 178 95402 45778 110447941
Computerised tomogram thorax abnormal 128.78 17.66 58 95522 2737 110490982
Fibromyalgia 128.01 17.66 381 95199 170528 110323191
Breast cancer stage III 127.36 17.66 238 95342 78879 110414840
Pemphigus 126.82 17.66 441 95139 214129 110279590
Hepatic enzyme increased 125.00 17.66 579 95001 320313 110173406
Maternal exposure timing unspecified 124.80 17.66 120 95460 20893 110472826
Pericarditis 124.05 17.66 444 95136 218670 110275049
Alopecia 123.35 17.66 632 94948 364121 110129598
Death 122.13 17.66 264 95316 698605 109795114
Pregnancy 118.67 17.66 181 95399 50886 110442833
Bursitis 117.30 17.66 310 95270 129608 110364111
Swollen joint count 116.93 17.66 80 95500 8594 110485125
Sinusitis 114.56 17.66 534 95046 296154 110197565
Synovitis 113.77 17.66 504 95076 273588 110220131
Decreased appetite 110.09 17.66 746 94834 475100 110018619
Infection 109.78 17.66 609 94971 361591 110132128
Overdose 109.42 17.66 33 95547 233761 110259958
Frequent bowel movements 109.03 17.66 210 95370 71180 110422539
Computerised tomogram thorax 108.86 17.66 33 95547 493 110493226
Neutrophil count decreased 108.60 17.66 288 95292 120653 110373066
Anti-cyclic citrullinated peptide antibody 103.73 17.66 106 95474 19858 110473861
Wound infection 103.69 17.66 246 95334 96219 110397500
C-reactive protein 101.24 17.66 128 95452 30203 110463516
Aplasia 99.99 17.66 70 95510 7803 110485916
Night sweats 95.89 17.66 294 95286 133689 110360030
Cardiac failure congestive 94.89 17.66 10 95570 150990 110342729
Hiccups 90.97 17.66 81 95499 12788 110480931
Myocardial infarction 90.08 17.66 27 95553 192056 110301663
Febrile bone marrow aplasia 89.41 17.66 92 95488 17373 110476346
Pyrexia 89.13 17.66 1175 94405 897090 109596629
Blood pressure increased 88.62 17.66 57 95523 258316 110235403
Peripheral venous disease 87.69 17.66 212 95368 83905 110409814
Somnolence 87.42 17.66 77 95503 297372 110196347
Drug tolerance decreased 85.30 17.66 112 95468 27428 110466291
Injection site pain 83.45 17.66 25 95555 177897 110315822
Hepatic cirrhosis 83.26 17.66 182 95398 67444 110426275
Type 2 diabetes mellitus 82.87 17.66 338 95242 176894 110316825
COVID-19 82.77 17.66 55 95525 245005 110248714
Insomnia 81.94 17.66 563 95017 360027 110133692
Lung disorder 80.75 17.66 339 95241 179708 110314011
Prescribed overdose 80.07 17.66 210 95370 87371 110406348
Influenza 78.87 17.66 24 95556 169077 110324642
Pulmonary fibrosis 78.77 17.66 230 95350 101812 110391907
Ear infection 77.42 17.66 169 95411 62563 110431156
Mucosal inflammation 77.40 17.66 220 95360 95921 110397798
Colitis ulcerative 76.42 17.66 191 95389 77172 110416547
Balance disorder 75.12 17.66 7 95573 116553 110377166
Foot deformity 73.27 17.66 142 95438 48338 110445381
Urinary tract infection 70.50 17.66 108 95472 326174 110167545
Encephalopathy 69.70 17.66 190 95390 80865 110412854
Swelling 68.76 17.66 529 95051 350512 110143207
Dry mouth 67.18 17.66 346 95234 199602 110294117
Chronic obstructive pulmonary disease 66.64 17.66 8 95572 109150 110384569
Hepatocellular injury 66.60 17.66 140 95440 50502 110443217
Prescribed underdose 66.58 17.66 163 95417 65011 110428708
Obesity 65.21 17.66 231 95349 113120 110380599
Suicidal ideation 65.18 17.66 4 95576 93933 110399786
Atelectasis 64.85 17.66 115 95465 36597 110457122
Pancreatitis 64.83 17.66 203 95377 93330 110400389
