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

Stem definitionDrug idCAS RN
estrogen antagonists, including estrogen receptor down-regulators 1255 129453-61-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ZD9238
  • fulvestrant
  • faslodex
  • ICI 182,780
An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer.
  • Molecular weight: 606.78
  • Formula: C32H47F5O3S
  • CLOGP: 7.54
  • LIPINSKI: 2
  • HAC: 3
  • HDO: 2
  • TPSA: 57.53
  • ALOGS: -4.96
  • ROTB: 15

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
8.30 mg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.00 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0.10 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.00 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 4.15 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 11.80 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.01 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 16 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
March 10, 2004 EMA
April 25, 2002 FDA ASTRAZENECA

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
Malignant neoplasm progression 4083.97 15.02 1860 60472 80261 63346429
Metastases to bone 2757.91 15.02 961 61371 20058 63406632
Neoplasm progression 2566.44 15.02 1057 61275 35371 63391319
Metastases to liver 2242.95 15.02 851 61481 22788 63403902
Neutropenia 1377.90 15.02 1233 61099 173772 63252918
White blood cell count decreased 872.56 15.02 865 61467 138239 63288451
Tumour marker increased 762.01 15.02 255 62077 4660 63422030
Metastases to lung 694.94 15.02 309 62023 12441 63414249
Osteonecrosis of jaw 550.56 15.02 373 61959 34750 63391940
Disease progression 522.97 15.02 623 61709 122135 63304555
Breast cancer metastatic 513.42 15.02 246 62086 11772 63414918
Neutrophil count decreased 445.26 15.02 399 61933 56007 63370683
Metastases to lymph nodes 407.26 15.02 186 62146 7972 63418718
Carbohydrate antigen 15-3 increased 396.14 15.02 116 62216 1332 63425358
PIK3CA-activated mutation 362.32 15.02 101 62231 958 63425732
Drug ineffective 346.54 15.02 312 62020 1044453 62382237
Fatigue 318.82 15.02 1709 60623 886319 62540371
Metastasis 305.90 15.02 133 62199 5064 63421626
Metastases to pleura 284.95 15.02 92 62240 1493 63425197
Leukopenia 264.62 15.02 352 61980 76938 63349752
Death 255.32 15.02 877 61455 373504 63053186
Bone pain 248.41 15.02 287 62045 54354 63372336
Metastases to spine 234.08 15.02 96 62236 3153 63423537
Breast cancer recurrent 216.73 15.02 99 62233 4242 63422448
Metastases to skin 213.72 15.02 75 62257 1588 63425102
Breast cancer 211.35 15.02 249 62083 48134 63378556
Thrombocytopenia 209.58 15.02 460 61872 150697 63275993
Infusion related reaction 206.24 15.02 8 62324 245513 63181177
Joint swelling 201.05 15.02 39 62293 327627 63099063
Maternal exposure during pregnancy 200.59 15.02 3 62329 220059 63206631
Rheumatoid arthritis 198.25 15.02 13 62319 253806 63172884
Bone lesion 193.89 15.02 101 62231 5780 63420910
Pleural effusion 187.82 15.02 332 62000 92878 63333812
Hyperglycaemia 185.40 15.02 217 62115 41650 63385040
Metastases to central nervous system 183.66 15.02 130 62202 12975 63413715
Systemic lupus erythematosus 178.24 15.02 6 62326 208912 63217778
Hepatic lesion 176.85 15.02 89 62243 4736 63421954
Therapeutic product effect decreased 174.51 15.02 3 62329 193184 63233506
Pseudocirrhosis 168.86 15.02 51 62281 656 63426034
Ascites 168.64 15.02 204 62128 40524 63386166
Palmar-plantar erythrodysaesthesia syndrome 166.22 15.02 155 62177 22860 63403830
Arthropathy 154.85 15.02 23 62309 234769 63191921
Asthenia 144.38 15.02 750 61582 382854 63043836
Hot flush 143.73 15.02 212 62120 50947 63375743
Metastases to peritoneum 139.54 15.02 68 62264 3374 63423316
Decreased appetite 135.46 15.02 546 61786 250506 63176184
Anaemia 135.04 15.02 608 61724 292822 63133868
Full blood count abnormal 133.15 15.02 160 62172 31557 63395133
Red blood cell count decreased 128.22 15.02 178 62154 40467 63386223
Drug hypersensitivity 126.65 15.02 74 62258 310613 63116077
Glossodynia 121.49 15.02 16 62316 178860 63247830
Platelet count decreased 118.46 15.02 314 62018 115808 63310882
Osteonecrosis 115.05 15.02 131 62201 24399 63402291
Pericarditis 115.02 15.02 3 62329 131576 63295114
Treatment failure 107.56 15.02 31 62301 199012 63227678
Second primary malignancy 107.07 15.02 77 62255 7876 63418814
Carcinoembryonic antigen increased 103.31 15.02 45 62287 1720 63424970
Musculoskeletal stiffness 95.69 15.02 31 62301 184587 63242103
Intentional product use issue 95.65 15.02 8 62324 127884 63298806
Hepatic failure 94.76 15.02 144 62188 35512 63391178
Nausea 92.88 15.02 1260 61072 853211 62573479
Neuropathy peripheral 91.25 15.02 282 62050 113385 63313305
Off label use 91.09 15.02 348 61984 674114 62752576
Mucosal inflammation 89.14 15.02 163 62169 46765 63379925
Hypotension 87.74 15.02 83 62249 272521 63154169
Malignant pleural effusion 86.60 15.02 45 62287 2561 63424129
Infusion site coldness 85.00 15.02 23 62309 193 63426497
Swelling 82.74 15.02 89 62243 275289 63151401
Wound 81.85 15.02 29 62303 163234 63263456
Polyneuropathy 78.95 15.02 84 62248 14505 63412185
Bone marrow failure 78.83 15.02 119 62213 29171 63397519
Helicobacter infection 77.92 15.02 3 62329 92782 63333908
Metastases to chest wall 77.18 15.02 27 62305 566 63426124
Gamma-glutamyltransferase decreased 76.07 15.02 23 62309 297 63426393
Cancer pain 75.23 15.02 44 62288 3161 63423529
Condition aggravated 74.64 15.02 179 62153 402038 63024652
