exemestane ๐Ÿถ 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 ยตM/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 1773.67 13.90 961 43608 67163 50493392
Metastases to bone 1244.25 13.90 500 44069 17495 50543060
Metastases to liver 999.83 13.90 442 44127 19662 50540893
Neoplasm progression 798.02 13.90 426 44143 28731 50531824
Osteonecrosis of jaw 583.61 13.90 361 44208 32165 50528390
Disease progression 521.04 13.90 525 44044 95341 50465214
Metastases to lung 427.40 13.90 204 44365 10816 50549739
Stomatitis 378.50 13.90 456 44113 100888 50459667
Tumour marker increased 358.93 13.90 133 44436 3707 50556848
Breast cancer metastatic 348.34 13.90 174 44395 10190 50550365
Metastases to lymph nodes 331.48 13.90 149 44420 6875 50553680
Pneumonitis 311.13 13.90 236 44333 29274 50531281
Drug ineffective 307.84 13.90 171 44398 819162 49741393
Mucosal inflammation 234.62 13.90 229 44340 39913 50520642
Pleural effusion 232.43 13.90 321 44248 81133 50479422
Metastases to skin 190.81 13.90 64 44505 1319 50559236
PIK3CA-activated mutation 189.08 13.90 56 44513 754 50559801
Bone pain 175.18 13.90 212 44357 47017 50513538
Osteonecrosis 173.53 13.90 150 44419 22367 50538188
Breast cancer 171.41 13.90 200 44369 42690 50517865
Lymphoedema 167.89 13.90 103 44466 9019 50551536
Metastases to pleura 158.89 13.90 55 44514 1251 50559304
Breast cancer recurrent 134.05 13.90 66 44503 3742 50556813
Bone disorder 126.75 13.90 116 44453 18636 50541919
Rheumatoid arthritis 126.55 13.90 15 44554 202535 50358020
Metastases to central nervous system 125.00 13.90 93 44476 11189 50549366
Metastases to spine 123.90 13.90 57 44512 2774 50557781
Bone lesion 123.16 13.90 69 44500 5101 50555454
Ascites 115.44 13.90 150 44419 35711 50524844
Bone sequestrum 115.22 13.90 44 44525 1334 50559221
Metastases to peritoneum 114.56 13.90 54 44515 2779 50557776
Palmar-plantar erythrodysaesthesia syndrome 114.28 13.90 113 44456 19985 50540570
Second primary malignancy 111.99 13.90 72 44497 6842 50553713
Hepatic lesion 107.92 13.90 58 44511 3950 50556605
Metastasis 105.88 13.90 59 44510 4316 50556239
General physical health deterioration 102.73 13.90 317 44252 142117 50418438
Off label use 102.13 13.90 163 44406 474263 50086292
Carbohydrate antigen 15-3 increased 101.36 13.90 38 44531 1094 50559461
Neutropenia 97.30 13.90 319 44250 147646 50412909
Nail disorder 96.47 13.90 75 44494 9633 50550922
Therapeutic product effect decreased 96.00 13.90 6 44563 136044 50424511
Ejection fraction decreased 95.91 13.90 99 44470 18421 50542134
Hot flush 94.20 13.90 152 44417 44017 50516538
Exposed bone in jaw 94.02 13.90 47 44522 2753 50557802
Malignant pleural effusion 92.95 13.90 44 44525 2286 50558269
Cough 91.88 13.90 438 44131 240826 50319729
Joint swelling 87.46 13.90 54 44515 245232 50315323
Pseudocirrhosis 86.30 13.90 29 44540 601 50559954
Pleural neoplasm 84.98 13.90 23 44546 218 50560337
Interstitial lung disease 83.55 13.90 160 44409 53016 50507539
Infusion related reaction 81.63 13.90 24 44545 169533 50391022
Hormone receptor positive breast cancer 81.21 13.90 26 44543 460 50560095
Synovitis 80.30 13.90 8 44561 123857 50436698
Lymphangiosis carcinomatosa 74.91 13.90 31 44538 1165 50559390
