Exemestane
Highest phase reached
Approved
Drug type
Small molecule
First approval year
1999
- First approval year
- 1999
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Exemestane
- Molecular weight
- 296.41
- Structure (SMILES)
- 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
- aromasin
- Aromasin
- exemestane
- Exemestane
- anastrozole letrozole exemestane
- Aromasin
- Aromatase Inhibitors (Aromasin)
- exemestane
- Exemestane
- exemestane (Aromasin)
- exemestane (Aromasin®)
- EXEMESTANE [EP MONOGRAPH]
- EXEMESTANE [HSDB]
- exemestane [INN]
- EXEMESTANE [JAN]
- EXEMESTANE [MART.]
- EXEMESTANE [MI]
- EXEMESTANE [ORANGE BOOK]
- EXEMESTANE [USAN]
- EXEMESTANE [USP MONOGRAPH]
- EXEMESTANE [USP-RS]
- EXEMESTANE [VANDF]
- Exemestane [WHO-DD]
- Exemestane 25 mg
- Exemestane 25 MG
- Exemestane 50 MG
- exemestane ep monograph
- exemestane hsdb
- exemestane inn
And 21 more, listed on the interactive page.
- ATC classification codes
- L02BG06
Sources for recorded values
- CAS registry numbers
- 107868-30-4
- ChEMBL ID
- CHEMBL1200374
- InChIKey
- BFYIZQONLCFLEV-DAELLWKTSA-N
- PubChem compound IDs
- 60198
- RxNorm IDs (RxCUI)
- 258494
- FDA ingredient codes (UNII)
- NY22HMQ4BX
- Applicant
- PFIZER
- Approval date
- 21 Oct 1999
- Application number
- NDA020753
- Patents
- 0
- Designations
- 1
- First in class
- No
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Pharmacology name
- exemestane
- Type
- Synthetic organic
- Drug name stem
- -mestane
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- CYP19A1
- Gene symbol
- CYP19A1
- Protein identifier
- P11511
- Median affinity
- 7.6
- Affinity units
- pKi
- Mechanism
- Cytochrome P450 19A1 inhibitor
- Action type
- Inhibitor
- Target
- Aromatase
- Protein identifier
- P11511
Open Targets mechanisms
- Mechanism
- Cytochrome P450 19A1 inhibitor
- Action type
- Inhibitor
- Target
- Aromatase
DrugCentral mechanisms
- Action type
- Inhibitor
- Gene symbol
- CYP19A1
- Protein identifier
- P11511
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Breast Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000305
- Subject identifier
- D001943
- Condition
- Carcinoma, Intraductal, Noninfiltrating
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000432
- Subject identifier
- D002285
- Condition
- Lymphoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000574
- Subject identifier
- D008223
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Breast Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0003869
- Subject identifier
- D001943
- Condition
- Triple Negative Breast Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0005537
- Subject identifier
- D064726
- Condition
- Breast Neoplasms, Male
- Highest recorded phase
- 3
- Condition identifier
- EFO:0006861
- Subject identifier
- D018567
- Condition
- Endometrial Hyperplasia
- Highest recorded phase
- 2
- Condition identifier
- EFO:1000098
- Subject identifier
- D004714
- Condition
- Breast Carcinoma In Situ
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0004658
- Subject identifier
- D000071960
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0004992
- Subject identifier
- D009369
- Condition
- Breast Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0007254
- Subject identifier
- D001943
- Condition
- Ovarian Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0008170
- Subject identifier
- D010051
- Condition
- Prostatic Neoplasms, Castration-Resistant
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0008315
- Subject identifier
- D064129
- Condition
- Lung Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0008903
- Subject identifier
- D008175
- Condition
- Endometrial Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0011962
- Subject identifier
- D016889
- Condition
- Granulosa Cell Tumor
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0020541
- Subject identifier
- D006106
- Condition identifier
- EFO_0000305
- Condition identifier
- EFO_0000574
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0003060
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003869
- Highest recorded phase
- 3
- Condition identifier
- EFO_0006461
- Highest recorded phase
- 2
- Condition identifier
- EFO_0006861
- Highest recorded phase
- 3
- Condition identifier
- EFO_0009870
- Highest recorded phase
- 2
- Condition identifier
- EFO_1000235
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002146
- Condition identifier
- MONDO_0002447
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004379
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0004658
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004989
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0004992
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005023
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005062
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005070
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005086
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005089
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005140
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005233
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005315
- Condition identifier
- MONDO_0005494
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0006512
- Highest recorded phase
- 1
And 14 more, listed on the interactive page.