Full blood count decreased 73.29 15.02 108 62224 25916 63400774
Bone disorder 72.70 15.02 97 62235 21229 63405461
Discomfort 72.29 15.02 37 62295 167337 63259353
Tumour marker abnormal 71.76 15.02 23 62309 364 63426326
Diarrhoea 71.14 15.02 1039 61293 714327 62712363
Lymphangiosis carcinomatosa 69.14 15.02 32 62300 1413 63425277
Abdominal lymphadenopathy 67.58 15.02 26 62306 719 63425971
Haematotoxicity 67.40 15.02 63 62269 9313 63417377
Metastases to pelvis 67.32 15.02 23 62309 448 63426242
Spinal pain 66.46 15.02 73 62259 13066 63413624
Fall 66.32 15.02 183 62149 392151 63034539
Lymphoedema 66.26 15.02 69 62263 11623 63415067
Overdose 65.78 15.02 16 62316 115062 63311628
Bone sequestrum 65.45 15.02 31 62301 1443 63425247
Asthma 65.06 15.02 22 62310 127539 63299151
Injection site necrosis 65.04 15.02 30 62302 1314 63425376
Skin toxicity 64.28 15.02 46 62286 4668 63422022
Sinusitis 63.98 15.02 77 62255 226576 63200114
Myelosuppression 61.95 15.02 95 62237 23608 63403082
Metastases to spinal cord 61.07 15.02 16 62316 117 63426573
Pleural neoplasm 60.48 15.02 20 62312 351 63426339
Invasive ductal breast carcinoma 60.39 15.02 52 62280 6906 63419784
Fibromyalgia 60.20 15.02 5 62327 80415 63346275
Mobility decreased 59.90 15.02 22 62310 121137 63305553
Hypersensitivity 59.35 15.02 124 62208 292561 63134129
Stomatitis 58.88 15.02 281 62051 138444 63288246
Pneumonia 57.51 15.02 242 62090 456525 62970165
Intentional overdose 57.23 15.02 4 62328 74148 63352542
Oestradiol increased 55.96 15.02 14 62318 83 63426607
Osteolysis 55.96 15.02 35 62297 2839 63423851
Metastases to thorax 55.56 15.02 17 62315 229 63426461
Metastases to adrenals 53.06 15.02 22 62310 743 63425947
Metastases to the mediastinum 51.41 15.02 19 62313 469 63426221
Lymphadenopathy 50.89 15.02 115 62217 38343 63388347
Back pain 50.62 15.02 437 61895 263708 63162982
Toxicity to various agents 49.90 15.02 105 62227 247145 63179545
Drug intolerance 49.89 15.02 147 62185 308514 63118176
Cough 49.83 15.02 472 61860 292271 63134419
Metastatic neoplasm 49.77 15.02 38 62294 4257 63422433
Oral pain 49.39 15.02 95 62237 28299 63398391
Interstitial lung disease 49.10 15.02 153 62179 61755 63364935
Lower respiratory tract infection 49.07 15.02 35 62297 132272 63294418
Metastases to retroperitoneum 48.68 15.02 14 62318 150 63426540
Confusional state 48.03 15.02 100 62232 236280 63190410
Portal hypertension 46.94 15.02 35 62297 3784 63422906
Abdominal discomfort 46.83 15.02 160 62172 320725 63105965
Invasive lobular breast carcinoma 46.53 15.02 21 62311 874 63425816
Adverse event 45.94 15.02 6 62326 67553 63359137
Electrocardiogram PR shortened 45.11 15.02 15 62317 268 63426422
Tooth extraction 45.07 15.02 53 62279 10211 63416479
Adnexa uteri mass 44.95 15.02 18 62314 555 63426135
Taste disorder 44.83 15.02 61 62271 13601 63413089
Bradycardia 44.22 15.02 9 62323 73218 63353472
Pneumonitis 44.04 15.02 103 62229 35119 63391571
Drug interaction 44.01 15.02 100 62232 229031 63197659
Therapeutic product effect incomplete 43.91 15.02 35 62297 125021 63301669
Adverse drug reaction 43.80 15.02 12 62320 79702 63346988
Acute kidney injury 43.61 15.02 124 62208 263291 63163399
Isosthenuria 43.60 15.02 12 62320 108 63426582
Infusion site induration 43.20 15.02 22 62310 1200 63425490
Eastern Cooperative Oncology Group performance status worsened 42.66 15.02 22 62310 1232 63425458
Psoriasis 42.62 15.02 16 62316 86941 63339749
Nasopharyngitis 42.60 15.02 119 62213 254138 63172552
Hormone receptor positive breast cancer 42.36 15.02 17 62315 527 63426163
Blister 42.33 15.02 39 62293 129775 63296915
Epistaxis 42.19 15.02 162 62170 72563 63354127
General physical health deterioration 41.64 15.02 339 61993 201063 63225627
Recurrent cancer 40.72 15.02 25 62307 1962 63424728
Carbohydrate antigen 27.29 increased 40.61 15.02 10 62322 55 63426635
Suicide attempt 40.04 15.02 6 62326 60912 63365778
Metastases to eye 39.90 15.02 12 62320 152 63426538
Bone cancer metastatic 39.54 15.02 12 62320 157 63426533
Bladder hypertrophy 39.37 15.02 13 62319 227 63426463
Haemoglobin decreased 39.29 15.02 261 62071 145224 63281466
Metastases to meninges 39.22 15.02 27 62305 2575 63424115
Aspartate aminotransferase increased 38.38 15.02 183 62149 90094 63336596
Hepatic enzyme increased 38.28 15.02 89 62243 202239 63224451
Arthritis 37.59 15.02 35 62297 115886 63310804
Neoplasm 37.48 15.02 41 62291 7304 63419386
Blood bilirubin increased 37.38 15.02 100 62232 37040 63389650
Hypermetabolism 37.03 15.02 12 62320 197 63426493
Suicidal ideation 37.02 15.02 8 62324 62413 63364277
Cardio-respiratory arrest 36.98 15.02 7 62325 59952 63366738
Headache 36.91 15.02 421 61911 632820 62793870
Tumour flare 36.84 15.02 14 62318 374 63426316
Ejection fraction decreased 36.75 15.02 73 62259 22259 63404431
Hepatic function abnormal 36.37 15.02 99 62233 37043 63389647
Pyelitis 36.32 15.02 12 62320 210 63426480
Constipation 35.94 15.02 358 61974 224585 63202105
Bone marrow infiltration 35.41 15.02 16 62316 668 63426022
Ill-defined disorder 35.39 15.02 18 62314 81737 63344953
Hospitalisation 34.97 15.02 20 62312 85061 63341629
Post-traumatic neck syndrome 34.80 15.02 23 62309 2051 63424639
Jaw disorder 34.77 15.02 34 62298 5315 63421375
Superinfection 34.54 15.02 25 62307 2582 63424108
Metastases to bone marrow 34.47 15.02 14 62318 448 63426242
Tumour marker decreased 34.33 15.02 9 62323 66 63426624
Weight increased 34.11 15.02 136 62196 260656 63166034
Hypertransaminasaemia 33.91 15.02 37 62295 6572 63420118