Injection site pain 69.85 13.90 8 44561 111016 50449539
Hyperglycaemia 67.90 13.90 118 44451 36287 50524268
Lymphadenopathy mediastinal 66.66 13.90 36 44533 2475 50558080
Hypotension 66.04 13.90 66 44503 235403 50325152
Abdominal discomfort 66.04 13.90 64 44505 231577 50328978
Aphthous ulcer 64.77 13.90 62 44507 10535 50550020
Gamma-glutamyltransferase increased 63.23 13.90 102 44467 29521 50531034
Eastern Cooperative Oncology Group performance status worsened 62.94 13.90 23 44546 615 50559940
Skin toxicity 61.53 13.90 40 44529 3873 50556682
Neuropathy peripheral 59.45 13.90 204 44365 96553 50464002
Osteolysis 57.86 13.90 33 44536 2524 50558031
Polyneuropathy 57.73 13.90 62 44507 12069 50548486
Gingival swelling 57.73 13.90 38 44531 3757 50556798
Arthropathy 57.30 13.90 34 44535 157872 50402683
Tooth extraction 57.18 13.90 54 44515 9021 50551534
Glossodynia 56.26 13.90 16 44553 115553 50445002
Device related thrombosis 56.21 13.90 26 44543 1281 50559274
Treatment failure 55.29 13.90 26 44543 137611 50422944
Epistaxis 54.33 13.90 151 44418 63803 50496752
Decreased appetite 52.87 13.90 330 44239 200593 50359962
Abdominal lymphadenopathy 50.74 13.90 20 44549 661 50559894
Sinusitis 47.57 13.90 48 44521 170510 50390045
Toxicity to various agents 47.49 13.90 71 44498 212428 50348127
Overdose 46.38 13.90 15 44554 99712 50460843
Metastases to chest wall 46.30 13.90 17 44552 461 50560094
Fall 45.85 13.90 147 44422 334785 50225770
Injection site erythema 45.65 13.90 6 44563 74930 50485625
Oral pain 45.19 13.90 80 44489 24953 50535602
Discomfort 44.26 13.90 20 44549 108360 50452195
Peritoneal disorder 43.64 13.90 16 44553 432 50560123
Dysgeusia 43.57 13.90 102 44467 38814 50521741
Intentional overdose 43.35 13.90 3 44566 62501 50498054
Lung infiltration 43.05 13.90 56 44513 13337 50547218
Product dose omission issue 41.48 13.90 61 44508 183777 50376778
Oral cavity fistula 41.40 13.90 17 44552 626 50559929
Blood lactate dehydrogenase increased 41.25 13.90 67 44502 19495 50541060
Drug hypersensitivity 41.11 13.90 101 44468 250909 50309646
Weight decreased 41.06 13.90 334 44235 220911 50339644
Hepatic failure 41.03 13.90 89 44480 32194 50528361
Osteitis 40.66 13.90 28 44541 2982 50557573
Hypersensitivity 40.64 13.90 80 44489 215081 50345474
Intentional product use issue 40.62 13.90 9 44560 76909 50483646
Metastases to meninges 40.43 13.90 24 44545 1978 50558577
Therapeutic product effect incomplete 40.43 13.90 15 44554 91500 50469055
Periodontitis 40.17 13.90 28 44541 3041 50557514
Superinfection 39.84 13.90 24 44545 2032 50558523
Osteomyelitis 39.79 13.90 71 44498 22282 50538273
Fatigue 39.52 13.90 856 43713 706745 49853810
Pulmonary mass 39.35 13.90 64 44505 18641 50541914
Metastases to the mediastinum 39.27 13.90 15 44554 455 50560100
Metastases to pelvis 39.16 13.90 14 44555 351 50560204
Invasive ductal breast carcinoma 38.78 13.90 36 44533 5885 50554670
Gingival erythema 38.47 13.90 16 44553 609 50559946
Swelling 37.67 13.90 75 44494 200797 50359758
Invasive lobular breast carcinoma 37.28 13.90 16 44553 659 50559896
Metastases to soft tissue 37.08 13.90 11 44558 149 50560406
Metastases to adrenals 36.85 13.90 16 44553 678 50559877