Nasal congestion 63.07 17.66 6 95574 98276 110395443
Arthropathy 62.39 17.66 444 95136 287078 110206641
Inflammation 61.89 17.66 330 95250 192908 110300811
Walking aid user 61.27 17.66 91 95489 24984 110468735
Injection site reaction 61.18 17.66 4 95576 89066 110404653
Weight fluctuation 60.89 17.66 85 95495 22060 110471659
Cerebrovascular accident 60.78 17.66 41 95539 181243 110312476
Laboratory test abnormal 58.13 17.66 122 95458 43957 110449762
Incorrect dose administered 57.68 17.66 10 95570 103631 110390088
Sense of oppression 56.83 17.66 28 95552 1620 110492099
Ulcer haemorrhage 56.72 17.66 83 95497 22488 110471231
Amnesia 56.55 17.66 210 95370 105198 110388521
Rhabdomyolysis 56.30 17.66 17 95563 120384 110373335
Nasopharyngitis 55.70 17.66 553 95027 393808 110099911
Erythema 55.28 17.66 436 95144 291011 110202708
Intentional product misuse 54.92 17.66 23 95557 132881 110360838
Flushing 54.81 17.66 207 95373 104529 110389190
Chronic kidney disease 53.69 17.66 3 95577 76288 110417431
Heart rate decreased 53.24 17.66 5 95575 82751 110410968
Hypoglycaemia 53.20 17.66 17 95563 116087 110377632
Grip strength decreased 52.82 17.66 171 95409 80003 110413716
General physical health deterioration 52.81 17.66 581 94999 424714 110069005
Illness 52.77 17.66 5 95575 82166 110411553
Myalgia 52.59 17.66 69 95511 222312 110271407
Musculoskeletal pain 52.24 17.66 303 95277 182720 110310999
Hyperkalaemia 52.22 17.66 26 95554 135770 110357949
Lactic acidosis 51.55 17.66 9 95571 92802 110400917
Blood glucose increased 51.51 17.66 25 95555 132471 110361248
Cardiac disorder 50.74 17.66 4 95576 76276 110417443
Wheezing 50.71 17.66 386 95194 254844 110238875
Psoriatic arthropathy 49.97 17.66 316 95264 196445 110297274
Cardiac arrest 49.73 17.66 58 95522 196695 110297024
Cognitive disorder 49.69 17.66 8 95572 87503 110406216
Wrong technique in product usage process 49.56 17.66 8 95572 87340 110406379
Herpes zoster 49.43 17.66 16 95564 108363 110385356
Delirium 49.11 17.66 239 95341 134786 110358933
Blood pressure systolic increased 48.46 17.66 7 95573 82984 110410735
Confusional state 48.37 17.66 618 94962 468062 110025657
Haemorrhage 48.22 17.66 16 95564 106676 110387043
Cardiac failure 47.75 17.66 55 95525 187571 110306148
Respiratory failure 47.73 17.66 70 95510 215262 110278457
Thrombocytopenia 47.69 17.66 486 95094 348399 110145320
Rectal haemorrhage 47.14 17.66 217 95363 119616 110374103
Influenza like illness 46.10 17.66 10 95570 88402 110405317
Pruritus 46.09 17.66 732 94848 580828 109912891
Anaphylactic shock 45.49 17.66 122 95458 51424 110442295
Nephrolithiasis 45.40 17.66 3 95577 66209 110427510
Sleep disorder due to a general medical condition 44.64 17.66 122 95458 51990 110441729
Cellulitis 44.29 17.66 27 95553 125989 110367730
Pulmonary oedema 43.93 17.66 16 95564 100643 110393076
Nausea 43.78 17.66 1386 94194 1234304 109259415
Rheumatoid arthritis 43.67 17.66 423 95157 299190 110194529
Vascular pain 43.66 17.66 21 95559 1152 110492567
Blood cholesterol increased 43.39 17.66 291 95289 184494 110309225
White blood cell count increased 43.12 17.66 182 95398 96660 110397059
Therapeutic product effect incomplete 42.87 17.66 80 95500 223725 110269994
Neuropathy peripheral 42.50 17.66 283 95297 178994 110314725
Osteoporosis 42.13 17.66 168 95412 86984 110406735
Neutropenia 42.09 17.66 502 95078 374118 110119601
Injection site swelling 41.78 17.66 3 95577 61787 110431932
