exemestane 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
aromatase inhibitors 1122 107868-30-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • aromasine
  • FCE 24304
  • exemestane
  • aromasin
a hormonal antineoplastic agent
  • Molecular weight: 296.41
  • Formula: C20H24O2
  • CLOGP: 3.28
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 0
  • TPSA: 34.14
  • ALOGS: -4.64
  • ROTB: 0
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
25 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 1 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 1.35 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 42 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Oct. 21, 1999 FDA PHARMACIA AND UPJOHN

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 1894.25 13.71 1025 48305 81096 63358596
Metastases to bone 1354.28 13.71 536 48794 20483 63419209
Metastases to liver 1084.03 13.71 473 48857 23166 63416526
Neoplasm progression 914.84 13.71 482 48848 35946 63403746
Osteonecrosis of jaw 675.88 13.71 390 48940 34733 63404959
Disease progression 552.10 13.71 573 48757 122185 63317507
Metastases to lung 450.83 13.71 213 49117 12537 63427155
Breast cancer metastatic 389.12 13.71 189 49141 11829 63427863
Metastases to lymph nodes 376.12 13.71 164 49166 7994 63431698
Tumour marker increased 371.85 13.71 141 49189 4774 63434918
Stomatitis 335.68 13.71 473 48857 138252 63301440
Pneumonitis 322.07 13.71 246 49084 34976 63404716
Drug ineffective 297.74 13.71 228 49102 1044537 62395155
Mucosal inflammation 252.92 13.71 242 49088 46686 63393006
Pleural effusion 246.62 13.71 332 48998 92878 63346814
PIK3CA-activated mutation 206.83 13.71 62 49268 997 63438695
Metastases to skin 198.88 13.71 67 49263 1596 63438096
Breast cancer 197.84 13.71 215 49115 48168 63391524
Metastases to pleura 194.07 13.71 65 49265 1520 63438172
Bone pain 193.02 13.71 225 49105 54416 63385276
Lymphoedema 186.11 13.71 115 49215 11577 63428115
Osteonecrosis 182.84 13.71 152 49178 24378 63415314
Breast cancer recurrent 157.96 13.71 74 49256 4267 63435425
Metastases to spine 151.97 13.71 66 49264 3183 63436509
Rheumatoid arthritis 143.91 13.71 15 49315 253804 63185888
Ascites 137.65 13.71 164 49166 40564 63399128
Metastasis 133.77 13.71 70 49260 5127 63434565
Bone lesion 131.14 13.71 72 49258 5809 63433883
Bone disorder 130.32 13.71 118 49212 21208 63418484
Neutropenia 126.99 13.71 360 48970 174645 63265047
Bone sequestrum 125.04 13.71 46 49284 1428 63438264
Palmar-plantar erythrodysaesthesia syndrome 124.53 13.71 119 49211 22896 63416796
Metastases to central nervous system 122.96 13.71 93 49237 13012 63426680
Hot flush 122.84 13.71 174 49156 50985 63388707
Carbohydrate antigen 15-3 increased 122.14 13.71 45 49285 1403 63438289
Therapeutic product effect decreased 121.85 13.71 7 49323 193180 63246512
Hepatic lesion 121.38 13.71 64 49266 4761 63434931
Second primary malignancy 120.95 13.71 76 49254 7877 63431815
Nail disorder 119.11 13.71 91 49239 12924 63426768
Contraindicated product administered 118.01 13.71 15 49315 217633 63222059
Infusion related reaction 117.30 13.71 24 49306 245497 63194195
Metastases to peritoneum 110.99 13.71 54 49276 3388 63436304
Ejection fraction decreased 110.59 13.71 110 49220 22222 63417470
Off label use 107.19 13.71 228 49102 674234 62765458
Joint swelling 103.98 13.71 63 49267 327603 63112089
Exposed bone in jaw 100.71 13.71 48 49282 2877 63436815
Malignant pleural effusion 93.51 13.71 44 49286 2562 63437130
Interstitial lung disease 92.88 13.71 170 49160 61738 63377954
Cough 92.68 13.71 461 48869 292282 63147410
Glossodynia 88.55 13.71 16 49314 178860 63260832
Synovitis 87.75 13.71 19 49311 186899 63252793
Pseudocirrhosis 86.58 13.71 29 49301 678 63439014
Neuropathy peripheral 84.50 13.71 236 49094 113431 63326261
Hormone receptor positive breast cancer 81.53 13.71 26 49304 518 63439174
Arthropathy 80.43 13.71 41 49289 234751 63204941
Abdominal discomfort 78.68 13.71 80 49250 320805 63118887
Pleural neoplasm 78.02 13.71 23 49307 348 63439344
Gingival swelling 76.83 13.71 46 49284 4372 63435320
Lymphangiosis carcinomatosa 76.33 13.71 32 49298 1413 63438279
Device related thrombosis 72.99 13.71 33 49297 1752 63437940
Epistaxis 70.60 13.71 167 49163 72558 63367134
Hyperglycaemia 69.25 13.71 120 49210 41747 63397945