Lymphadenopathy 36.62 13.90 87 44482 33412 50527143
Sequestrectomy 34.37 13.90 16 44553 800 50559755
Aspartate aminotransferase increased 34.36 13.90 148 44421 77850 50482705
Creutzfeldt-Jakob disease 33.74 13.90 10 44559 135 50560420
Haematotoxicity 33.50 13.90 38 44531 7857 50552698
Blood alkaline phosphatase increased 33.25 13.90 90 44479 37436 50523119
Bradycardia 33.10 13.90 8 44561 64418 50496137
Wound 32.78 13.90 27 44542 105767 50454788
Hepatic enzyme increased 32.55 13.90 44 44525 137336 50423219
Blood creatinine increased 32.40 13.90 143 44426 76017 50484538
Confusional state 31.87 13.90 73 44496 185855 50374700
Irritable bowel syndrome 31.62 13.90 4 44565 51437 50509118
Psoriatic arthropathy 30.56 13.90 3 44566 47029 50513526
Anaemia 30.42 13.90 348 44221 252108 50308447
Jaw disorder 30.35 13.90 29 44540 4914 50555641
Condition aggravated 30.03 13.90 147 44422 296911 50263644
Somnolence 29.79 13.90 57 44512 154928 50405627
Purulent discharge 29.66 13.90 27 44542 4305 50556250
Musculoskeletal stiffness 29.59 13.90 42 44527 128439 50432116
Fibrous histiocytoma 29.09 13.90 12 44557 447 50560108
Dyspnoea 28.74 13.90 657 43912 546951 50013604
C-reactive protein increased 27.65 13.90 124 44445 66350 50494205
Radiation skin injury 27.55 13.90 14 44555 849 50559706
Pericardial effusion 27.48 13.90 66 44503 25523 50535032
Blister 27.47 13.90 21 44548 85397 50475158
Breast cancer female 27.39 13.90 32 44537 6830 50553725
Multiple sclerosis relapse 27.25 13.90 3 44566 42961 50517594
Weight increased 26.62 13.90 90 44479 201801 50358754
Carcinoid tumour pulmonary 26.61 13.90 11 44558 412 50560143
Pain in jaw 26.23 13.90 84 44485 38344 50522211
Adverse drug reaction 26.21 13.90 8 44561 55214 50505341
Pathological fracture 26.07 13.90 33 44536 7649 50552906
Gingivitis 25.85 13.90 32 44537 7252 50553303
Ill-defined disorder 25.80 13.90 8 44561 54646 50505909
Metastases to thorax 25.58 13.90 9 44560 215 50560340
Tumour marker abnormal 25.39 13.90 9 44560 220 50560335
Myocardial infarction 24.86 13.90 25 44544 89002 50471553
Feeding disorder 24.65 13.90 38 44531 10575 50549980
Hospitalisation 24.10 13.90 15 44554 67922 50492633
Mouth swelling 24.09 13.90 23 44546 3893 50556662
Pancreatic neoplasm 24.08 13.90 12 44557 698 50559857
Product use issue 23.78 13.90 61 44508 149414 50411141
Hepatic atrophy 23.75 13.90 9 44560 267 50560288
Mouth ulceration 23.62 13.90 66 44503 27958 50532597
Hallucination 23.56 13.90 6 44563 46651 50513904
Debridement 23.46 13.90 14 44555 1165 50559390
Uterine mass 23.41 13.90 9 44560 278 50560277
Excessive granulation tissue 23.38 13.90 12 44557 743 50559812
Oedema peripheral 23.35 13.90 227 44342 157734 50402821
Tremor 23.20 13.90 41 44528 114862 50445693
Pulmonary tumour thrombotic microangiopathy 23.18 13.90 6 44563 47 50560508
Wrong technique in product usage process 23.04 13.90 10 44559 55500 50505055
Incorrect dose administered 23.01 13.90 7 44562 48407 50512148
Mobility decreased 22.85 13.90 22 44547 79926 50480629
Trigger finger 22.84 13.90 22 44547 3766 50556789
Loss of personal independence in daily activities 22.80 13.90 17 44552 70033 50490522
Asthenia 22.77 13.90 401 44168 318641 50241914
Nail dystrophy 22.57 13.90 12 44557 799 50559756