- Event
- alopecia
- Reports
- 639
- Reporting signal score
- 501.312
- Event
- arthralgia
- Reports
- 1,386
- Reporting signal score
- 765.913
- Event
- bone pain
- Reports
- 484
- Reporting signal score
- 555.489
- Event
- breast cancer
- Reports
- 743
- Reporting signal score
- 1,385.02
- Event
- breast cancer metastatic
- Reports
- 694
- Reporting signal score
- 2,389.79
- Event
- breast cancer recurrent
- Reports
- 219
- Reporting signal score
- 659.304
- Event
- carbohydrate antigen 15-3 increased
- Reports
- 97
- Reporting signal score
- 362.498
- Event
- disease progression
- Reports
- 792
- Reporting signal score
- 782.053
- Event
- fatigue
- Reports
- 1,437
- Reporting signal score
- 262.387
- Event
- hot flush
- Reports
- 580
- Reporting signal score
- 830.428
- Event
- hyperglycaemia
- Reports
- 73
- Reporting signal score
- 68.9653
- Event
- lymphoedema
- Reports
- 48
- Reporting signal score
- 105.388
- Event
- malignant neoplasm progression
- Reports
- 1,687
- Reporting signal score
- 3,439.35
- Event
- metastases to bone
- Reports
- 932
- Reporting signal score
- 2,764.47
- Event
- metastases to liver
- Reports
- 743
- Reporting signal score
- 2,049
- Event
- metastases to lung
- Reports
- 361
- Reporting signal score
- 881.03
- Event
- metastases to lymph nodes
- Reports
- 272
- Reporting signal score
- 695.901
- Event
- metastases to skin
- Reports
- 85
- Reporting signal score
- 255.875
- Event
- metastases to spine
- Reports
- 118
- Reporting signal score
- 315.521
- Event
- mucosal inflammation
- Reports
- 109
- Reporting signal score
- 144.846
- Event
- nail disorder
- Reports
- 44
- Reporting signal score
- 92.7876
- Event
- neoplasm progression
- Reports
- 774
- Reporting signal score
- 1,655.37
- Event
- neutropenia
- Reports
- 1,371
- Reporting signal score
- 1,379.67
- Event
- pik3ca-activated mutation
- Reports
- 95
- Reporting signal score
- 399.946
- Event
- pleural effusion
- Reports
- 109
- Reporting signal score
- 88.9586
And 5 more, listed on the interactive page.
- NCT00002777
- NCT00003418
- NCT00010010
- NCT00016432
- NCT00032136
- NCT00057993
- NCT00065325
- NCT00066573
- NCT00066703
- NCT00066807
- NCT00080613
- NCT00083174
- NCT00128843
- NCT00194792
- NCT00200174
- NCT00201773
- NCT00201864
- NCT00253422
- NCT00265759
- NCT00432172
- NCT00525096
- NCT00541086
- NCT00573755
- NCT00615524
- NCT00626106
And 164 more, listed on the interactive page.
- Dose
- 25mg
- Route
- Oral
- How often
- Once daily
Conditions of use
- Take after a meal
- Hydrogen bond acceptors
- 2
- Hydrogen bond donors
- 0
- Polar surface area
- 34.14
- Calculated partition coefficient (ALogP)
- 4.03
- Calculated partition coefficient (XLogP)
- 3.1
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 0
- Heavy atoms
- 22
- Molecular formula
- C20H24O2
- Monoisotopic mass
- 296.177630004
- Natural product
- Yes
- 0009-7663
- 0832-0595
- 51991-005
- 59651-516
- 68382-383
- 69097-316
- 71921-190
- 72603-329
- 59762-2858
- 63629-2056
- 70771-1374
- Recorded assays
- 1,169
- Active assays
- 77
- Confirmatory
- Other
- Screening
- Summary
- Antineoplastic Agents
- Aromatase Inhibitors
Related records
Trials (278)
- 1st Line Treatment of Bevacizumab-Taxane vs Bevacizumab-Exemestane in Metastatic Breast Cancer
- 4EVER - Efficacy, Safety, Health Economics, Translational Research of Postmenopausal Women With Estrogen Receptor Positive Locally Advanced or Metastatic Breast Cancer
- A Clinical Study of Darcilil Combined With AI Combined With Pyrrotinib in the Treatment of TPBC
- A Clinical Trial Assessing Efficacy and Safety of Sunitinib and Exemestane in Patients With ER [Estrogen Receptor] + and/or PgR [Progesterone Receptor] + Breast Cancer
- A Non-Interventional Study With Aromasin® As Adjuvant Treatment Of Invasive Early Breast Cancer
- A Phase 3 Study of HRS-8080 Versus Treatment Chosen by Physicians in Locally Advanced and Metastatic Breast Cancer
- A Phase II Study of Everolimus in Combination With Exemestane Versus Everolimus Alone Versus Capecitabine in Advance Breast Cancer.
