Exemestane
Aromasin, Exemestane (exemestane) is a small molecule pharmaceutical. Exemestane was first approved as Aromasin on 1999-10-21. It is used to treat breast neoplasms in the USA. The pharmaceutical is active against aromatase.
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Commercial
Therapeutic Areas
Therapeutic Area | MeSH |
|---|---|
| neoplasms | D009369 |
| skin and connective tissue diseases | D017437 |
Trade Name
FDA
EMA
Aromasin, Exemestane (discontinued: Exemestane)
Labels
FDA
EMA
Brand Name | Status | Last Update |
|---|---|---|
| aromasin | New Drug Application | 2023-09-08 |
| exemestane | ANDA | 2024-05-29 |
Indications
FDA
EMA
Indication | Ontology | MeSH | ICD-10 |
|---|---|---|---|
| breast neoplasms | EFO_0003869 | D001943 | C50 |
Agency Specific
FDA
EMA
No data
Patent Expiration
No data
HCPCS
Code | Description |
|---|---|
| S0156 | Exemestane, 25 mg |
Clinical
Clinical Trials
353 clinical trials
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Indications Phases 4
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Breast neoplasms | D001943 | EFO_0003869 | C50 | 33 | 151 | 87 | 12 | 62 | 330 |
| Neoplasms | D009369 | — | C80 | 6 | 8 | 2 | 1 | 2 | 18 |
| Triple negative breast neoplasms | D064726 | — | — | 1 | 8 | 3 | 1 | — | 13 |
| Osteoporosis | D010024 | HP_0000939 | M81.0 | — | — | 1 | 1 | 3 | 5 |
| Arthralgia | D018771 | HP_0002829 | M25.5 | — | — | — | 1 | 3 | 4 |
| Postmenopause | D017698 | — | — | — | 2 | — | 1 | 1 | 4 |
| Invasive hydatidiform mole | D002820 | — | D39.2 | 1 | — | 1 | 1 | 1 | 4 |
| Breast carcinoma in situ | D000071960 | — | D05 | — | 1 | 1 | 1 | — | 3 |
| Osteoporotic fractures | D058866 | — | — | — | — | — | 1 | — | 1 |
| Sexuality | D019529 | — | — | — | — | — | 1 | — | 1 |
Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Carcinoma | D002277 | — | C80.0 | 3 | 7 | 3 | — | — | 13 |
| Male breast neoplasms | D018567 | — | — | 2 | 4 | 3 | — | 3 | 12 |
| Recurrence | D012008 | — | — | — | 7 | 3 | — | 1 | 11 |
| Carcinoma in situ | D002278 | — | D09.9 | 1 | 2 | 1 | — | — | 4 |
| Intraductal carcinoma noninfiltrating | D002285 | — | D05.1 | 1 | 1 | 1 | — | 1 | 4 |
| Ovarian neoplasms | D010051 | EFO_0003893 | C56 | — | 2 | 1 | — | — | 3 |
| Ovarian epithelial carcinoma | D000077216 | — | — | — | 2 | 1 | — | — | 3 |
| Disease progression | D018450 | — | — | — | 1 | 1 | — | 1 | 3 |
| Adenocarcinoma | D000230 | — | — | — | 1 | 2 | — | — | 3 |
| Ductal carcinoma | D044584 | — | — | 1 | 1 | 1 | — | — | 3 |
Show 9 more
Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Non-small-cell lung carcinoma | D002289 | — | — | 2 | 1 | — | — | — | 3 |
| Lung neoplasms | D008175 | HP_0100526 | C34.90 | 2 | 1 | — | — | — | 3 |
| Endometrial neoplasms | D016889 | EFO_0004230 | — | 1 | 2 | — | — | — | 3 |
| Breast diseases | D001941 | — | N60-N65 | — | 2 | — | — | — | 2 |
| Sarcoma | D012509 | — | — | — | 2 | — | — | — | 2 |
| Prostatic neoplasms | D011471 | — | C61 | — | 2 | — | — | — | 2 |
| Urologic neoplasms | D014571 | — | C64-C68 | — | 1 | — | — | — | 1 |
| Urinary bladder neoplasms | D001749 | — | C67 | — | 1 | — | — | — | 1 |
| Transitional cell carcinoma | D002295 | — | — | — | 1 | — | — | — | 1 |
| Menopause | D008593 | EFO_0003922 | N95 | — | 1 | — | — | — | 1 |
Show 15 more
Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Obesity | D009765 | EFO_0001073 | E66.9 | 1 | — | — | — | 2 | 3 |