Mucosal dryness 22.56 13.90 18 44551 2399 50558156
Tumour marker decreased 22.06 13.90 6 44563 58 50560497
Axillary pain 22.02 13.90 15 44554 1569 50558986
Erysipelas 21.81 13.90 28 44541 6580 50553975
Medication error 21.73 13.90 3 44566 36101 50524454
Cancer pain 21.49 13.90 18 44551 2569 50557986
Suicidal ideation 21.41 13.90 11 44558 55374 50505181
Adverse event 21.40 13.90 6 44563 43757 50516798
Urticaria 21.28 13.90 52 44517 129509 50431046
Cardiac failure 21.28 13.90 127 44442 75913 50484642
Neoplasm malignant 21.13 13.90 57 44512 23658 50536897
Osteopenia 20.58 13.90 46 44523 16972 50543583
Actinomycosis 20.58 13.90 12 44557 957 50559598
Blood glucose increased 20.53 13.90 120 44449 71204 50489351
Periodontal disease 20.29 13.90 14 44555 1496 50559059
Cell marker increased 20.28 13.90 8 44561 265 50560290
Concomitant disease aggravated 20.26 13.90 30 44539 8061 50552494
Hepatic function abnormal 20.13 13.90 69 44500 32612 50527943
Radiation fibrosis 19.94 13.90 5 44564 34 50560521
Skin lesion 19.70 13.90 60 44509 26667 50533888
Leukopenia 19.68 13.90 114 44455 67414 50493141
Coma 19.57 13.90 13 44556 56866 50503689
Drug interaction 19.45 13.90 100 44469 199521 50361034
Acne 19.40 13.90 49 44520 19546 50541009
Contusion 19.24 13.90 44 44525 112139 50448416
Radioisotope scan 19.14 13.90 4 44565 10 50560545
Ocular vasculitis 19.12 13.90 5 44564 41 50560514
Cardio-respiratory arrest 18.98 13.90 12 44557 53880 50506675
Suicide attempt 18.94 13.90 11 44558 51721 50508834
Fibromyalgia 18.83 13.90 8 44561 44970 50515585
Diarrhoea 18.79 13.90 663 43906 587813 49972742
Onychoclasis 18.72 13.90 23 44546 5173 50555382
Psoriasis 18.56 13.90 20 44549 68980 50491575
Recurrent cancer 18.38 13.90 14 44555 1743 50558812
Carcinoembryonic antigen increased 18.25 13.90 13 44556 1461 50559094
Lung disorder 18.20 13.90 83 44486 44716 50515839
Thrombocytopenia 18.14 13.90 182 44387 127491 50433064
Oral disorder 18.10 13.90 28 44541 7816 50552739
Folliculitis 18.05 13.90 6 44563 39219 50521336
Unevaluable event 18.03 13.90 9 44560 46057 50514498
Product use in unapproved indication 17.85 13.90 48 44521 115771 50444784
Heart rate decreased 17.85 13.90 5 44564 36492 50524063
Arthralgia 17.85 13.90 509 44060 438193 50122362
Bone debridement 17.71 13.90 7 44562 233 50560322
Congestive cardiomyopathy 17.62 13.90 23 44546 5495 50555060
Sedation 17.38 13.90 3 44566 30607 50529948
Lacrimation increased 17.36 13.90 43 44526 16949 50543606
Peripheral sensory neuropathy 17.31 13.90 25 44544 6566 50553989
Hip arthroplasty 17.24 13.90 3 44566 30426 50530129
Hilar lymphadenopathy 17.19 13.90 11 44558 1036 50559519
Fibrin D dimer increased 17.18 13.90 20 44549 4252 50556303
Biopsy site unspecified abnormal 17.16 13.90 4 44565 19 50560536
Heart rate increased 17.05 13.90 26 44543 77224 50483331
Loss of consciousness 17.04 13.90 42 44527 104311 50456244
Lymphangitis 17.00 13.90 10 44559 810 50559745
Lymphatic obstruction 16.99 13.90 4 44565 20 50560535
Bone neoplasm 16.98 13.90 9 44560 596 50559959
Bronchitis 16.95 13.90 42 44527 104117 50456438
Abscess jaw 16.87 13.90 12 44557 1346 50559209
Neoplasm recurrence 16.68 13.90 15 44554 2354 50558201