Loss of consciousness 33.44 15.02 40 62292 118081 63308609
Drug resistance 33.08 15.02 71 62261 22862 63403828
Alopecia 32.85 15.02 489 61843 337047 63089643
Jaundice 32.78 15.02 82 62250 29169 63397521
Gastrointestinal disorder 32.53 15.02 49 62283 131190 63295500
Metastases to kidney 32.50 15.02 11 62321 208 63426482
Onychoclasis 32.21 15.02 35 62297 6187 63420503
Oxygen saturation decreased 32.10 15.02 24 62308 88561 63338129
Bone marrow disorder 31.64 15.02 23 62309 2391 63424299
Dry skin 31.59 15.02 125 62207 56762 63369928
BRAF gene mutation 31.35 15.02 8 62324 52 63426638
Nephroangiosclerosis 31.33 15.02 10 62322 156 63426534
Transaminases increased 31.11 15.02 84 62248 31283 63395407
Hepatic echinococciasis 30.84 15.02 8 62324 56 63426634
Hip arthroplasty 30.61 15.02 5 62327 47641 63379049
Prehypertension 30.25 15.02 7 62325 28 63426662
Creatinine renal clearance increased 30.10 15.02 14 62318 625 63426065
Metastases to soft tissue 30.06 15.02 10 62322 179 63426511
Acquired gene mutation 29.90 15.02 16 62316 967 63425723
Neoplasm recurrence 29.82 15.02 23 62309 2615 63424075
Hepatic cancer metastatic 29.60 15.02 12 62320 382 63426308
Vasodilatation 29.55 15.02 22 62310 2373 63424317
Blood bilirubin abnormal 29.54 15.02 16 62316 991 63425699
Tachycardia 29.39 15.02 44 62288 118112 63308578
Injury 29.00 15.02 18 62314 73229 63353461
Dysgeusia 28.70 15.02 106 62226 46604 63380086
Loss of personal independence in daily activities 28.56 15.02 32 62300 97258 63329432
Metastases to bladder 28.48 15.02 10 62322 212 63426478
Dyspnoea exertional 28.41 15.02 126 62206 60176 63366514
Blood creatinine increased 28.34 15.02 165 62167 87679 63339011
Cytopenia 28.23 15.02 45 62287 11556 63415134
Pulmonary mass 28.16 15.02 66 62266 22530 63404160
Decreased immune responsiveness 27.91 15.02 29 62303 4872 63421818
Seizure 27.86 15.02 55 62277 132579 63294111
Pain in jaw 27.82 15.02 100 62232 43396 63383294
Exposed bone in jaw 27.73 15.02 23 62309 2902 63423788
Cardiac arrest 27.65 15.02 30 62302 92515 63334175
Inappropriate schedule of product administration 27.56 15.02 37 62295 103928 63322762
Wheezing 27.45 15.02 32 62300 95563 63331127
Osteomyelitis 27.14 15.02 71 62261 25949 63400741
Blood pressure increased 27.01 15.02 76 62256 161986 63264704
Product use issue 26.96 15.02 118 62214 220402 63206288
Mouth swelling 26.91 15.02 28 62304 4712 63421978
Pathological fracture 26.82 15.02 38 62294 8796 63417894
Tremor 26.78 15.02 56 62276 132183 63294507
Oestrogen receptor assay positive 26.58 15.02 12 62320 500 63426190
Pustule 26.49 15.02 18 62314 1681 63425009
Pulmonary tumour thrombotic microangiopathy 26.39 15.02 7 62325 54 63426636
Osteosclerosis 25.81 15.02 25 62307 3863 63422827
Musculoskeletal chest pain 25.64 15.02 61 62271 21022 63405668
Malignant peritoneal neoplasm 25.61 15.02 13 62319 704 63425986
International normalised ratio increased 25.48 15.02 7 62325 46418 63380272
Hydronephrosis 25.45 15.02 41 62291 10621 63416069
Joint neoplasm 25.43 15.02 7 62325 63 63426627
Lacrimation increased 25.42 15.02 60 62272 20571 63406119
Cardiac failure congestive 25.42 15.02 32 62300 92401 63334289
Ovarian disorder 25.39 15.02 13 62319 717 63425973
Osteoarthritis 25.20 15.02 34 62298 95309 63331381
Metastases to nervous system 25.05 15.02 7 62325 67 63426623
Hepatic cyst 24.97 15.02 28 62304 5126 63421564
Type 2 diabetes mellitus 24.87 15.02 16 62316 63852 63362838
Hypoglycaemia 24.86 15.02 14 62318 60051 63366639
Retinal detachment 24.86 15.02 30 62302 5939 63420751
Soft tissue neoplasm 24.60 15.02 7 62325 72 63426618
Spinal cord compression 24.44 15.02 25 62307 4123 63422567
Granulocytopenia 24.43 15.02 29 62303 5643 63421047
Bone cancer 24.22 15.02 16 62316 1426 63425264
Carcinoid tumour pulmonary 24.17 15.02 11 62321 467 63426223
RET gene mutation 24.15 15.02 5 62327 10 63426680
Urticaria 23.93 15.02 83 62249 165719 63260971
Bone debridement 23.84 15.02 9 62323 236 63426454
Vulvovaginal dryness 23.81 15.02 21 62311 2880 63423810
White blood cell count abnormal 23.78 15.02 30 62302 6212 63420478
Injection site hypoaesthesia 23.76 15.02 11 62321 486 63426204
Bile duct stenosis 23.71 15.02 15 62317 1241 63425449
Peritoneal disorder 23.65 15.02 11 62321 491 63426199
Bronchitis 23.58 15.02 55 62277 124880 63301810
Intestinal metastasis 23.55 15.02 8 62324 153 63426537
Transaminases 23.54 15.02 7 62325 85 63426605
Mediastinal disorder 23.49 15.02 10 62322 361 63426329
Blood cholesterol increased 23.40 15.02 35 62297 93997 63332693
Pulmonary embolism 23.33 15.02 195 62137 116489 63310201
Vein disorder 23.33 15.02 27 62305 5114 63421576
Peripheral swelling 23.32 15.02 159 62173 265783 63160907
Agitation 23.23 15.02 15 62317 59742 63366948
Nail disorder 23.19 15.02 44 62288 12971 63413719
Body surface area increased 23.13 15.02 6 62326 42 63426648
Hyponatraemia 22.99 15.02 47 62285 111853 63314837
Metabolic acidosis 22.58 15.02 8 62324 45061 63381629
Plasma cell myeloma 22.55 15.02 4 62328 35901 63390789
Erysipelas 22.53 15.02 33 62299 7872 63418818
Oral disorder 22.45 15.02 35 62297 8819 63417871
Hyperchromic anaemia 22.43 15.02 6 62326 48 63426642
Somnolence 22.21 15.02 95 62237 178590 63248100
Gene mutation 22.14 15.02 16 62316 1649 63425041
COVID-19 22.08 15.02 188 62144 112915 63313775
Influenza 22.05 15.02 46 62286 108676 63318014
Blood pressure fluctuation 21.91 15.02 9 62323 46308 63380382
Fluid retention 21.84 15.02 16 62316 59670 63367020
Metastases to breast 21.84 15.02 9 62323 299 63426391