| Renal cell carcinoma | D002292 | EFO_0000376 | — | 1 | — | — | — | — | 1 |
| Kidney neoplasms | D007680 | EFO_0003865 | C64 | 1 | — | — | — | — | 1 |
| Neuroendocrine tumors | D018358 | EFO_1001901 | D3A.8 | 1 | — | — | — | — | 1 |
| Lymphoma | D008223 | — | C85.9 | 1 | — | — | — | — | 1 |
| Healthy volunteers/patients | — | — | — | 1 | — | — | — | — | 1 |
Indications Without Phase
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Pain | D010146 | EFO_0003843 | R52 | — | — | — | — | 2 | 2 |
| Lung diseases | D008171 | HP_0002088 | J98.4 | — | — | — | — | 1 | 1 |
| Interstitial lung diseases | D017563 | HP_0006530 | J84.89 | — | — | — | — | 1 | 1 |
| Pregnancy rate | D018873 | — | — | — | — | — | — | 1 | 1 |
| Infertility | D007246 | HP_0000789 | — | — | — | — | — | 1 | 1 |
| Vitamin d deficiency | D014808 | EFO_0003762 | E55 | — | — | — | — | 1 | 1 |
| Drug-related side effects and adverse reactions | D064420 | — | T88.7 | — | — | — | — | 1 | 1 |
| Nutrition disorders | D009748 | EFO_0001069 | — | — | — | — | — | 1 | 1 |
| Periodontal diseases | D010510 | — | K05.6 | — | — | — | — | 1 | 1 |
| Xerostomia | D014987 | — | K11.7 | — | — | — | — | 1 | 1 |
Show 7 more
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | Exemestane |
| INN | exemestane |
| Description | Exemestane is a 17-oxo steroid that is androsta-1,4-diene-3,17-dione in which the hydrogens at position 6 are replaced by a double bond to a methylene group. A selective inhibitor of the aromatase (oestrogen synthase) system, it is used in the treatment of advanced breast cancer. It has a role as an EC 1.14.14.14 (aromatase) inhibitor, an antineoplastic agent, an environmental contaminant and a xenobiotic. It is a 17-oxo steroid and a 3-oxo-Delta(1),Delta(4)-steroid. It derives from a hydride of an androstane. |
| Classification | Small molecule |
| Drug class | antineoplastics (aromatase inhibitors) |
| Image (chem structure or protein) |  |
| Structure (InChI/SMILES or Protein Sequence) | C=C1C[C@@H]2[C@H](CC[C@]3(C)C(=O)CC[C@@H]23)[C@@]2(C)C=CC(=O)C=C12 |
Identifiers
| PDB | — |
| CAS-ID | 107868-30-4 |
| RxCUI | — |
| ChEMBL ID | CHEMBL1200374 |
| ChEBI ID | 4953 |
| PubChem CID | 60198 |
| DrugBank | DB00990 |
| UNII ID | NY22HMQ4BX (ChemIDplus, GSRS) |
Target
Agency Approved
CYP19A1
CYP19A1
Organism
Homo sapiens
Gene name
CYP19A1
Gene synonyms
ARO1, CYAR, CYP19
NCBI Gene ID
Protein name
aromatase
Protein synonyms
CYPXIX, Cytochrome P-450AROM, Cytochrome P450 19A1, cytochrome P450, family 19, subfamily A, polypeptide 1, cytochrome P450, subfamily XIX (aromatization of androgens), Estrogen synthase, estrogen synthetase, flavoprotein-linked monooxygenase, microsomal monooxygenase
Uniprot ID
Mouse ortholog
Cyp19a1 (13075)
aromatase (P28649)
Alternate
No data
Variants
No data
Financial
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Aromasin – Pfizer
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Estimated US medical usage
Exemestane
Total medical expenditures per year (USD, in millions)
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Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 7,702 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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13,701 adverse events reported
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