Metastases to pelvis 68.49 13.71 22 49308 449 63439243
General physical health deterioration 67.84 13.71 323 49007 201079 63238613
Gamma-glutamyltransferase increased 67.69 13.71 106 49224 33925 63405767
Lymphadenopathy mediastinal 67.12 13.71 36 49294 2772 63436920
Polyneuropathy 67.00 13.71 69 49261 14520 63425172
Hypotension 66.76 13.71 68 49262 272536 63167156
Discomfort 65.61 13.71 24 49306 167350 63272342
Intentional product use issue 64.24 13.71 11 49319 127881 63311811
Eastern Cooperative Oncology Group performance status worsened 63.67 13.71 27 49303 1227 63438465
Metastases to chest wall 63.52 13.71 22 49308 571 63439121
Aphthous ulcer 62.35 13.71 65 49265 13873 63425819
Skin toxicity 61.71 13.71 41 49289 4673 63435019
Tooth extraction 61.15 13.71 56 49274 10208 63429484
Osteolysis 60.83 13.71 34 49296 2840 63436852
Psoriatic arthropathy 58.66 13.71 3 49327 91517 63348175
Swelling 58.46 13.71 77 49253 275301 63164391
Wound 58.18 13.71 27 49303 163236 63276456
Treatment failure 56.74 13.71 43 49287 199000 63240692
Decreased appetite 55.94 13.71 360 48970 250692 63189000
Therapeutic product effect incomplete 54.21 13.71 15 49315 125041 63314651
Blood alkaline phosphatase increased 53.42 13.71 109 49221 42858 63396834
Oral pain 53.11 13.71 86 49244 28308 63411384
Metastases to the mediastinum 51.87 13.71 18 49312 470 63439222
Abdominal lymphadenopathy 51.43 13.71 20 49310 725 63438967
Aspartate aminotransferase increased 50.74 13.71 170 49160 90107 63349585
Hypersensitivity 50.55 13.71 94 49236 292591 63147101
Hepatic enzyme increased 50.05 13.71 50 49280 202278 63237414
Fatigue 49.82 13.71 966 48364 887062 62552630
Irritable bowel syndrome 48.98 13.71 4 49326 82408 63357284
Lung infiltration 46.82 13.71 57 49273 14406 63425286
Haematotoxicity 46.07 13.71 46 49284 9330 63430362
Intentional overdose 45.78 13.71 3 49327 74149 63365543
Gingival erythema 44.47 13.71 18 49312 726 63438966
Product use issue 44.43 13.71 64 49266 220456 63219236
Injection site erythema 44.40 13.71 6 49324 83168 63356524
Overdose 44.25 13.71 17 49313 115061 63324631
Osteitis 44.13 13.71 29 49301 3245 63436447
Injection site pain 43.92 13.71 23 49307 129777 63309915
Periodontitis 43.89 13.71 29 49301 3274 63436418
Peritoneal disorder 43.82 13.71 16 49314 486 63439206
Invasive ductal breast carcinoma 43.48 13.71 39 49291 6919 63432773
Anaemia 42.87 13.71 381 48949 293049 63146643
Drug hypersensitivity 42.79 13.71 113 49217 310574 63129118
Oral cavity fistula 42.79 13.71 17 49313 653 63439039
Hepatic failure 42.61 13.71 89 49241 35567 63404125
Product dose omission issue 42.47 13.71 73 49257 234240 63205452
Metastases to meninges 42.44 13.71 26 49304 2576 63437116
Osteomyelitis 42.26 13.71 74 49256 25946 63413746
Dysgeusia 41.83 13.71 104 49226 46606 63393086
Confusional state 41.61 13.71 75 49255 236305 63203387
Toxicity to various agents 41.28 13.71 81 49249 247169 63192523
Sinusitis 40.72 13.71 71 49259 226582 63213110
Blood creatinine increased 40.46 13.71 155 49175 87689 63352003
Pulmonary mass 40.31 13.71 67 49263 22529 63417163
Mobility decreased 40.21 13.71 22 49308 121137 63318555
Condition aggravated 39.83 13.71 169 49161 402048 63037644
Blister 39.67 13.71 26 49304 129788 63309904
Blood lactate dehydrogenase increased 39.19 13.71 67 49263 23049 63416643
Lymphadenopathy 39.15 13.71 90 49240 38368 63401324
Fibromyalgia 38.07 13.71 8 49322 80412 63359280
Weight decreased 37.68 13.71 354 48976 276444 63163248
Jaw disorder 37.48 13.71 32 49298 5317 63434375
Superinfection 37.36 13.71 24 49306 2583 63437109
Metastases to adrenals 37.28 13.71 16 49314 749 63438943
Metastases to soft tissue 36.63 13.71 11 49319 178 63439514
Metastases to abdominal wall 36.21 13.71 10 49320 118 63439574
Sequestrectomy 36.10 13.71 16 49314 810 63438882
Folliculitis 35.41 13.71 6 49324 70311 63369381
Weight increased 35.03 13.71 96 49234 260696 63178996
Invasive lobular breast carcinoma 34.87 13.71 16 49314 879 63438813
Asthenia 33.68 13.71 450 48880 383154 63056538
Adverse event 33.50 13.71 6 49324 67553 63372139
Diarrhoea 33.08 13.71 757 48573 714609 62725083
Fall 32.89 13.71 175 49155 392159 63047533
Creutzfeldt-Jakob disease 32.68 13.71 10 49320 173 63439519
Tumour marker abnormal 32.54 13.71 12 49318 375 63439317
Product use in unapproved indication 32.24 13.71 56 49274 179024 63260668