Oestradiol abnormal 21.80 15.02 6 62326 54 63426636
Feeling cold 21.74 15.02 62 62270 23826 63402864
Red blood cell sedimentation rate increased 21.70 15.02 8 62324 43974 63382716
Heart rate increased 21.63 15.02 37 62295 94201 63332489
Dyskinesia 21.38 15.02 3 62329 31999 63394691
Platelet count abnormal 21.15 15.02 21 62311 3343 63423347
Hepatotoxicity 21.06 15.02 82 62250 36959 63389731
Hallucination 20.98 15.02 14 62318 54803 63371887
Drug ineffective for unapproved indication 20.96 15.02 4 62328 34059 63392631
Pancreatitis 20.93 15.02 11 62321 49044 63377646
Gingivitis 20.93 15.02 33 62299 8396 63418294
Gamma-glutamyltransferase increased 20.72 15.02 77 62255 33954 63392736
Orthostatic hypotension 20.71 15.02 5 62327 36155 63390535
Elliptocytosis 20.64 15.02 6 62326 67 63426623
Septic shock 20.57 15.02 21 62311 66608 63360082
Medication error 20.49 15.02 13 62319 52271 63374419
Gastrointestinal haemorrhage 20.41 15.02 30 62302 81146 63345544
Skin sensitisation 20.33 15.02 12 62320 877 63425813
Weight decreased 20.28 15.02 383 61949 276415 63150275
Malignant ascites 20.12 15.02 12 62320 894 63425796
Cytogenetic analysis abnormal 19.94 15.02 12 62320 908 63425782
Sepsis 19.91 15.02 80 62252 153043 63273647
Mean cell haemoglobin decreased 19.90 15.02 25 62307 5154 63421536
Breast pain 19.88 15.02 33 62299 8765 63417925
Treatment noncompliance 19.80 15.02 6 62326 37319 63389371
Gingival swelling 19.71 15.02 23 62309 4395 63422295
Breast cancer stage IV 19.63 15.02 16 62316 1970 63424720
Gingival erythema 19.56 15.02 11 62321 733 63425957
Joint range of motion decreased 19.55 15.02 4 62328 32424 63394266
Prescribed underdose 19.33 15.02 3 62329 29686 63397004
Infection 19.11 15.02 139 62193 229034 63197656
Coma 19.07 15.02 21 62311 64343 63362347
Metastases to uterus 19.02 15.02 6 62326 90 63426600
BRCA2 gene mutation 18.89 15.02 6 62326 92 63426598
Aphthous ulcer 18.79 15.02 42 62290 13896 63412794
Generalised tonic-clonic seizure 18.74 15.02 3 62329 29013 63397677
Product quality issue 18.60 15.02 6 62326 35859 63390831
Uterine mass 18.53 15.02 8 62324 299 63426391
Metastases to ovary 18.42 15.02 9 62323 449 63426241
Nail avulsion 18.32 15.02 7 62325 190 63426500
Pleural disorder 18.20 15.02 10 62322 637 63426053
Hormone refractory breast cancer 18.18 15.02 4 62328 12 63426678
Transaminases abnormal 17.93 15.02 10 62322 656 63426034
Intentional product misuse 17.91 15.02 20 62312 60897 63365793
Product use in unapproved indication 17.78 15.02 103 62229 178977 63247713
Foot deformity 17.72 15.02 3 62329 27850 63398840
Overflow diarrhoea 17.60 15.02 6 62326 116 63426574
Depressed level of consciousness 17.58 15.02 21 62311 62057 63364633
Pain 17.58 15.02 574 61758 740054 62686636
Glomerular filtration rate decreased 17.56 15.02 40 62292 13401 63413289
Pneumonia aspiration 17.53 15.02 6 62326 34534 63392156
Herpes zoster 17.48 15.02 34 62298 82428 63344262
Syncope 17.45 15.02 58 62274 117327 63309363
Angioedema 17.37 15.02 13 62319 47952 63378738
Pancytopenia 17.30 15.02 158 62174 96775 63329915
Blood creatinine abnormal 17.25 15.02 18 62314 3038 63423652
Ear infection 17.16 15.02 8 62324 38205 63388485
Drug reaction with eosinophilia and systemic symptoms 16.96 15.02 6 62326 33830 63392860
Unresponsive to stimuli 16.94 15.02 6 62326 33810 63392880
Debridement 16.87 15.02 12 62320 1206 63425484
Hyperkalaemia 16.83 15.02 17 62315 54186 63372504
Lymphadenopathy mediastinal 16.68 15.02 17 62315 2791 63423899
Laryngitis viral 16.65 15.02 5 62327 63 63426627
No adverse event 16.63 15.02 10 62322 41395 63385295
Injection site mass 16.57 15.02 48 62284 18608 63408082
Therapy partial responder 16.54 15.02 34 62298 10624 63416066
Myocardial infarction 16.52 15.02 47 62285 99846 63326844
Metastases to muscle 16.47 15.02 6 62326 142 63426548
Cachexia 16.46 15.02 24 62308 5702 63420988
Gingival pain 16.32 15.02 29 62303 8133 63418557
Gastrointestinal submucosal tumour 16.09 15.02 4 62328 23 63426667
Adenocarcinoma 15.98 15.02 17 62315 2933 63423757
Platelet disorder 15.98 15.02 14 62318 1902 63424788
Encephalopathy 15.98 15.02 9 62323 38611 63388079
Body surface area decreased 15.95 15.02 4 62328 24 63426666
Radiation fibrosis - lung 15.95 15.02 4 62328 24 63426666
Blood creatine phosphokinase increased 15.94 15.02 5 62327 30425 63396265
Sequestrectomy 15.93 15.02 10 62322 816 63425874
Excessive granulation tissue 15.86 15.02 10 62322 823 63425867
Mucinous breast carcinoma 15.81 15.02 4 62328 25 63426665
Infusion site haemorrhage 15.62 15.02 22 62310 5064 63421626
Blood creatinine decreased 15.59 15.02 23 62309 5522 63421168
Glycosylated haemoglobin 15.43 15.02 5 62327 82 63426608
Breast injury 15.32 15.02 5 62327 84 63426606
Aspartate aminotransferase abnormal 15.28 15.02 11 62321 1127 63425563
Incorrect dose administered 15.23 15.02 22 62310 59946 63366744
Invasive breast carcinoma 15.22 15.02 9 62323 660 63426030
Product dose omission in error 15.16 15.02 27 62305 7585 63419105
Tumour pain 15.10 15.02 12 62320 1425 63425265
Mean cell volume increased 15.04 15.02 18 62314 3533 63423157

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
Xerosis 53.10 49.57 9 521 595 34955806

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
Neoplasm progression 2136.84 15.34 898 48428 50784 79644278
Metastases to bone 1780.38 15.34 641 48685 23786 79671276
Malignant neoplasm progression 1776.11 15.34 1082 48244 134908 79560154
Metastases to liver 1317.99 15.34 536 48790 27778 79667284