Cell-mediated immune deficiency 16.68 13.90 4 44565 22 50560533
Dermatitis 16.65 13.90 38 44531 14213 50546342
Metastases to bone marrow 16.57 13.90 7 44562 277 50560278
Hiccups 16.34 13.90 13 44556 1726 50558829
Gastrointestinal disorder 16.24 13.90 37 44532 94419 50466136
Breast pain 16.12 13.90 26 44543 7518 50553037
Bone marrow tumour cell infiltration 16.11 13.90 4 44565 26 50560529
Pleural mass 16.03 13.90 3 44566 3 50560552
Pustule 16.01 13.90 11 44558 1167 50559388
Metastases to bladder 15.99 13.90 6 44563 173 50560382
Fractured sacrum 15.95 13.90 13 44556 1785 50558770
Wound treatment 15.93 13.90 6 44563 175 50560380
Nasopharyngitis 15.91 13.90 102 44467 192825 50367730
Fingerprint loss 15.85 13.90 4 44565 28 50560527
Blood phosphorus decreased 15.68 13.90 18 44551 3771 50556784
Exostosis of jaw 15.67 13.90 11 44558 1208 50559347
Blood pressure fluctuation 15.60 13.90 6 44563 35817 50524738
Fluid retention 15.59 13.90 13 44556 50636 50509919
Pneumonitis chemical 15.55 13.90 6 44563 187 50560368
Drug intolerance 15.55 13.90 121 44448 218983 50341572
Metastases to abdominal wall 15.48 13.90 5 44564 91 50560464
Dry skin 15.36 13.90 77 44492 43114 50517441
Blood pressure decreased 15.27 13.90 16 44553 55893 50504662
Metastases to ovary 15.17 13.90 7 44562 343 50560212
Alanine aminotransferase increased 15.08 13.90 131 44438 88228 50472327
Congenital haematological disorder 15.07 13.90 4 44565 35 50560520
Aortic arteriosclerosis 15.00 13.90 21 44548 5361 50555194
Respiratory arrest 14.88 13.90 4 44565 30005 50530550
Nail infection 14.86 13.90 13 44556 1968 50558587
Recall phenomenon 14.84 13.90 8 44561 548 50560007
Ascariasis 14.82 13.90 3 44566 6 50560549
Corneal epithelial microcysts 14.82 13.90 3 44566 6 50560549
Radiation pneumonitis 14.77 13.90 11 44558 1324 50559231
Hyperbaric oxygen therapy 14.77 13.90 4 44565 38 50560517
Hyperparathyroidism secondary 14.66 13.90 11 44558 1339 50559216
Computerised tomogram abnormal 14.56 13.90 13 44556 2021 50558534
Red blood cell sedimentation rate increased 14.44 13.90 4 44565 29412 50531143
Alveolar lung disease 14.43 13.90 5 44564 114 50560441
Cardiomyopathy 14.43 13.90 38 44531 15548 50545007
Breast inflammation 14.35 13.90 5 44564 116 50560439
Skin mass 14.26 13.90 20 44549 5115 50555440
Encephalopathy 14.10 13.90 6 44563 33705 50526850
Depressed level of consciousness 14.04 13.90 15 44554 51938 50508617
Rib fracture 14.02 13.90 43 44526 19178 50541377
Metastases to eye 13.92 13.90 5 44564 127 50560428

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 1005.04 14.46 380 31992 20055 64446305
Malignant neoplasm progression 870.14 14.46 597 31775 112274 64354086
Metastases to liver 652.86 14.46 292 32080 23649 64442711
Neoplasm progression 641.68 14.46 342 32030 40622 64425738
Osteonecrosis of jaw 410.01 14.46 253 32119 39572 64426788
Disease progression 363.69 14.46 400 31972 141280 64325080
Metastases to lung 328.19 14.46 158 32214 15106 64451254
Stomatitis 308.44 14.46 325 32047 109280 64357080
Metastases to lymph nodes 291.95 14.46 123 32249 8594 64457766
Breast cancer metastatic 290.68 14.46 116 32256 7053 64459307
Tumour marker increased 263.48 14.46 89 32283 3361 64462999