Pathological fracture 32.21 13.71 37 49293 8797 63430895
Bradycardia 31.32 13.71 9 49321 73218 63366474
Radiation skin injury 31.02 13.71 15 49315 928 63438764
Purulent discharge 30.64 13.71 27 49303 4679 63435013
Alanine aminotransferase increased 30.35 13.71 160 49170 103610 63336082
Axillary pain 30.28 13.71 19 49311 1964 63437728
Medication error 29.82 13.71 3 49327 52281 63387411
Leukopenia 29.73 13.71 129 49201 77161 63362531
Nail dystrophy 29.59 13.71 15 49315 1028 63438664
Dyspnoea 29.07 13.71 695 48635 660618 62779074
Fibrous histiocytoma 27.70 13.71 12 49318 575 63439117
Debridement 27.40 13.71 15 49315 1203 63438489
Feeding disorder 27.09 13.71 42 49288 13320 63426372
Multiple sclerosis relapse 27.09 13.71 3 49327 48475 63391217
Urticaria 27.07 13.71 55 49275 165747 63273945
Musculoskeletal stiffness 27.06 13.71 65 49265 184553 63255139
Pericardial effusion 26.99 13.71 67 49263 29991 63409701
Contusion 26.93 13.71 47 49283 149997 63289695
Excessive granulation tissue 26.65 13.71 13 49317 820 63438872
Carcinoid tumour pulmonary 26.65 13.71 11 49319 467 63439225
Hip arthroplasty 26.49 13.71 3 49327 47643 63392049
Blood bilirubin increased 26.48 13.71 76 49254 37064 63402628
Cardiac failure 26.44 13.71 138 49192 89004 63350688
Pain in jaw 26.30 13.71 84 49246 43412 63396280
Nail infection 26.12 13.71 19 49311 2504 63437188
Hospitalisation 26.04 13.71 17 49313 85064 63354628
Onychoclasis 26.02 13.71 28 49302 6194 63433498
Mouth ulceration 25.99 13.71 70 49260 32914 63406778
Metastases to thorax 25.86 13.71 9 49321 237 63439455
Adverse drug reaction 25.69 13.71 15 49315 79699 63359993
Oral disorder 25.63 13.71 33 49297 8821 63430871
Neoplasm recurrence 25.36 13.71 19 49311 2619 63437073
Somnolence 25.33 13.71 64 49266 178621 63261071
Gingivitis 25.32 13.71 32 49298 8397 63431295
Lacrimation increased 25.24 13.71 52 49278 20579 63419113
Blood glucose increased 25.08 13.71 130 49200 83626 63356066
Oedema peripheral 25.07 13.71 241 49089 189270 63250422
Pancreatic neoplasm 24.94 13.71 12 49318 734 63438958
Hallucination 24.85 13.71 6 49324 54811 63384881
Hepatic atrophy 24.63 13.71 9 49321 274 63439418
Hepatic function abnormal 24.56 13.71 74 49256 37068 63402624
Incorrect dose administered 24.51 13.71 8 49322 59960 63379732
Myocardial infarction 24.32 13.71 25 49305 99868 63339824
Blood phosphorus decreased 24.03 13.71 23 49307 4430 63435262
Uterine mass 23.91 13.71 9 49321 298 63439394
White blood cell count decreased 23.66 13.71 187 49143 138917 63300775
Hiccups 23.55 13.71 17 49313 2214 63437478
Protein total decreased 23.43 13.71 26 49304 5951 63433741
Psoriasis 23.24 13.71 20 49310 86937 63352755
Periodontal disease 23.20 13.71 15 49315 1633 63438059
Pulmonary tumour thrombotic microangiopathy 23.09 13.71 6 49324 55 63439637
Loss of personal independence in daily activities 22.96 13.71 25 49305 97265 63342427
Mouth swelling 22.82 13.71 23 49307 4717 63434975
Mucosal dryness 22.53 13.71 18 49312 2726 63436966
Trigger finger 22.35 13.71 22 49308 4386 63435306
Osteopenia 22.04 13.71 48 49282 19737 63419955
Thrombocytopenia 21.89 13.71 196 49134 150961 63288731
Tumour marker decreased 21.87 13.71 6 49324 69 63439623
Vulvovaginal dryness 21.65 13.71 18 49312 2883 63436809
Serous cystadenocarcinoma ovary 21.54 13.71 5 49325 27 63439665
Exostosis of jaw 21.33 13.71 13 49317 1276 63438416
Cell marker increased 21.14 13.71 8 49322 269 63439423
Cardiomyopathy 21.13 13.71 44 49286 17540 63422152
Actinomycosis 21.08 13.71 12 49318 1038 63438654
Skin lesion 21.07 13.71 62 49268 30659 63409033
Congestive cardiomyopathy 21.05 13.71 25 49305 6157 63433535
Erysipelas 20.62 13.71 28 49302 7877 63431815
Heart rate decreased 20.62 13.71 5 49325 45555 63394137
Radiation fibrosis 20.56 13.71 5 49325 34 63439658
Concomitant disease aggravated 20.40 13.71 30 49300 9082 63430610
Blood phosphorus increased 20.39 13.71 18 49312 3127 63436565
Injection site pruritus 20.33 13.71 5 49325 45111 63394581
Suicide attempt 20.29 13.71 11 49319 60907 63378785
Sedation 20.24 13.71 3 49327 38806 63400886
Cancer pain 20.10 13.71 18 49312 3187 63436505
Bronchitis 19.92 13.71 42 49288 124893 63314799
Bone marrow infiltration 19.88 13.71 10 49320 674 63439018
Drug interaction 19.84 13.71 101 49229 229030 63210662
Pain 19.80 13.71 432 48898 740196 62699496