- A Phase II Trial of Ridaforolimus and Exemestane, Compared to Ridaforolimus, Dalotuzumab and Exemestane in Participants With Breast Cancer (MK-8669-064)
- A Phase III Trial Comparing HRS-8080 With Standard Endocrine Therapy in Patients With Intermediate or High Risk Early Breast Cancer
- A Precision Medicine Approach (SMMART-ACT) for the Treatment of Patients With Advanced Sarcoma, Prostate, Breast, Ovarian or Pancreatic Cancer
- A Randomized, Open-label, Multi-center Phase IV Study Evaluating Palbociclib Plus Endocrine Treatment Versus a Chemotherapy-based Treatment Strategy in Patients With Hormone Receptor Positive / HER2 Negative Breast Cancer in a Real World Setting (GBG 93 - PADMA Study).
- A Study Evaluating Megestrol Acetate Modulation in Hormone Receptor Positive Advanced Breast Cancer
- A Study Evaluating the Efficacy and Safety of Giredestrant Plus Everolimus Compared With the Physician's Choice of Endocrine Therapy Plus Everolimus in Participants With Estrogen Receptor-Positive, HER2-Negative, Locally Advanced or Metastatic Breast Cancer (evERA Breast Cancer)
- A Study for Safety and Effectiveness of IMC-A12 by Itself or Combined With Antiestrogens to Treat Breast Cancer
- A Study of Abiraterone Acetate Plus Prednisone With or Without Exemestane in Postmenopausal Women With Estrogen Receptor-Positive (ER+) Metastatic Breast Cancer Progressing After Letrozole or Anastrozole Therapy
- A Study of Camizestrant in ER+/HER2- Early Breast Cancer After at Least 2 Years of Standard Adjuvant Endocrine Therapy
- A Study of E7090 as Monotherapy and in Combination With Other Anticancer Agents in Participants With Estrogen Receptor Positive (ER+) and Human Epidermal Growth Receptor 2 Negative (HER2-) Recurrent/Metastatic Breast Cancer
- A Study of Elacestrant Versus Standard Endocrine Therapy in Women and Men With ER+,HER2-, Early Breast Cancer With High Risk of Recurrence
- A Study of Everolimus Plus Exemestane in Chinese Postmenopausal Women With Estrogen Receptor Positive, Locally Advanced, Recurrent, or Metastatic Breast Cancer After Recurrence or Progression on Non-steroidal Aromatase Inhibitor
- A Study of Imlunestrant Versus Standard Endocrine Therapy in Participants With Early Breast Cancer
Approved for (5)
- Breast cancer
- Breast carcinoma
- Breast neoplasm
- Cancer
- Neoplasm
In development for (13)
- Atypical endometrial hyperplasia Phase 2
- Breast carcinoma in situ Phase 2
- Ductal breast carcinoma in situ Phase 3
- Endometrial cancer Phase 2
- Female breast carcinoma Phase 3
- Lung cancer Phase 1
- Lymphoma Phase 1
- Male breast carcinoma Phase 3
- Maligant granulosa cell tumor of ovary Phase 2
- Non-small cell lung carcinoma Phase 2
- Ovarian cancer Phase 3
- Prostate cancer Phase 2
- Triple-negative breast carcinoma Phase 2
Targets (1)
- CYP19A1 Cytochrome P450 19A1 inhibitor