Haemoglobin decreased 41.65 17.66 96 95484 248631 110245088
Cystitis haemorrhagic 41.50 17.66 52 95528 12157 110481562
Weight increased 41.46 17.66 549 95031 419095 110074624
Diabetes mellitus 41.38 17.66 17 95563 99364 110394355
Gastrooesophageal reflux disease 41.38 17.66 57 95523 179919 110313800
Paraesthesia 41.09 17.66 392 95188 276129 110217590
Abdominal distension 40.72 17.66 55 95525 175048 110318671
Tremor 39.88 17.66 71 95509 202161 110291558
Disturbance in attention 39.21 17.66 4 95576 61991 110431728
Bradycardia 39.13 17.66 46 95534 155471 110338248
Hypercholesterolaemia 39.12 17.66 169 95411 90668 110403051
Joint dislocation 38.70 17.66 89 95491 34101 110459618
Bone marrow failure 38.66 17.66 124 95456 57724 110435995
Gastrointestinal haemorrhage 38.47 17.66 52 95528 165466 110328253
Lymphadenopathy 38.18 17.66 5 95575 63830 110429889
Pneumonia 37.84 17.66 532 95048 876182 109617537
Liver injury 37.21 17.66 240 95340 150173 110343546
Full blood count abnormal 37.11 17.66 3 95577 56049 110437670
Neutropenic colitis 36.86 17.66 40 95540 8025 110485694
Heart rate increased 36.77 17.66 42 95538 143792 110349927
Hallucination 36.68 17.66 21 95559 101411 110392308
Pulmonary hypertension 36.44 17.66 3 95577 55217 110438502
Injection site erythema 36.26 17.66 18 95562 94158 110399561
Blood creatinine increased 36.25 17.66 64 95516 182825 110310894
Electrocardiogram QT prolonged 36.04 17.66 25 95555 108935 110384784
Agitation 36.01 17.66 27 95553 113024 110380695
Multiple organ dysfunction syndrome 35.94 17.66 47 95533 151663 110342056
Testicular germ cell cancer metastatic 35.71 17.66 9 95571 64 110493655
Pain 35.59 17.66 596 94984 954359 109539360
Mobility decreased 35.48 17.66 337 95243 237085 110256634
Therapy non-responder 34.72 17.66 244 95336 157063 110336656
Injection site vasculitis 34.70 17.66 7 95573 14 110493705
Rash maculo-papular 34.23 17.66 141 95439 74081 110419638
Blood pressure fluctuation 34.20 17.66 11 95569 74813 110418906
Hepatic cytolysis 34.09 17.66 115 95465 54938 110438781
Adverse event 33.59 17.66 184 95396 108625 110385094
Urticaria 33.52 17.66 422 95158 318435 110175284
Angioedema 33.38 17.66 22 95558 98478 110395241
Dyspnoea exertional 32.95 17.66 25 95555 104035 110389684
Infusion site streaking 32.89 17.66 14 95566 576 110493143
Nail bed inflammation 32.89 17.66 21 95559 2009 110491710
Oesophagitis 32.78 17.66 75 95505 28640 110465079
Interstitial lung disease 32.45 17.66 219 95361 139115 110354604
Hypotension 32.38 17.66 293 95287 523556 109970163
Sedation 32.28 17.66 10 95570 69673 110424046
Palpitations 32.20 17.66 55 95525 159157 110334562
Drug ineffective for unapproved indication 32.19 17.66 25 95555 102813 110390906
Depressed level of consciousness 31.85 17.66 30 95550 112248 110381471
Oedema 31.84 17.66 299 95281 209677 110284042
Nasal mucosal disorder 31.80 17.66 20 95560 1863 110491856
Orthostatic hypotension 31.62 17.66 9 95571 66240 110427479
Vomiting 31.52 17.66 1019 94561 909656 109584063
Alveolitis 31.49 17.66 28 95552 4411 110489308
Disease recurrence 31.44 17.66 7 95573 60777 110432942
Renal impairment 30.53 17.66 74 95506 188371 110305348
Unevaluable event 30.27 17.66 7 95573 59220 110434499
Drug resistance 30.17 17.66 6 95574 56368 110437351
Cholelithiasis 29.57 17.66 9 95571 63413 110430306
Chemotherapy 29.42 17.66 20 95560 2126 110491593