Skin exfoliation 19.79 13.71 76 49254 43026 63396666
COVID-19 19.78 13.71 36 49294 113067 63326625
Suicidal ideation 19.75 13.71 12 49318 62409 63377283
Breast pain 19.75 13.71 29 49301 8769 63430923
Wrong technique in product usage process 19.71 13.71 12 49318 62328 63377364
Radioisotope scan 19.64 13.71 4 49326 10 63439682
Peripheral swelling 19.38 13.71 124 49206 265818 63173874
Arthralgia 19.31 13.71 579 48751 569131 62870561
Bone neoplasm 19.21 13.71 10 49320 724 63438968
Sensory loss 19.13 13.71 31 49299 10207 63429485
Peripheral sensory neuropathy 18.85 13.71 26 49304 7425 63432267
Nasopharyngitis 18.81 13.71 118 49212 254139 63185553
Breast cancer female 18.78 13.71 36 49294 13523 63426169
Ocular vasculitis 18.51 13.71 5 49325 54 63439638
Bone debridement 18.42 13.71 7 49323 238 63439454
Recurrent cancer 18.41 13.71 14 49316 1973 63437719
Spinal pain 18.34 13.71 35 49295 13104 63426588
Dry skin 18.22 13.71 90 49240 56797 63382895
Coma 18.20 13.71 14 49316 64350 63375342
C-reactive protein increased 18.17 13.71 131 49199 94576 63345116
Pustule 18.06 13.71 13 49317 1686 63438006
Type 2 diabetes mellitus 17.92 13.71 14 49316 63854 63375838
Acne 17.91 13.71 49 49281 23244 63416448
Abscess jaw 17.88 13.71 12 49318 1390 63438302
Gastrointestinal disorder 17.83 13.71 48 49282 131191 63308501
Carcinoembryonic antigen increased 17.61 13.71 13 49317 1752 63437940
Dermatitis 17.60 13.71 40 49290 16918 63422774
Atrophic vulvovaginitis 17.59 13.71 13 49317 1755 63437937
Blood pressure fluctuation 17.54 13.71 7 49323 46310 63393382
Unevaluable event 17.53 13.71 9 49321 51377 63388315
Lymphatic obstruction 17.49 13.71 4 49326 20 63439672
Neoplasm malignant 17.45 13.71 57 49273 29804 63409888
Recall phenomenon 17.43 13.71 9 49321 641 63439051
Lymphangitis 17.23 13.71 10 49320 897 63438795
Ill-defined disorder 17.17 13.71 23 49307 81732 63357960
Death 17.16 13.71 396 48934 373985 63065707
Computerised tomogram abnormal 17.06 13.71 14 49316 2203 63437489
Cardio-respiratory arrest 17.01 13.71 13 49317 59946 63379746
Hilar lymphadenopathy 16.90 13.71 11 49319 1211 63438481
Fluid retention 16.85 13.71 13 49317 59673 63380019
Rib fracture 16.85 13.71 47 49283 22550 63417142
Drug intolerance 16.81 13.71 156 49174 308505 63131187
Anticipatory anxiety 16.66 13.71 11 49319 1240 63438452
Bone marrow tumour cell infiltration 16.60 13.71 4 49326 26 63439666
Fibrin D dimer increased 16.55 13.71 20 49310 5014 63434678
Migraine 16.26 13.71 35 49295 103311 63336381
Fingerprint loss 16.23 13.71 4 49326 29 63439663
Loss of consciousness 16.20 13.71 43 49287 118078 63321614
Fractured sacrum 16.08 13.71 13 49317 2003 63437689
Wound treatment 16.08 13.71 6 49324 194 63439498
Liver injury 16.07 13.71 14 49316 60506 63379186
Muscle twitching 15.75 13.71 42 49288 19626 63420066
Depressed level of consciousness 15.73 13.71 15 49315 62063 63377629
Progesterone receptor assay positive 15.64 13.71 7 49323 363 63439329
Heart rate increased 15.60 13.71 31 49299 94207 63345485
Congenital haematological disorder 15.56 13.71 4 49326 35 63439657
Metastases to bladder 15.47 13.71 6 49324 216 63439476
Osteosclerosis 15.39 13.71 17 49313 3871 63435821
Wheezing 15.35 13.71 32 49298 95563 63344129
Hyperbaric oxygen therapy 15.27 13.71 4 49326 38 63439654
Cell-mediated immune deficiency 15.27 13.71 4 49326 38 63439654
Corneal epithelial microcysts 15.19 13.71 3 49327 6 63439686
Ascariasis 15.19 13.71 3 49327 6 63439686
Pleural mass 15.19 13.71 3 49327 6 63439686
Pneumonitis chemical 15.11 13.71 6 49324 230 63439462
Hyperparathyroidism secondary 15.08 13.71 11 49319 1456 63438236
Red blood cell count decreased 14.99 13.71 67 49263 40578 63399114
Fistula 14.90 13.71 28 49302 10365 63429327
Musculoskeletal chest pain 14.89 13.71 43 49287 21040 63418652
Drug reaction with eosinophilia and systemic symptoms 14.76 13.71 4 49326 33832 63405860
Aortic arteriosclerosis 14.72 13.71 21 49309 6188 63433504
Hydronephrosis 14.39 13.71 28 49302 10634 63429058
Encephalopathy 14.36 13.71 6 49324 38614 63401078
Biopsy site unspecified abnormal 14.35 13.71 4 49326 49 63439643
Radiation pneumonitis 14.33 13.71 11 49319 1572 63438120
Blood pressure increased 14.27 13.71 71 49259 161991 63277701
Pulmonary embolism 14.26 13.71 146 49184 116538 63323154