Neutropenia 935.56 15.34 1014 48312 286696 79408366
White blood cell count decreased 919.66 15.34 829 48497 187459 79507603
Tumour marker increased 582.79 15.34 180 49146 4092 79690970
Fatigue 498.70 15.34 1476 47850 928251 78766811
Metastases to lung 479.13 15.34 231 49095 17932 79677130
Osteonecrosis of jaw 445.56 15.34 297 49029 42929 79652133
Breast cancer metastatic 366.44 15.34 153 49173 8449 79686613
Neutrophil count decreased 341.00 15.34 352 48974 93607 79601455
Carbohydrate antigen 15-3 increased 306.04 15.34 82 49244 1097 79693965
Metastases to lymph nodes 279.51 15.34 134 49192 10263 79684799
Disease progression 259.79 15.34 433 48893 183929 79511133
Bone pain 237.55 15.34 228 49098 55514 79639548
Breast cancer recurrent 201.22 15.34 74 49252 2903 79692159
Drug ineffective 196.22 15.34 229 49097 1080684 78614378
PIK3CA-activated mutation 195.31 15.34 50 49276 553 79694509
Pseudocirrhosis 184.58 15.34 49 49277 631 79694431
Bone lesion 173.55 15.34 81 49245 5838 79689224
Metastases to pleura 172.63 15.34 56 49270 1498 79693564
Alopecia 171.78 15.34 416 48910 230939 79464123
Breast cancer 170.69 15.34 152 49174 33629 79661433
Hot flush 161.17 15.34 184 49142 54693 79640369
Metastases to skin 158.57 15.34 54 49272 1685 79693377
Asthenia 155.58 15.34 677 48649 511012 79184050
Nausea 148.13 15.34 1054 48272 956142 78738920
Full blood count abnormal 141.96 15.34 149 49177 40325 79654737
Metastases to spine 141.92 15.34 64 49262 4260 79690802
Metastasis 138.79 15.34 73 49253 6807 79688255
Death 129.12 15.34 690 48636 565824 79129238
Leukopenia 127.16 15.34 245 49081 116268 79578794
Metastases to central nervous system 125.62 15.34 94 49232 16281 79678781
Decreased appetite 122.78 15.34 477 48849 341941 79353121
Red blood cell count decreased 119.32 15.34 162 49164 57351 79637711
Infusion related reaction 111.56 15.34 8 49318 230229 79464833
Thrombocytopenia 107.94 15.34 385 48941 264874 79430188
Hepatic lesion 102.42 15.34 60 49266 6899 79688163
Hypotension 99.75 15.34 76 49250 440241 79254821
Stomatitis 97.37 15.34 253 49073 146504 79548558
Acute kidney injury 97.10 15.34 107 49219 519297 79175765
Full blood count decreased 96.30 15.34 100 49226 26719 79668343
Platelet count decreased 95.52 15.34 301 49025 194363 79500699
Hyperglycaemia 93.32 15.34 161 49165 70174 79624888
Infusion site coldness 93.24 15.34 23 49303 216 79694846
Joint swelling 90.04 15.34 33 49293 288613 79406449
Carcinoembryonic antigen increased 89.75 15.34 38 49288 2171 79692891
Rheumatoid arthritis 88.59 15.34 12 49314 208458 79486604
Therapeutic product effect decreased 87.90 15.34 3 49323 163860 79531202
Off label use 84.53 15.34 284 49042 906931 78788131
Pleural effusion 83.91 15.34 238 49088 145024 79550038
Gamma-glutamyltransferase decreased 82.42 15.34 23 49303 361 79694701
Palmar-plantar erythrodysaesthesia syndrome 82.25 15.34 102 49224 33032 79662030
Second primary malignancy 79.37 15.34 68 49258 14282 79680780
Osteonecrosis 79.25 15.34 97 49229 30998 79664064
Spinal pain 77.22 15.34 69 49257 15323 79679739
Toxicity to various agents 75.31 15.34 90 49236 421450 79273612
Diarrhoea 74.86 15.34 852 48474 879637 78815425
Oral pain 74.34 15.34 95 49231 31703 79663359
Anaemia 73.02 15.34 498 48828 444517 79250545
Neuropathy peripheral 72.52 15.34 222 49104 141083 79553979
Drug interaction 71.68 15.34 91 49235 415092 79279970
Metastases to peritoneum 70.48 15.34 40 49286 4332 79690730
Pneumonia 70.46 15.34 194 49132 660052 79035010
Intentional product use issue 68.98 15.34 7 49319 152105 79542957
Overdose 68.63 15.34 15 49311 184191 79510871
Cancer pain 66.26 15.34 41 49285 5204 79689858
Ascites 64.87 15.34 144 49182 75418 79619644
Lymphangiosis carcinomatosa 64.77 15.34 30 49296 2124 79692938
Skin toxicity 64.38 15.34 48 49278 8266 79686796
Systemic lupus erythematosus 62.34 15.34 3 49323 121146 79573916
Injection site necrosis 61.96 15.34 26 49300 1452 79693610
Bone disorder 61.08 15.34 67 49259 19046 79676016
Tumour marker abnormal 60.33 15.34 17 49309 277 79694785
Adnexa uteri mass 59.69 15.34 18 49308 376 79694686
Bradycardia 59.53 15.34 7 49319 135550 79559512
Arthropathy 59.13 15.34 18 49308 177093 79517969
Drug hypersensitivity 58.66 15.34 59 49267 298857 79396205
Myelosuppression 58.43 15.34 96 49230 40200 79654862
Back pain 58.18 15.34 354 48972 303826 79391236
Cough 58.06 15.34 407 48919 366382 79328680
Lymphoedema 57.09 15.34 53 49273 12360 79682702
Infusion site induration 54.49 15.34 22 49304 1113 79693949
Metastases to pelvis 54.32 15.34 19 49307 643 79694419
Metastases to chest wall 53.94 15.34 18 49308 527 79694535
Bone marrow failure 53.92 15.34 106 49220 51001 79644061
Metastases to eye 52.80 15.34 15 49311 252 79694810
Pericarditis 52.31 15.34 3 49323 104233 79590829
Fall 51.41 15.34 144 49182 487485 79207577
Intentional overdose 50.40 15.34 4 49322 105956 79589106
Electrocardiogram PR shortened 50.35 15.34 15 49311 300 79694762
Mucosal inflammation 49.77 15.34 130 49196 75450 79619612
Sepsis 49.71 15.34 56 49270 269372 79425690
Isosthenuria 48.81 15.34 12 49314 111 79694951
Abdominal lymphadenopathy 47.80 15.34 21 49305 1313 79693749
Treatment failure 47.50 15.34 23 49303 170463 79524599
Tooth extraction 46.85 15.34 45 49281 10950 79684112
Cardiac arrest 46.77 15.34 24 49302 172072 79522990
Condition aggravated 46.41 15.34 157 49169 500967 79194095
Post-traumatic neck syndrome 44.47 15.34 23 49303 2071 79692991
Cardio-respiratory arrest 44.33 15.34 7 49319 108503 79586559