Pneumonitis 179.60 14.46 170 32202 50195 64416165
Metastases to skin 174.97 14.46 53 32319 1399 64464961
Mucosal inflammation 166.00 14.46 180 32192 62404 64403956
Breast cancer 162.29 14.46 127 32245 29021 64437339
Drug ineffective 130.82 14.46 138 32234 840109 63626251
Bone pain 129.94 14.46 139 32233 47433 64418927
Pleural effusion 126.04 14.46 227 32145 126332 64340028
Osteonecrosis 125.67 14.46 108 32264 28121 64438239
PIK3CA-activated mutation 121.86 14.46 32 32340 493 64465867
Nail disorder 120.94 14.46 67 32305 8557 64457803
Lymphoedema 114.91 14.46 68 32304 9837 64456523
Hot flush 108.86 14.46 125 32247 46110 64420250
Carbohydrate antigen 15-3 increased 97.74 14.46 31 32341 956 64465404
Bone disorder 97.57 14.46 75 32297 16684 64449676
Pseudocirrhosis 97.22 14.46 28 32344 617 64465743
Breast cancer recurrent 95.07 14.46 39 32333 2544 64463816
Pleural neoplasm 87.60 14.46 21 32351 218 64466142
Bone lesion 86.29 14.46 45 32327 5092 64461268
Fatigue 84.25 14.46 652 31720 748078 63718282
Metastases to pleura 82.50 14.46 29 32343 1235 64465125
Exposed bone in jaw 80.73 14.46 38 32334 3449 64462911
Cough 78.73 14.46 330 32042 301818 64164542
Ejection fraction decreased 78.58 14.46 84 32288 28623 64437737
Hypotension 77.19 14.46 48 32324 380926 64085434
Metastases to spine 73.13 14.46 36 32336 3607 64462753
Metastases to central nervous system 71.81 14.46 58 32314 13854 64452506
Hepatic lesion 67.59 14.46 40 32332 5784 64460576
Second primary malignancy 67.02 14.46 53 32319 12284 64454076
Off label use 65.08 14.46 138 32234 632668 63833692
Neuropathy peripheral 60.82 14.46 162 32210 117363 64348997
Metastases to peritoneum 59.37 14.46 31 32341 3516 64462844
Device related thrombosis 58.59 14.46 26 32346 2059 64464301
Hormone receptor positive breast cancer 57.89 14.46 16 32356 302 64466058
Tooth extraction 55.96 14.46 43 32329 9558 64456802
Toxicity to various agents 55.95 14.46 60 32312 363453 64102907
Aphthous ulcer 54.64 14.46 48 32324 12858 64453502
Drug abuse 54.21 14.46 3 32369 132371 64333989
Malignant pleural effusion 52.74 14.46 27 32345 2940 64463420
Lymphangiosis carcinomatosa 52.11 14.46 23 32349 1798 64464562
Lymphadenopathy mediastinal 51.31 14.46 29 32343 3847 64462513
Neutropenia 51.28 14.46 247 32125 239377 64226983
Oral pain 51.14 14.46 66 32306 27427 64438933
Ascites 50.29 14.46 102 32270 61899 64404461
Osteolysis 48.35 14.46 25 32347 2778 64463582
Rheumatoid arthritis 47.41 14.46 12 32360 164282 64302078
Peritoneal disorder 46.64 14.46 16 32356 633 64465727
Overdose 45.38 14.46 12 32360 159554 64306806
Bone sequestrum 44.17 14.46 18 32354 1154 64465206
Metastasis 43.40 14.46 30 32342 5665 64460695
Therapeutic product effect decreased 43.25 14.46 4 32368 115347 64351013
Interstitial lung disease 42.96 14.46 127 32245 97605 64368755
Metastases to the mediastinum 41.65 14.46 14 32358 520 64465840
Acute kidney injury 39.69 14.46 106 32266 449134 64017226
Bradycardia 39.63 14.46 6 32366 118213 64348147
Arthralgia 38.82 14.46 365 32007 441895 64024465
Palmar-plantar erythrodysaesthesia syndrome 38.44 14.46 59 32313 28760 64437600
Oral cavity fistula 38.42 14.46 14 32358 662 64465698
Abdominal lymphadenopathy 38.06 14.46 16 32356 1110 64465250