Incorrect product formulation administered 14.21 13.71 5 49325 136 63439556
Metastases to ovary 14.21 13.71 7 49323 451 63439241
Metastases to bone marrow 14.15 13.71 7 49323 455 63439237
Oral pustule 14.13 13.71 4 49326 52 63439640
Haemoglobin decreased 14.13 13.71 174 49156 145311 63294381
Nasal mucosal disorder 14.05 13.71 7 49323 462 63439230
Onycholysis 14.01 13.71 11 49319 1625 63438067
Respiratory arrest 13.98 13.71 4 49326 32641 63407051
Blood pressure decreased 13.96 13.71 18 49312 65004 63374688
Portal hypertension 13.93 13.71 16 49314 3803 63435889
Skin mass 13.91 13.71 20 49310 5935 63433757
Breath odour 13.80 13.71 10 49320 1310 63438382
Tendon calcification 13.79 13.71 4 49326 57 63439635
Alveolar lung disease 13.72 13.71 5 49325 151 63439541
Loose tooth 13.71 13.71 15 49315 3379 63436313

FDA Adverse Event Reporting System (Male)

None

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
Metastases to bone 1060.73 14.42 403 35566 24024 79684395
Malignant neoplasm progression 900.99 14.42 629 35340 135361 79573058
Neoplasm progression 731.07 14.42 389 35580 51293 79657126
Metastases to liver 679.95 14.42 306 35663 28008 79680411
Osteonecrosis of jaw 478.51 14.42 277 35692 42949 79665470
Disease progression 372.98 14.42 437 35532 183925 79524494
Metastases to lung 345.01 14.42 167 35802 17996 79690423
Breast cancer metastatic 334.14 14.42 131 35838 8471 79699948
Metastases to lymph nodes 300.16 14.42 128 35841 10269 79698150
Stomatitis 288.54 14.42 343 35626 146414 79562005
Tumour marker increased 269.57 14.42 93 35876 4179 79704240
Pneumonitis 184.39 14.42 179 35790 60681 79647738
Mucosal inflammation 177.78 14.42 194 35775 75386 79633033
Metastases to skin 171.12 14.42 53 35916 1686 79706733
Breast cancer 168.42 14.42 132 35837 33649 79674770
Bone pain 139.71 14.42 148 35821 55594 79652825
Hot flush 138.06 14.42 146 35823 54731 79653688
Nail disorder 136.49 14.42 78 35891 11774 79696645
Lymphoedema 135.78 14.42 79 35890 12334 79696085
Drug ineffective 132.56 14.42 177 35792 1080736 78627683
Pleural effusion 132.35 14.42 236 35733 145026 79563393
PIK3CA-activated mutation 130.45 14.42 34 35935 569 79707850
Osteonecrosis 128.65 14.42 109 35860 30986 79677433
Breast cancer recurrent 110.90 14.42 44 35925 2933 79705486
Carbohydrate antigen 15-3 increased 103.77 14.42 33 35936 1146 79707273
Bone disorder 100.29 14.42 77 35892 19036 79689383
Fatigue 98.78 14.42 736 35233 928991 78779428
Pseudocirrhosis 98.71 14.42 28 35941 652 79707767
Ejection fraction decreased 94.15 14.42 96 35873 34481 79673938
Metastases to pleura 90.99 14.42 32 35937 1522 79706897
Neuropathy peripheral 87.04 14.42 195 35774 141110 79567309
Exposed bone in jaw 85.39 14.42 39 35930 3681 79704738
Bone lesion 84.81 14.42 45 35924 5874 79702545
Metastases to spine 82.81 14.42 40 35929 4284 79704135
Hypotension 81.34 14.42 49 35920 440268 79268151
Pleural neoplasm 80.82 14.42 21 35948 347 79708072
Cough 77.43 14.42 349 35620 366440 79341979
Device related thrombosis 77.31 14.42 33 35936 2650 79705769
Off label use 77.25 14.42 186 35783 907029 78801390
Metastases to central nervous system 68.95 14.42 58 35911 16317 79692102
Hepatic lesion 67.52 14.42 41 35928 6918 79701501
Second primary malignancy 67.06 14.42 54 35915 14296 79694123
Neutropenia 63.87 14.42 278 35691 287432 79420987
Drug abuse 60.86 14.42 3 35966 162688 79545731
Ascites 57.82 14.42 114 35855 75448 79632971
Rheumatoid arthritis 57.42 14.42 12 35957 208458 79499961
Hormone receptor positive breast cancer 57.31 14.42 16 35953 351 79708068
Tooth extraction 57.03 14.42 44 35925 10951 79697468
Metastases to peritoneum 56.39 14.42 31 35938 4341 79704078
Therapeutic product effect decreased 55.51 14.42 5 35964 163858 79544561
Lymphangiosis carcinomatosa 53.94 14.42 24 35945 2130 79706289
Oral pain 53.77 14.42 69 35900 31729 79676690
Aphthous ulcer 53.61 14.42 51 35918 16838 79691581
Metastases to the mediastinum 53.38 14.42 17 35952 593 79707826
Infusion related reaction 52.68 14.42 19 35950 230218 79478201
Malignant pleural effusion 52.14 14.42 27 35942 3353 79705066
Lymphadenopathy mediastinal 50.79 14.42 29 35940 4367 79704052
Metastasis 50.51 14.42 34 35935 6846 79701573
Toxicity to various agents 50.39 14.42 70 35899 421470 79286949
Maternal exposure during pregnancy 49.57 14.42 3 35966 136535 79571884