Hepatic failure 44.17 15.34 109 49217 61103 79633959
Lymphadenopathy 42.94 15.34 99 49227 53148 79641914
Metastases to retroperitoneum 42.61 15.34 14 49312 390 79694672
Confusional state 41.36 15.34 84 49242 317913 79377149
Asthma 41.16 15.34 16 49310 135079 79559983
Musculoskeletal stiffness 41.12 15.34 29 49297 174979 79520083
Carbohydrate antigen 27.29 increased 40.46 15.34 9 49317 51 79695011
Tumour marker decreased 40.31 15.34 9 49317 52 79695010
Pleural neoplasm 39.81 15.34 13 49313 355 79694707
Mobility decreased 39.73 15.34 13 49313 122162 79572900
Lacrimation increased 38.77 15.34 58 49268 22419 79672643
Metastases to breast 38.66 15.34 12 49314 277 79694785
Taste disorder 38.13 15.34 48 49278 15775 79679287
Constipation 37.89 15.34 302 49024 282748 79412314
Metastases to meninges 37.68 15.34 25 49301 3576 79691486
Hyperkalaemia 37.50 15.34 12 49314 114386 79580676
Pain in jaw 37.42 15.34 86 49240 46065 79648997
Dry skin 36.90 15.34 109 49217 67886 79627176
Loss of consciousness 36.68 15.34 30 49296 167913 79527149
Pyelitis 36.64 15.34 12 49314 331 79694731
Prehypertension 36.41 15.34 7 49319 16 79695046
Portal hypertension 35.92 15.34 32 49294 7076 79687986
International normalised ratio increased 35.68 15.34 5 49321 84716 79610346
Osteolysis 34.89 15.34 26 49300 4472 79690590
Hepatic echinococciasis 34.76 15.34 8 49318 54 79695008
Malignant pleural effusion 34.25 15.34 23 49303 3357 79691705
Metastases to thorax 33.71 15.34 10 49316 197 79694865
Metastases to the mediastinum 33.39 15.34 13 49313 597 79694465
Vasodilatation 33.02 15.34 22 49304 3169 79691893
Tachycardia 32.71 15.34 37 49289 177731 79517331
Haematotoxicity 32.60 15.34 44 49282 15475 79679587
Haemoglobin decreased 32.50 15.34 242 49084 221877 79473185
Suicide attempt 32.44 15.34 6 49320 82926 79612136
Ovarian disorder 32.42 15.34 12 49314 479 79694583
Bladder hypertrophy 32.42 15.34 13 49313 646 79694416
Ejection fraction decreased 32.07 15.34 68 49258 34509 79660553
Hormone receptor positive breast cancer 31.92 15.34 11 49315 356 79694706
Hypertransaminasaemia 31.68 15.34 38 49288 11886 79683176
Vein disorder 31.64 15.34 26 49300 5156 79689906
Hypermetabolism 31.60 15.34 11 49315 367 79694695
Creatinine renal clearance increased 31.51 15.34 14 49312 899 79694163
Gastrointestinal haemorrhage 31.50 15.34 27 49299 147692 79547370
Oxygen saturation decreased 30.82 15.34 21 49305 129026 79566036
Superinfection 30.78 15.34 25 49301 4877 79690185
Septic shock 30.66 15.34 19 49307 122782 79572280
Metastases to bladder 30.49 15.34 10 49316 277 79694785
Oestradiol increased 30.43 15.34 8 49318 99 79694963
Decreased immune responsiveness 30.39 15.34 26 49300 5449 79689613
Metastases to spinal cord 30.20 15.34 7 49319 49 79695013
Metabolic acidosis 30.16 15.34 7 49319 82522 79612540
Drug intolerance 30.06 15.34 75 49251 264044 79431018
Infusion site haemorrhage 29.97 15.34 22 49304 3698 79691364
Onychoclasis 29.97 15.34 26 49300 5552 79689510
Hypoglycaemia 29.38 15.34 13 49313 101581 79593481
Syncope 29.21 15.34 41 49285 179408 79515654
Joint neoplasm 28.64 15.34 7 49319 63 79694999
Hyponatraemia 28.59 15.34 41 49285 177807 79517255
Nephroangiosclerosis 28.57 15.34 10 49316 339 79694723
Dysgeusia 28.53 15.34 89 49237 57088 79637974
Breast pain 28.21 15.34 30 49296 8235 79686827
Mouth swelling 28.14 15.34 26 49300 6025 79689037
Invasive lobular breast carcinoma 28.12 15.34 12 49314 699 79694363
Myocardial infarction 28.10 15.34 44 49282 184085 79510977
Malignant peritoneal neoplasm 28.07 15.34 12 49314 702 79694360
Cardiac failure congestive 28.03 15.34 28 49298 142374 79552688
Seizure 27.99 15.34 46 49280 188788 79506274
Irritable bowel syndrome 27.86 15.34 3 49323 62238 79632824
Metastases to kidney 27.70 15.34 11 49315 533 79694529
Feeling cold 27.22 15.34 57 49269 28672 79666390
Agitation 26.94 15.34 14 49312 99701 79595361
Interstitial lung disease 26.75 15.34 139 49187 112461 79582601
Soft tissue neoplasm 26.74 15.34 7 49319 85 79694977
Fibromyalgia 26.62 15.34 4 49322 64336 79630726
Product dose omission in error 26.10 15.34 28 49298 7760 79687302
Pulmonary tumour thrombotic microangiopathy 26.03 15.34 7 49319 95 79694967
BRCA2 gene mutation 26.03 15.34 7 49319 95 79694967
Pustule 26.01 15.34 16 49310 2009 79693053
Atrial fibrillation 25.94 15.34 52 49274 197834 79497228
Neoplasm 25.79 15.34 30 49296 9086 79685976
Mean cell haemoglobin decreased 25.63 15.34 25 49301 6199 79688863
Exposed bone in jaw 25.55 15.34 20 49306 3700 79691362
Blood creatine phosphokinase increased 25.39 15.34 5 49321 66085 79628977
Pneumonitis 25.25 15.34 89 49237 60771 79634291
Suicidal ideation 25.03 15.34 8 49318 76332 79618730
Vulvovaginal dryness 24.64 15.34 16 49310 2208 79692854
Peritoneal disorder 24.50 15.34 11 49315 724 79694338
Osteosclerosis 24.40 15.34 20 49306 3951 79691111
Hospitalisation 24.34 15.34 14 49312 94222 79600840
Adverse event 24.33 15.34 4 49322 60210 79634852
Skin sensitisation 24.26 15.34 12 49314 983 79694079
Toothache 24.26 15.34 44 49282 19926 79675136
Recurrent cancer 24.16 15.34 17 49309 2676 79692386
Epistaxis 24.00 15.34 134 49192 111381 79583681
Nail avulsion 23.98 15.34 7 49319 130 79694932
Blood pressure fluctuation 23.94 15.34 6 49320 67139 79627923
Pneumonia aspiration 23.84 15.34 6 49320 66961 79628101
Psoriasis 23.58 15.34 13 49313 89574 79605488
Adverse drug reaction 23.54 15.34 6 49320 66386 79628676
Blood pressure increased 23.29 15.34 61 49265 211299 79483763
Hallucination 23.22 15.34 12 49314 85733 79609329