Creutzfeldt-Jakob disease 37.05 14.46 10 32362 172 64466188
Decreased appetite 36.55 14.46 254 32118 281035 64185325
Dysgeusia 36.50 14.46 76 32296 46971 64419389
Superinfection 35.71 14.46 23 32349 3863 64462497
Infusion related reaction 35.70 14.46 19 32353 164448 64301912
Asthenia 34.48 14.46 347 32025 427697 64038663
Injection site pain 34.41 14.46 7 32365 111401 64354959
Intentional overdose 34.04 14.46 3 32369 89941 64376419
Metastases to soft tissue 33.46 14.46 11 32361 381 64465979
Trigger finger 32.62 14.46 21 32351 3524 64462836
Invasive ductal breast carcinoma 32.53 14.46 24 32348 5018 64461342
Sequestrectomy 31.86 14.46 13 32359 836 64465524
Hyperglycaemia 31.47 14.46 84 32288 60884 64405476
Weight decreased 31.41 14.46 248 32124 285491 64180869
Synovitis 31.07 14.46 6 32366 99084 64367276
Skin toxicity 30.88 14.46 26 32346 6576 64459784
Gingival swelling 30.70 14.46 21 32351 3899 64462461
Metastases to eye 30.48 14.46 9 32363 217 64466143
Joint swelling 30.45 14.46 38 32334 215344 64251016
Fibrous histiocytoma 30.03 14.46 11 32361 528 64465832
Metastases to chest wall 29.51 14.46 10 32362 381 64465979
Myocardial infarction 29.44 14.46 24 32348 165797 64300563
Nail dystrophy 28.99 14.46 12 32360 801 64465559
Pathological fracture 27.59 14.46 28 32344 8977 64457383
Drug interaction 27.23 14.46 92 32280 361991 64104369
Mouth ulceration 27.04 14.46 54 32318 32390 64433970
Tumour marker abnormal 27.01 14.46 8 32364 195 64466165
Lacrimation increased 26.52 14.46 39 32333 18307 64448053
Pulmonary mass 26.35 14.46 45 32327 23971 64442389
Fall 26.14 14.46 114 32258 416712 64049648
Mouth swelling 25.74 14.46 21 32351 5086 64461274
Intentional product use issue 25.58 14.46 8 32364 95356 64371004
Osteitis 25.09 14.46 18 32354 3604 64462756
Cardio-respiratory arrest 25.09 14.46 9 32363 98384 64367976
Pain in jaw 25.05 14.46 60 32312 40695 64425665
Confusional state 24.26 14.46 60 32312 261084 64205276
Radioisotope scan 24.15 14.46 4 32368 3 64466357
Alopecia 24.13 14.46 154 32218 165536 64300824
Lung disorder 23.97 14.46 76 32296 60624 64405736
Hallucination 23.70 14.46 4 32368 72784 64393576
Pulmonary tumour thrombotic microangiopathy 23.38 14.46 6 32366 84 64466276
Axillary pain 23.04 14.46 13 32359 1719 64464641
Pancreatic neoplasm 22.80 14.46 12 32360 1383 64464977
Radiation fibrosis 22.37 14.46 5 32367 37 64466323
Oral herpes 22.34 14.46 40 32332 22112 64444248
Nail infection 22.26 14.46 13 32359 1834 64464526
General physical health deterioration 22.21 14.46 177 32195 204248 64262112
Osteomyelitis 21.90 14.46 45 32327 27542 64438818
Diarrhoea 21.90 14.46 495 31877 722209 63744151
Metastases to meninges 21.85 14.46 15 32357 2800 64463560
Blood alkaline phosphatase increased 21.80 14.46 70 32302 56209 64410151
Cell marker increased 21.29 14.46 9 32363 633 64465727
Hepatic atrophy 21.27 14.46 8 32364 414 64465946
Debridement 21.08 14.46 12 32360 1614 64464746
Breast mass 20.99 14.46 19 32353 5291 64461069
Therapeutic product effect incomplete 20.96 14.46 13 32359 103469 64362891
Rhabdomyolysis 20.79 14.46 10 32362 91716 64374644
Pustule 20.22 14.46 11 32361 1354 64465006
Epistaxis 20.11 14.46 100 32272 98031 64368329