Interstitial lung disease 48.85 14.42 136 35833 112464 79595955
Gingival swelling 46.90 14.42 28 35941 4581 79703838
Peritoneal disorder 46.36 14.42 16 35953 719 79707700
Palmar-plantar erythrodysaesthesia syndrome 45.53 14.42 65 35904 33069 79675350
Bone sequestrum 45.21 14.42 18 35951 1211 79707208
Asthenia 44.70 14.42 388 35581 511301 79197118
Overdose 44.22 14.42 14 35955 184192 79524227
Arthralgia 42.60 14.42 419 35550 571384 79137035
Osteolysis 42.35 14.42 26 35943 4472 79703947
Contraindicated product administered 41.50 14.42 10 35959 157528 79550891
Blood alkaline phosphatase increased 40.44 14.42 89 35880 63575 79644844
Decreased appetite 40.06 14.42 278 35691 342140 79366279
Oral cavity fistula 39.27 14.42 14 35955 693 79707726
Bradycardia 39.01 14.42 7 35962 135550 79572869
Invasive ductal breast carcinoma 38.26 14.42 27 35942 5865 79702554
Nail dystrophy 37.83 14.42 15 35954 998 79707421
Intentional product use issue 37.52 14.42 11 35958 152101 79556318
Abdominal lymphadenopathy 37.09 14.42 16 35953 1318 79707101
Lacrimation increased 36.79 14.42 48 35921 22429 79685990
Intentional overdose 36.52 14.42 3 35966 105957 79602462
Creutzfeldt-Jakob disease 36.46 14.42 10 35959 205 79708214
Joint swelling 36.44 14.42 46 35923 288600 79419819
Pathological fracture 35.71 14.42 33 35936 10504 79697915
Acute kidney injury 34.86 14.42 119 35850 519285 79189134
Diarrhoea 34.26 14.42 572 35397 879917 78828502
Dysgeusia 34.15 14.42 78 35891 57099 79651320
Nail infection 33.69 14.42 18 35951 2381 79706038
Superinfection 33.08 14.42 23 35946 4879 79703540
Sequestrectomy 33.02 14.42 13 35956 849 79707570
Trigger finger 31.21 14.42 21 35948 4224 79704195
Therapeutic product effect incomplete 30.23 14.42 13 35956 141632 79566787
Drug interaction 30.01 14.42 92 35877 415091 79293328
Metastases to eye 29.95 14.42 9 35960 258 79708161
Metastases to soft tissue 29.87 14.42 11 35958 598 79707821
Axillary pain 29.83 14.42 16 35953 2133 79706286
White blood cell count decreased 29.60 14.42 165 35804 188123 79520296
Hyperglycaemia 29.56 14.42 84 35885 70251 79638168
Confusional state 29.52 14.42 62 35907 317935 79390484
Mouth ulceration 29.45 14.42 58 35911 38336 79670083
Myocardial infarction 29.31 14.42 24 35945 184105 79524314
Alopecia 28.31 14.42 190 35779 231165 79477254
Skin toxicity 28.10 14.42 26 35943 8288 79700131
Fibrous histiocytoma 28.09 14.42 11 35958 708 79707711
Osteitis 27.79 14.42 19 35950 3924 79704495
Synovitis 27.46 14.42 17 35952 150717 79557702
Metastases to chest wall 27.30 14.42 10 35959 535 79707884
Weight decreased 27.22 14.42 262 35707 354936 79353483
Epistaxis 27.21 14.42 111 35858 111404 79597015
Haematotoxicity 26.75 14.42 34 35935 15485 79692934
Pulmonary mass 26.17 14.42 47 35922 28987 79679432
Hallucination 25.62 14.42 4 35965 85741 79622678
Metastases to pelvis 25.41 14.42 10 35959 652 79707767
Back pain 25.12 14.42 228 35741 303952 79404467
Tumour marker abnormal 24.93 14.42 8 35961 286 79708133
Nausea 24.79 14.42 585 35384 956611 78751808
Cardio-respiratory arrest 24.73 14.42 9 35960 108501 79599918
Mouth swelling 24.58 14.42 21 35948 6030 79702389
Radioisotope scan 24.58 14.42 4 35965 3 79708416
Pain in jaw 24.35 14.42 60 35909 46091 79662328
Hydrothorax 23.43 14.42 12 35957 1456 79706963
Pancreatic neoplasm 23.37 14.42 12 35957 1464 79706955
Pulmonary tumour thrombotic microangiopathy 23.27 14.42 6 35963 96 79708323
Oral herpes 22.93 14.42 43 35926 27411 79681008
Radiation fibrosis 22.90 14.42 5 35964 37 79708382
Wound 22.74 14.42 12 35957 116167 79592252
Anticipatory anxiety 22.64 14.42 11 35958 1193 79707226
Pustule 22.44 14.42 13 35956 2012 79706407
Exostosis of jaw 22.21 14.42 11 35958 1243 79707176
Muscle twitching 22.21 14.42 40 35929 24724 79683695
Cell marker increased 22.10 14.42 9 35960 642 79707777
Progesterone receptor assay positive 22.07 14.42 7 35962 241 79708178
Hepatic atrophy 21.75 14.42 8 35961 433 79707986
Discomfort 21.75 14.42 15 35954 125602 79582817
Debridement 21.48 14.42 12 35957 1733 79706686
Product use in unapproved indication 21.44 14.42 51 35918 250308 79458111
Periodontitis 21.18 14.42 17 35952 4479 79703940
Blood phosphorus decreased 20.90 14.42 20 35949 6648 79701771
Vaginal discharge 20.82 14.42 21 35948 7442 79700977
Breast pain 20.79 14.42 22 35947 8243 79700176
Breast mass 20.69 14.42 20 35949 6734 79701685