Metastases to soft tissue 23.17 15.34 10 49316 599 79694463
Angioedema 23.16 15.34 9 49317 76026 79619036
Osteomyelitis 23.15 15.34 58 49268 32807 79662255
Invasive ductal breast carcinoma 23.02 15.34 23 49303 5869 79689193
Metastases to uterus 22.99 15.34 6 49320 72 79694990
Transaminases 22.62 15.34 6 49320 77 79694985
Therapeutic product effect incomplete 22.42 15.34 33 49293 141612 79553450
Discomfort 22.19 15.34 27 49299 125590 79569472
Metastatic neoplasm 22.17 15.34 21 49305 5021 79690041
Tremor 22.03 15.34 45 49281 170038 79525024
Unresponsive to stimuli 21.90 15.34 4 49322 55784 79639278
Bone sequestrum 21.87 15.34 12 49314 1217 79693845
Oral disorder 21.78 15.34 29 49297 10066 79684996
Febrile neutropenia 21.59 15.34 72 49254 230927 79464135
Elliptocytosis 21.57 15.34 6 49320 93 79694969
Madarosis 21.30 15.34 16 49310 2786 79692276
Coronary artery disease 21.22 15.34 7 49319 65467 79629595
RET gene mutation 21.17 15.34 4 49322 8 79695054
Hypersensitivity 21.07 15.34 87 49239 262152 79432910
Metastases to ovary 20.94 15.34 8 49318 349 79694713
Pathological fracture 20.81 15.34 29 49297 10508 79684554
Coma 20.73 15.34 19 49307 100630 79594432
Glossodynia 20.70 15.34 20 49306 103317 79591745
Hepatic cyst 20.60 15.34 22 49304 6067 79688995
Plasma cell myeloma 20.52 15.34 4 49322 53255 79641807
Wound 20.49 15.34 25 49301 116154 79578908
Tooth disorder 20.30 15.34 48 49278 26185 79668877
Blood pressure systolic increased 20.29 15.34 8 49318 66978 79628084
Mental status changes 20.28 15.34 8 49318 66951 79628111
Aphthous ulcer 20.25 15.34 37 49289 16852 79678210
Depressed level of consciousness 20.20 15.34 18 49308 96634 79598428
Musculoskeletal chest pain 19.91 15.34 46 49280 24718 79670344
Transaminases abnormal 19.85 15.34 10 49316 852 79694210
Gingival pain 19.65 15.34 26 49300 8972 79686090
Nail disorder 19.61 15.34 30 49296 11822 79683240
Gingivitis 19.60 15.34 26 49300 8995 79686067
Hepatotoxicity 19.53 15.34 73 49253 51279 79643783
Pancreatitis 19.48 15.34 9 49317 68566 79626496
Drug ineffective for unapproved indication 19.42 15.34 4 49322 51234 79643828
Neoplasm recurrence 19.39 15.34 18 49308 4196 79690866
Inappropriate schedule of product administration 19.38 15.34 33 49293 133595 79561467
Respiratory failure 19.33 15.34 53 49273 180858 79514204
Injury 19.33 15.34 12 49314 77484 79617578
Swelling 19.27 15.34 69 49257 216642 79478420
Aspartate aminotransferase increased 19.11 15.34 149 49177 138492 79556570
Body surface area increased 19.07 15.34 6 49320 145 79694917
Bone debridement 19.06 15.34 8 49318 447 79694615
Dysarthria 19.01 15.34 9 49317 67613 79627449
Laryngitis viral 18.93 15.34 5 49321 63 79694999
Drug reaction with eosinophilia and systemic symptoms 18.93 15.34 8 49318 64236 79630826
Sinusitis 18.91 15.34 60 49266 195441 79499621
Excessive granulation tissue 18.91 15.34 10 49316 942 79694120
Encephalopathy 18.90 15.34 9 49317 67388 79627674
Cytopenia 18.80 15.34 40 49286 20343 79674719
Adenocarcinoma 18.66 15.34 17 49309 3869 79691193
Eastern Cooperative Oncology Group performance status worsened 18.44 15.34 13 49313 2052 79693010
Dorsal ramus syndrome 18.40 15.34 4 49322 20 79695042
Overflow diarrhoea 18.30 15.34 6 49320 166 79694896
Hydronephrosis 18.16 15.34 36 49290 17418 79677644
Medication error 18.01 15.34 10 49316 68632 79626430
Lower respiratory tract infection 17.76 15.34 33 49293 129187 79565875
Chronic obstructive pulmonary disease 17.74 15.34 16 49310 85403 79609659
Breast injury 17.71 15.34 5 49321 82 79694980
Loose tooth 17.70 15.34 15 49311 3102 79691960
Blood creatinine decreased 17.69 15.34 23 49303 7802 79687260
Retinal detachment 17.60 15.34 25 49301 9222 79685840
Heart rate decreased 17.38 15.34 11 49315 70305 79624757
Intentional product misuse 17.29 15.34 20 49306 95145 79599917
Melaena 17.28 15.34 8 49318 60882 79634180
Mucinous breast carcinoma 17.26 15.34 4 49322 28 79695034
Sequestrectomy 16.97 15.34 9 49317 853 79694209
Carcinoid tumour pulmonary 16.92 15.34 7 49319 377 79694685
Wheezing 16.74 15.34 29 49297 116635 79578427
Product use in unapproved indication 16.61 15.34 89 49237 250270 79444792
Congenital haematological disorder 16.47 15.34 4 49322 35 79695027
Parosmia 16.46 15.34 21 49305 6993 79688069
Bone cancer 16.44 15.34 12 49314 2000 79693062
Hepatic enzyme increased 16.33 15.34 58 49268 182552 79512510
Unevaluable event 16.25 15.34 7 49319 55578 79639484
Treatment noncompliance 16.23 15.34 6 49320 52262 79642800
Fractured sacrum 16.22 15.34 11 49315 1632 79693430
Ascariasis 15.87 15.34 3 49323 6 79695056
Debridement 15.62 15.34 11 49315 1734 79693328
Abdominal wall cyst 15.56 15.34 4 49322 45 79695017
Breast mass 15.50 15.34 20 49306 6734 79688328
White blood cell disorder 15.40 15.34 14 49312 3178 79691884

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L02BA03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ENDOCRINE THERAPY
HORMONE ANTAGONISTS AND RELATED AGENTS
Anti-estrogens
FDA MoA N0000000145 Estrogen Receptor Antagonists
FDA MoA N0000000168 Selective Estrogen Receptor Modulators
FDA EPC N0000175582 Estrogen Receptor Antagonist
MeSH PA D000970 Antineoplastic Agents
MeSH PA D018931 Antineoplastic Agents, Hormonal
MeSH PA D004965 Estrogen Antagonists
MeSH PA D065171 Estrogen Receptor Antagonists
MeSH PA D006727 Hormone Antagonists
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:50792 estrogen receptor antagonists
CHEBI has role CHEBI:50837 oestrogen antagonist