Hypervolaemia 29.28 17.66 4 95576 49456 110444263
Inappropriate schedule of product administration 29.18 17.66 85 95495 203552 110290167
Therapeutic product effect decreased 29.02 17.66 331 95249 243985 110249734
Hypoaesthesia 28.93 17.66 406 95174 313817 110179902
Inappropriate antidiuretic hormone secretion 28.74 17.66 79 95501 33772 110459947
Off label use 28.73 17.66 1035 94545 1499150 108994569
Cytomegalovirus infection 28.71 17.66 6 95574 54438 110439281
Renal failure 28.67 17.66 100 95480 226474 110267245
Condition aggravated 28.54 17.66 455 95125 734381 109759338
Psychotic disorder 28.16 17.66 5 95575 50932 110442787
Joint stiffness 28.11 17.66 124 95456 67119 110426600
Headache 28.06 17.66 566 95014 881811 109611908
Skin ulcer 27.97 17.66 10 95570 63635 110430084
Viral infection 27.72 17.66 6 95574 53133 110440586
Dry eye 27.72 17.66 7 95573 55786 110437933
Plasma cell myeloma 27.47 17.66 10 95570 62926 110430793
Therapy interrupted 27.30 17.66 5 95575 49817 110443902
Joint swelling 27.04 17.66 535 95045 442310 110051409
Vascular device infection 26.97 17.66 50 95530 16462 110477257
Feeling abnormal 26.94 17.66 74 95506 180637 110313082
Acute myocardial infarction 26.69 17.66 20 95560 83757 110409962
Head injury 26.63 17.66 3 95577 43014 110450705
Blood creatine phosphokinase increased 26.61 17.66 15 95565 73062 110420657
Aggression 26.54 17.66 9 95571 59201 110434518
Cystitis 26.37 17.66 12 95568 66024 110427695
Osteonecrosis of jaw 25.93 17.66 5 95575 48012 110445707
Respiratory arrest 25.89 17.66 9 95571 58290 110435429
Lip swelling 25.87 17.66 6 95574 50661 110443058
Drug reaction with eosinophilia and systemic symptoms 25.64 17.66 20 95560 82075 110411644
Psoriasis 25.10 17.66 52 95528 139941 110353778
Respiratory disorder 24.98 17.66 125 95455 71257 110422462
International normalised ratio increased 24.83 17.66 23 95557 86749 110406970
Vision blurred 24.80 17.66 46 95534 128976 110364743
Oral pain 24.78 17.66 80 95500 37364 110456355
Injection site phlebitis 24.60 17.66 8 95572 152 110493567
Loss of consciousness 24.59 17.66 87 95493 196219 110297500
Product prescribing error 24.45 17.66 7 95573 51324 110442395
Coeliac disease 24.40 17.66 4 95576 43183 110450536
Joint injury 24.24 17.66 3 95577 39991 110453728
Gait inability 24.19 17.66 201 95379 136175 110357544
Hip arthroplasty 24.15 17.66 104 95476 55709 110438010
Haemoptysis 24.09 17.66 16 95564 71338 110422381
Red blood cell sedimentation rate increased 23.88 17.66 132 95448 78170 110415549
Eye pain 23.55 17.66 7 95573 50092 110443627
Toxic encephalopathy 23.52 17.66 45 95535 15169 110478550
Abdominal discomfort 23.43 17.66 474 95106 393384 110100335
Seminoma 23.36 17.66 9 95571 285 110493434
Live birth 23.14 17.66 120 95460 69364 110424355
Accidental overdose 23.02 17.66 8 95572 51826 110441893
Streptococcal sepsis 22.91 17.66 25 95555 5047 110488672
Burning sensation 22.73 17.66 16 95564 69196 110424523
Colony stimulating factor therapy 22.41 17.66 11 95569 631 110493088
Change of bowel habit 22.17 17.66 19 95561 2850 110490869
Serotonin syndrome 21.74 17.66 12 95568 59141 110434578
Therapy cessation 21.58 17.66 6 95574 44851 110448868
Acute kidney injury 21.57 17.66 403 95177 635027 109858692
Bronchitis 21.45 17.66 67 95513 156965 110336754
Movement disorder 21.42 17.66 3 95577 36401 110457318
Melaena 21.16 17.66 17 95563 68740 110424979