Arthropathy 20.54 14.42 30 35939 177081 79531338
Hypersensitivity 20.47 14.42 56 35913 262183 79446236
Coma 20.29 14.42 10 35959 100639 79607780
Sensory loss 20.12 14.42 27 35942 12964 79695455
Neoplasm recurrence 19.99 14.42 16 35953 4198 79704221
Metastases to meninges 19.97 14.42 15 35954 3586 79704833
Incorrect dose administered 19.91 14.42 5 35964 76625 79631794
Bone neoplasm 19.83 14.42 9 35960 837 79707582
Osteomyelitis 19.81 14.42 45 35924 32820 79675599
Rhabdomyolysis 19.67 14.42 11 35958 103120 79605299
Poor peripheral circulation 19.67 14.42 15 35954 3668 79704751
Heart rate decreased 19.45 14.42 4 35965 70312 79638107
Fractured sacrum 19.42 14.42 11 35958 1632 79706787
Nipple exudate bloody 19.16 14.42 5 35964 84 79708335
Metastases to thorax 19.07 14.42 6 35963 201 79708218
Carcinoid tumour pulmonary 19.07 14.42 7 35962 377 79708042
Protein total decreased 19.06 14.42 22 35947 9070 79699349
Aspartate aminotransferase increased 18.87 14.42 117 35852 138524 79569895
Medication error 18.79 14.42 4 35965 68638 79639781
Vulvovaginal dryness 18.79 14.42 12 35957 2212 79706207
Injection site erythema 18.66 14.42 6 35963 78191 79630228
Skin exfoliation 18.64 14.42 61 35908 55039 79653380
Dry skin 18.46 14.42 70 35899 67925 79640494
Irritable bowel syndrome 18.37 14.42 3 35966 62238 79646181
Glossodynia 18.34 14.42 12 35957 103325 79605094
Febrile neutropenia 18.27 14.42 49 35920 230950 79477469
Condition aggravated 18.12 14.42 142 35827 500982 79207437
Periodontal disease 18.09 14.42 11 35958 1859 79706560
Mucosal ulceration 18.08 14.42 11 35958 1862 79706557
Treatment failure 17.76 14.42 31 35938 170455 79537964
Congenital haematological disorder 17.72 14.42 4 35965 35 79708384
Fall 17.71 14.42 138 35831 487491 79220928
Weight increased 17.60 14.42 65 35904 277321 79431098
Recall phenomenon 17.30 14.42 9 35960 1128 79707291
Cardiac arrest 17.30 14.42 32 35937 172064 79536355
Teeth brittle 17.27 14.42 7 35962 493 79707926
Oral disorder 17.21 14.42 22 35947 10073 79698346
Lung disorder 17.19 14.42 77 35892 80480 79627939
Lymphadenopathy 17.17 14.42 58 35911 53189 79655230
Loss of consciousness 17.08 14.42 31 35938 167912 79540507
Drug reaction with eosinophilia and systemic symptoms 17.07 14.42 4 35965 64240 79644179
Ascariasis 16.82 14.42 3 35966 6 79708413
Incorrect product formulation administered 16.75 14.42 5 35964 140 79708279
Recurrent cancer 16.70 14.42 12 35957 2681 79705738
Product administered at inappropriate site 16.60 14.42 14 35955 3951 79704468
Somnolence 16.51 14.42 54 35915 238927 79469492
Blood pressure fluctuation 16.29 14.42 5 35964 67140 79641279
Blood bilirubin increased 16.21 14.42 66 35903 66166 79642253
Depressed level of consciousness 16.13 14.42 12 35957 96640 79611779
Injection site pain 16.05 14.42 21 35948 129817 79578602
Tumour marker decreased 15.95 14.42 4 35965 57 79708362
Gingivitis 15.92 14.42 20 35949 9001 79699418
Mobility decreased 15.89 14.42 19 35950 122156 79586263
Suicide attempt 15.60 14.42 9 35960 82923 79625496
Feeding disorder 15.54 14.42 27 35942 16227 79692192
Adverse event 15.51 14.42 4 35965 60210 79648209
Metabolic acidosis 15.46 14.42 9 35960 82520 79625899
Hospitalisation 15.34 14.42 12 35957 94224 79614195
Abdominal discomfort 15.10 14.42 60 35909 250667 79457752
Chronic obstructive pulmonary disease 15.05 14.42 10 35959 85409 79623010
Musculoskeletal chest pain 15.02 14.42 34 35935 24730 79683689
Encephalopathy 14.67 14.42 6 35963 67391 79641028
Eastern Cooperative Oncology Group performance status worsened 14.67 14.42 10 35959 2055 79706364
Dyspnoea 14.63 14.42 497 35472 856528 78851891
Insomnia 14.61 14.42 172 35797 244998 79463421
Actinomycosis 14.61 14.42 8 35961 1111 79707308
Pericardial effusion 14.59 14.42 50 35919 46187 79662232
Congestive cardiomyopathy 14.58 14.42 22 35947 11758 79696661
Hyperparathyroidism secondary 14.57 14.42 11 35958 2649 79705770
Osteosclerosis 14.56 14.42 13 35956 3958 79704461
Bone debridement 14.46 14.42 6 35963 449 79707970
Skin mass 14.43 14.42 18 35951 8045 79700374

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L02BG06 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ENDOCRINE THERAPY
HORMONE ANTAGONISTS AND RELATED AGENTS
Aromatase inhibitors
FDA MoA N0000175080 Aromatase Inhibitors