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

DiseaseRelationSNOMED_IDDOID
Metastatic Breast Cancer Progression Post-Antiestrogen Therapy indication
Blood coagulation disorder contraindication 64779008 DOID:1247
Disease of liver contraindication 235856003 DOID:409
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Breastfeeding (mother) contraindication 413712001




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 10.92 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
250MG/5ML (50MG/ML) FULVESTRANT FRESENIUS KABI USA N210326 May 20, 2019 RX SOLUTION INTRAMUSCULAR 10188663 Feb. 14, 2034 TREATMENT OF HORMONE RECEPTOR POSITIVE ADVANCED BREAST CANCER IN POSTMENOPAUSAL WOMEN
250MG/5ML (50MG/ML) FULVESTRANT FRESENIUS KABI USA N210326 May 20, 2019 RX SOLUTION INTRAMUSCULAR 9833459 Feb. 14, 2034 TREATMENT OF HORMONE RECEPTOR POSITIVE ADVANCED BREAST CANCER IN POSTMENOPAUSAL WOMEN
250MG/5ML (50MG/ML) FULVESTRANT FRESENIUS KABI USA N210326 May 20, 2019 RX SOLUTION INTRAMUSCULAR 9271990 May 17, 2034 TREATMENT OF HORMONE RECEPTOR POSITIVE ADVANCED BREAST CANCER IN POSTMENOPAUSAL WOMEN

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Estrogen receptor Nuclear hormone receptor ANTAGONIST Ki 9.62 WOMBAT-PK CHEMBL
Estrogen receptor beta Nuclear hormone receptor ANTAGONIST Ki 8.74 WOMBAT-PK CHEMBL
Progesterone receptor Nuclear hormone receptor IC50 9.68 CHEMBL
G-protein coupled estrogen receptor 1 GPCR EC50 7 WOMBAT-PK
Bile acid receptor Nuclear hormone receptor IC50 6.10 CHEMBL
Steroid hormone receptor ERR1 Nuclear hormone receptor IC50 8.70 CHEMBL
Bifunctional epoxide hydrolase 2 Enzyme Ki 7.59 CHEMBL
Nuclear receptor subfamily 1 group I member 2 Nuclear hormone receptor EC50 5.71 CHEMBL
NAD-dependent protein deacylase sirtuin-5, mitochondrial Enzyme IC50 5.58 CHEMBL
Estrogen receptor Transcription factor IC50 8.23 CHEMBL
Beta-lactamase TEM Enzyme IC50 4.25 CHEMBL

External reference:

IDSource
4021350 VUID
N0000148770 NUI
D01161 KEGG_DRUG
4021350 VANDF
C0935916 UMLSCUI
CHEBI:31638 CHEBI
FVS PDB_CHEM_ID
CHEMBL1358 ChEMBL_ID
D000077267 MESH_DESCRIPTOR_UI
DB00947 DRUGBANK_ID
1015 IUPHAR_LIGAND_ID
7712 INN_ID
22X328QOC4 UNII
104741 PUBCHEM_CID
203870 RXNORM
16618 MMSL
300687 MMSL
43430 MMSL
d04799 MMSL
009642 NDDF
385519002 SNOMEDCT_US
404845006 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Fulvestrant HUMAN PRESCRIPTION DRUG LABEL 1 0143-9022 INJECTION 50 mg INTRAMUSCULAR ANDA 25 sections
Fulvestrant HUMAN PRESCRIPTION DRUG LABEL 1 0143-9022 INJECTION 50 mg INTRAMUSCULAR ANDA 25 sections
FASLODEX HUMAN PRESCRIPTION DRUG LABEL 1 0310-0720 INJECTION 50 mg INTRAMUSCULAR NDA 25 sections
FASLODEX HUMAN PRESCRIPTION DRUG LABEL 1 0310-0720 INJECTION 50 mg INTRAMUSCULAR NDA 25 sections
Fulvestrant HUMAN PRESCRIPTION DRUG LABEL 1 0310-7720 INJECTION 50 mg INTRAMUSCULAR NDA authorized generic 25 sections
Fulvestrant HUMAN PRESCRIPTION DRUG LABEL 1 0310-7720 INJECTION 50 mg INTRAMUSCULAR NDA authorized generic 25 sections
Fulvestrant HUMAN PRESCRIPTION DRUG LABEL 1 0591-5019 INJECTION 250 mg INTRAMUSCULAR NDA 27 sections
Fulvestrant HUMAN PRESCRIPTION DRUG LABEL 1 0591-5019 INJECTION 250 mg INTRAMUSCULAR NDA 27 sections
Fulvestrant HUMAN PRESCRIPTION DRUG LABEL 1 0591-5019 INJECTION 250 mg INTRAMUSCULAR NDA 27 sections
Fulvestrant HUMAN PRESCRIPTION DRUG LABEL 1 0781-3079 INJECTION 50 mg INTRAMUSCULAR ANDA 27 sections
Fulvestrant HUMAN PRESCRIPTION DRUG LABEL 1 0781-3492 INJECTION 50 mg INTRAMUSCULAR ANDA 26 sections
Fulvestrant HUMAN PRESCRIPTION DRUG LABEL 1 0781-9055 INJECTION 50 mg INTRAMUSCULAR ANDA 27 sections
FULVESTRANT HUMAN PRESCRIPTION DRUG LABEL 1 16714-070 INJECTION, SOLUTION 50 mg INTRAMUSCULAR ANDA 18 sections
FULVESTRANT HUMAN PRESCRIPTION DRUG LABEL 1 16714-070 INJECTION, SOLUTION 50 mg INTRAMUSCULAR ANDA 18 sections
Fulvestrant HUMAN PRESCRIPTION DRUG LABEL 1 16714-118 INJECTION 50 mg INTRAMUSCULAR ANDA 26 sections
FULVESTRANT HUMAN PRESCRIPTION DRUG LABEL 1 16729-436 INJECTION 250 mg INTRAMUSCULAR ANDA 25 sections
fulvestrant HUMAN PRESCRIPTION DRUG LABEL 1 25021-462 INJECTION, SOLUTION 50 mg INTRAMUSCULAR ANDA 27 sections
Fulvestrant HUMAN PRESCRIPTION DRUG LABEL 1 43598-262 INJECTION, SOLUTION 50 mg INTRAMUSCULAR ANDA 27 sections
Fulvestrant Human Prescription Drug Label 1 55150-394 INJECTION 50 mg INTRAVENOUS ANDA 27 sections
Fulvestrant Human Prescription Drug Label 1 62332-650 INJECTION 50 mg INTRAMUSCULAR ANDA 27 sections
Fulvestrant HUMAN PRESCRIPTION DRUG LABEL 1 63323-715 INJECTION, SOLUTION 50 mg INTRAMUSCULAR NDA 28 sections
Fulvestrant HUMAN PRESCRIPTION DRUG LABEL 1 67457-311 INJECTION 50 mg INTRAMUSCULAR ANDA 28 sections
fulvestrant HUMAN PRESCRIPTION DRUG LABEL 1 68001-424 INJECTION, SOLUTION 50 mg INTRAMUSCULAR ANDA 27 sections
Fulvestrant HUMAN PRESCRIPTION DRUG LABEL 1 68001-484 INJECTION, SOLUTION 250 mg INTRAMUSCULAR ANDA 27 sections
Fulvestrant68001-510 HUMAN PRESCRIPTION DRUG LABEL 1 68001-510 INJECTION 50 mg INTRAMUSCULAR ANDA 27 sections
FULVESTRANT HUMAN PRESCRIPTION DRUG LABEL 1 68001-522 INJECTION 250 mg INTRAMUSCULAR ANDA 25 sections
FULVESTRANT HUMAN PRESCRIPTION DRUG LABEL 1 68001-522 INJECTION 250 mg INTRAMUSCULAR ANDA 25 sections
Fulvestrant HUMAN PRESCRIPTION DRUG LABEL 1 68462-317 INJECTION 50 mg INTRAMUSCULAR ANDA 27 sections
Fulvestrant HUMAN PRESCRIPTION DRUG LABEL 1 68462-317 INJECTION 50 mg INTRAMUSCULAR ANDA 27 sections
Fulvestrant HUMAN PRESCRIPTION DRUG LABEL 1 70121-1463 INJECTION, SOLUTION 250 mg INTRAMUSCULAR ANDA 27 sections