Anaphylactic reaction 21.10 17.66 170 95410 114130 110379589
Mental disorder 21.03 17.66 4 95576 38787 110454932
Procedural pain 20.76 17.66 3 95577 35562 110458157
Enteritis 20.73 17.66 49 95531 19107 110474612
Haematochezia 20.64 17.66 43 95537 115481 110378238
Transposition of the great vessels 20.63 17.66 6 95574 77 110493642
Cataract 20.54 17.66 23 95557 79462 110414257
Hip fracture 20.44 17.66 3 95577 35148 110458571
Intestinal ischaemia 20.43 17.66 44 95536 16135 110477584
Blood pressure decreased 20.43 17.66 43 95537 115048 110378671
Ulcer 20.31 17.66 6 95574 43110 110450609
Cough 20.26 17.66 279 95301 461362 110032357
Liver function test abnormal 20.05 17.66 18 95562 68932 110424787
Sepsis 19.81 17.66 184 95396 327162 110166557
Tonsillar haemorrhage 19.75 17.66 8 95572 290 110493429
Syncope 19.65 17.66 99 95481 202437 110291282
Fluid retention 19.60 17.66 32 95548 94275 110399444
Faeces discoloured 19.50 17.66 3 95577 33945 110459774
Diplopia 19.43 17.66 6 95574 41888 110451831
Stoma site pain 19.39 17.66 15 95565 1948 110491771
Skin laceration 19.35 17.66 3 95577 33750 110459969
Speech disorder 19.23 17.66 15 95565 61554 110432165
Visual impairment 19.17 17.66 189 95391 134239 110359480
Eye irritation 19.12 17.66 3 95577 33449 110460270
Maternal exposure during pregnancy 19.08 17.66 318 95262 254565 110239154
Gastric disorder 19.05 17.66 3 95577 33354 110460365
Chest pain 18.87 17.66 442 95138 375933 110117786
Osteoarthritis 18.87 17.66 241 95339 182382 110311337
Finger deformity 18.84 17.66 3 95577 33089 110460630
Blood pressure diastolic decreased 18.83 17.66 4 95576 35881 110457838
Onychomycosis 18.83 17.66 5 95575 38526 110455193
Coagulopathy 18.72 17.66 6 95574 40905 110452814
Paronychia 18.66 17.66 34 95546 11047 110482672
Underdose 18.63 17.66 106 95474 63448 110430271
Hypokalaemia 18.53 17.66 240 95340 182208 110311511
Nodule 18.48 17.66 3 95577 32628 110461091
Staphylococcal infection 18.34 17.66 20 95560 69924 110423795
Hemianopia 18.21 17.66 17 95563 2851 110490868
Palmar-plantar erythrodysaesthesia syndrome 18.18 17.66 77 95503 40948 110452771
Fluid intake reduced 18.00 17.66 26 95554 6960 110486759
Neck pain 17.92 17.66 51 95529 123079 110370640
Acute polyneuropathy 17.79 17.66 10 95570 758 110492961
Oropharyngeal discomfort 17.79 17.66 32 95548 10295 110483424
Fungal infection 17.69 17.66 11 95569 50795 110442924
Rhinorrhoea 17.69 17.66 39 95541 102627 110391092

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 D005765 Gastrointestinal Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D064729 Neurokinin-1 Receptor Antagonists
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:22587 antiviral agent
CHEBI has role CHEBI:35469 antidepressant
CHEBI has role CHEBI:35480 analgesic
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:49110 peripheral nervous system drug
CHEBI has role CHEBI:50919 antiemetic
CHEBI has role CHEBI:55324 gastrointestinal drug
CHEBI has role CHEBI:55350 neurokinin-1 receptor antagonist
CHEBI has role CHEBI:55351 substance P receptor antagonist
CHEBI has role CHEBI:64946 anti-HIV agent

Related Drugs by ATC class:

A04AD Other antiemetics 8 drugs
casopitantcerium oxalatechlorobutanoldronabinolmetopimazinenabilonerolapitantscopolamine

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




🐶 Veterinary Drug Use

None