FDA EPC N0000175563 Aromatase Inhibitor
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:35703 Xenobiotic
CHEBI has role CHEBI:50790 aromatase inhibitors
CHEBI has role CHEBI:78298 environmental contaminants
MeSH PA D000970 Antineoplastic Agents
MeSH PA D047072 Aromatase Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D004965 Estrogen Antagonists
MeSH PA D006727 Hormone Antagonists
MeSH PA D065088 Steroid Synthesis Inhibitors

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

DiseaseRelationSNOMED_IDDOID
Hormone receptor positive malignant neoplasm of breast indication 417181009
Advanced Breast Cancer Progression Post-Antiestrogen Therapy indication
Prevention of Breast Carcinoma off-label use
Pregnancy, function contraindication 289908002
Osteopenia contraindication 312894000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Aromatase Enzyme INHIBITOR IC50 5.69 WOMBAT-PK CHEMBL
Androgen receptor Nuclear hormone receptor WOMBAT-PK

External reference:

IDSource
4021191 VUID
N0000148637 NUI
D00963 KEGG_DRUG
4021191 VANDF
C0851344 UMLSCUI
CHEBI:4953 CHEBI
EXM PDB_CHEM_ID
CHEMBL1200374 ChEMBL_ID
DB00990 DRUGBANK_ID
C056516 MESH_SUPPLEMENTAL_RECORD_UI
60198 PUBCHEM_CID
7073 IUPHAR_LIGAND_ID
6770 INN_ID
NY22HMQ4BX UNII
258494 RXNORM
180650 MMSL
31449 MMSL
8478 MMSL
d04461 MMSL
007997 NDDF
116115004 SNOMEDCT_US
387017005 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Aromasin HUMAN PRESCRIPTION DRUG LABEL 1 0009-7663 TABLET 25 mg ORAL NDA 27 sections
Aromasin HUMAN PRESCRIPTION DRUG LABEL 1 0009-7663 TABLET 25 mg ORAL NDA 27 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 0054-0080 TABLET, FILM COATED 25 mg ORAL ANDA 27 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 0054-0080 TABLET, FILM COATED 25 mg ORAL ANDA 27 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 0378-5001 TABLET, FILM COATED 25 mg ORAL ANDA 27 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 0832-0595 TABLET 25 mg ORAL ANDA 27 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 0832-0595 TABLET 25 mg ORAL ANDA 27 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 0832-0595 TABLET 25 mg ORAL ANDA 27 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 44278-025 TABLET 25 mg ORAL ANDA 26 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 47781-108 TABLET 25 mg ORAL ANDA 26 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 47781-108 TABLET 25 mg ORAL ANDA 26 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 50090-5193 TABLET 25 mg ORAL ANDA 26 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 51991-005 TABLET, FILM COATED 25 mg ORAL ANDA 31 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 51991-005 TABLET, FILM COATED 25 mg ORAL ANDA 31 sections
Aromasin HUMAN PRESCRIPTION DRUG LABEL 1 54868-5261 TABLET 25 mg ORAL NDA 13 sections
Exemestane Human Prescription Drug Label 1 59651-516 TABLET, FILM COATED 25 mg ORAL ANDA 26 sections
EXEMESTANE HUMAN PRESCRIPTION DRUG LABEL 1 59762-2858 TABLET, SUGAR COATED 25 mg ORAL NDA AUTHORIZED GENERIC 28 sections
EXEMESTANE HUMAN PRESCRIPTION DRUG LABEL 1 59762-2858 TABLET, SUGAR COATED 25 mg ORAL NDA AUTHORIZED GENERIC 28 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 63629-2056 TABLET, FILM COATED 25 mg ORAL ANDA 30 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 63629-2056 TABLET, FILM COATED 25 mg ORAL ANDA 30 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 63629-2056 TABLET, FILM COATED 25 mg ORAL ANDA 30 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 65162-240 TABLET, FILM COATED 25 mg ORAL ANDA 25 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 65162-240 TABLET, FILM COATED 25 mg ORAL ANDA 25 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 65162-240 TABLET, FILM COATED 25 mg ORAL ANDA 25 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 68382-383 TABLET 25 mg ORAL ANDA 25 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 68382-383 TABLET 25 mg ORAL ANDA 25 sections
EXEMESTANE HUMAN PRESCRIPTION DRUG LABEL 1 69097-316 TABLET 25 mg ORAL ANDA 22 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 70771-1374 TABLET 25 mg ORAL ANDA 1 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 70771-1374 TABLET 25 mg ORAL ANDA 1 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 71921-190 TABLET, FILM COATED 25 mg ORAL ANDA 28 sections