Breast cancer female 19.66 14.46 18 32354 5085 64461275
Fractured sacrum 19.43 14.46 11 32361 1464 64464896
Treatment failure 19.40 14.46 18 32354 116798 64349562
Carcinoid tumour pulmonary 19.31 14.46 7 32365 326 64466034
Nipple exudate bloody 19.29 14.46 5 32367 73 64466287
Metastases to thorax 19.23 14.46 6 32366 175 64466185
Vaginal discharge 19.23 14.46 16 32356 3981 64462379
Coma 19.18 14.46 10 32362 87605 64378755
Nausea 18.97 14.46 522 31850 785278 63681082
Injection site erythema 18.88 14.46 6 32366 70794 64395566
Periodontitis 18.68 14.46 16 32356 4143 64462217
White blood cell count decreased 18.43 14.46 139 32233 157698 64308662
Periodontal disease 18.03 14.46 11 32361 1680 64464680
Somnolence 17.98 14.46 48 32324 203597 64262763
Mucosal ulceration 17.82 14.46 11 32361 1716 64464644
Progesterone receptor assay positive 17.64 14.46 6 32366 231 64466129
Bone neoplasm 17.36 14.46 8 32364 692 64465668
Congenital haematological disorder 17.30 14.46 4 32368 35 64466325
Loss of consciousness 17.22 14.46 30 32342 148335 64318025
Cardiac arrest 17.12 14.46 32 32340 154032 64312328
Teeth brittle 17.03 14.46 7 32365 459 64465901
Recurrent cancer 16.91 14.46 12 32360 2361 64463999
Gingivitis 16.83 14.46 20 32352 7639 64458721
Haematotoxicity 16.63 14.46 26 32346 12870 64453490
Dry skin 16.62 14.46 60 32312 51101 64415259
Feeding disorder 16.55 14.46 26 32346 12923 64453437
Ascariasis 16.50 14.46 3 32369 6 64466354
Back pain 16.48 14.46 195 32177 249976 64216384
Incorrect dose administered 16.47 14.46 5 32367 60760 64405600
Breast pain 16.45 14.46 19 32353 7042 64459318
Tremor 16.29 14.46 31 32341 148199 64318161
Lymphadenopathy 16.24 14.46 56 32316 46630 64419730
Tumour marker decreased 16.16 14.46 4 32368 48 64466312
Metastases to pelvis 16.06 14.46 7 32365 531 64465829
Exostosis of jaw 15.98 14.46 9 32363 1185 64465175
Heart rate decreased 15.92 14.46 4 32368 55063 64411297
Hydrothorax 15.55 14.46 9 32363 1248 64465112
Arthropathy 15.41 14.46 23 32349 120944 64345416
Pericardial effusion 15.36 14.46 49 32323 39205 64427155
Acne 15.29 14.46 35 32337 23046 64443314
Dyspnoea 15.29 14.46 470 31902 718204 63748156
Actinomycosis 15.10 14.46 8 32364 934 64465426
Sinusitis 14.77 14.46 32 32340 145896 64320464
Skin mass 14.71 14.46 18 32354 7088 64459272
Recall phenomenon 14.61 14.46 8 32364 998 64465362
Carcinoembryonic antigen increased 14.59 14.46 10 32362 1863 64464497
Blood pressure fluctuation 14.55 14.46 4 32368 51867 64414493
Hospitalisation 14.48 14.46 10 32362 75197 64391163

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 (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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ 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
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 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 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
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 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 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 71921-190 TABLET, FILM COATED 25 mg ORAL ANDA 28 sections
Exemestane HUMAN PRESCRIPTION DRUG LABEL 1 71921-190 TABLET, FILM COATED 25 mg ORAL ANDA 28 sections