🐶 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 MSD N021549 March 26, 2003 RX CAPSULE ORAL 8258132 Sept. 26, 2027 FOR THE PREVENTION OF NAUSEA AND VOMITING ASSOCIATED WITH CHEMOTHERAPY
125MG EMEND MSD 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 MSD 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 MSD N021549 June 30, 2006 DISCN CAPSULE ORAL 8258132 Sept. 26, 2027 PREVENTION OF POSTOPERATIVE NAUSEA AND VOMITING
80MG EMEND MSD N021549 March 26, 2003 RX CAPSULE ORAL 8258132 Sept. 26, 2027 FOR THE PREVENTION OF NAUSEA AND VOMITING ASSOCIATED WITH CHEMOTHERAPY
80MG EMEND MSD 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
32MG/4.4ML (7.2MG/ML) APONVIE HERON THERAPS INC N216457 Sept. 16, 2022 RX EMULSION INTRAVENOUS 10624850 Sept. 18, 2035 A METHOD OF ADMINISTERING APREPITANT FOR PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING
32MG/4.4ML (7.2MG/ML) APONVIE HERON THERAPS INC N216457 Sept. 16, 2022 RX EMULSION INTRAVENOUS 10953018 Sept. 18, 2035 A METHOD OF ADMINISTERING APREPITANT FOR PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING
32MG/4.4ML (7.2MG/ML) APONVIE HERON THERAPS INC N216457 Sept. 16, 2022 RX EMULSION INTRAVENOUS 11744800 Sept. 18, 2035 A METHOD FOR PREVENTING OF POST-OPERATIVE NAUSEA AND VOMITING
32MG/4.4ML (7.2MG/ML) APONVIE HERON THERAPS INC N216457 Sept. 16, 2022 RX EMULSION INTRAVENOUS 11878074 Sept. 18, 2035 A METHOD FOR PREVENTING POST-OPERATIVE NAUSEA AND VOMITING
32MG/4.4ML (7.2MG/ML) APONVIE HERON THERAPS INC N216457 Sept. 16, 2022 RX EMULSION INTRAVENOUS 9561229 Sept. 18, 2035 A METHOD OF ADMINISTERING APREPITANT FOR PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING
32MG/4.4ML (7.2MG/ML) APONVIE HERON THERAPS INC N216457 Sept. 16, 2022 RX EMULSION INTRAVENOUS 9808465 Sept. 18, 2035 A METHOD OF ADMINISTERING APREPITANT FOR PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING
32MG/4.4ML (7.2MG/ML) APONVIE HERON THERAPS INC N216457 Sept. 16, 2022 RX EMULSION INTRAVENOUS 9974794 Sept. 18, 2035 A METHOD OF ADMINISTERING APREPITANT FOR PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING

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 IC50 7.70 CHEMBL
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
4021391 VANDF
009926 NDDF
398690007 SNOMEDCT_US
409205009 SNOMEDCT_US
1NF15YR6UY INXIGHT DRUGS

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 31 sections
APONVIE HUMAN PRESCRIPTION DRUG LABEL 1 47426-401 EMULSION 32 mg INTRAVENOUS NDA 29 sections
APREPITANT HUMAN PRESCRIPTION DRUG LABEL 1 51407-701 CAPSULE 40 mg ORAL ANDA 25 sections
APREPITANT HUMAN PRESCRIPTION DRUG LABEL 1 51407-701 CAPSULE 40 mg ORAL ANDA 25 sections
APREPITANT HUMAN PRESCRIPTION DRUG LABEL 1 51407-702 CAPSULE 80 mg ORAL ANDA 25 sections
APREPITANT HUMAN PRESCRIPTION DRUG LABEL 1 51407-702 CAPSULE 80 mg ORAL ANDA 25 sections
APREPITANT HUMAN PRESCRIPTION DRUG LABEL 1 51407-703 CAPSULE 125 mg ORAL ANDA 25 sections
APREPITANT HUMAN PRESCRIPTION DRUG LABEL 1 51407-703 CAPSULE 125 mg ORAL ANDA 25 sections
EMEND HUMAN PRESCRIPTION DRUG LABEL 1 54868-5231 CAPSULE 80 mg ORAL NDA 26 sections
Aprepitant HUMAN PRESCRIPTION DRUG LABEL 1 68001-666 CAPSULE 40 mg ORAL ANDA 25 sections
Aprepitant HUMAN PRESCRIPTION DRUG LABEL 1 68001-667 CAPSULE 80 mg ORAL ANDA 25 sections
Aprepitant HUMAN PRESCRIPTION DRUG LABEL 1 68001-668 CAPSULE 125 mg ORAL ANDA 25 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