> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/exemestane-367c47e6-e892-496e-bbb5-5b4926a3c31a
> Record changed: 2026-10-13

# Exemestane

Highest phase reached

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1200374)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1200374)

First approval year

1999

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1200374)

## Development status

**First approval year**

1999

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1200374)

**Listing at source**

Listed

**Highest phase reached**

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1200374)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1200374)

**Drug name**

Exemestane

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1200374)

**Molecular weight**

296.41

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1200374)

**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

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1200374)

### Brand names (4)

- aromasin
- Aromasin
- exemestane
- Exemestane

### Other names (46)

- 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.

## Identifiers

**ATC classification codes**

- L02BG06

Sources for recorded values

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1200374)

**CAS registry numbers**

- 107868-30-4

**ChEMBL ID**

CHEMBL1200374

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1200374)

**InChIKey**

BFYIZQONLCFLEV-DAELLWKTSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1200374)

**PubChem compound IDs**

- 60198

**RxNorm IDs (RxCUI)**

- 258494

**FDA ingredient codes (UNII)**

- NY22HMQ4BX

## Regulatory information

### United States

**Applicant**

PFIZER

**Approval date**

21 Oct 1999

**Application number**

NDA020753

### Other regulatory facts

**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

### Drug classification

**Pharmacology name**

exemestane

**Type**

Synthetic organic

**Drug name stem**

\-mestane

**Approval recorded by Guide to Pharmacology**

Yes

#### Administration routes

- Oral

### Mechanisms of action (2)

- **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

### Investigated indications (17)

- **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

### Open Targets indications (39)

- **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.

### Reported adverse events (30)

- **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.

### Trial references (189)

- NCT00002777  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00002777)
- NCT00003418  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00003418)
- NCT00010010  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00010010)
- NCT00016432  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00016432)
- NCT00032136  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00032136)
- NCT00057993  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00057993)
- NCT00065325  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00065325)
- NCT00066573  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00066573)
- NCT00066703  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00066703)
- NCT00066807  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00066807)
- NCT00080613  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00080613)
- NCT00083174  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00083174)
- NCT00128843  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00128843)
- NCT00194792  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00194792)
- NCT00200174  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00200174)
- NCT00201773  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00201773)
- NCT00201864  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00201864)
- NCT00253422  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00253422)
- NCT00265759  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00265759)
- NCT00432172  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00432172)
- NCT00525096  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00525096)
- NCT00541086  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00541086)
- NCT00573755  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00573755)
- NCT00615524  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00615524)
- NCT00626106  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00626106)

And 164 more, listed on the interactive page.

## Dosing

**Dose**

25mg

**Route**

Oral

**How often**

Once daily

### Conditions of use

- Take after a meal

## Chemical properties

**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

## National Drug Codes

- 0009-7663
- 0832-0595
- 51991-005
- 59651-516
- 68382-383
- 69097-316
- 71921-190
- 72603-329
- 59762-2858
- 63629-2056
- 70771-1374

## Evidence counts

**Recorded assays**

1,169

**Active assays**

77

### Active assay types (4)

- Confirmatory
- Other
- Screening
- Summary

## Pharmacologic actions

- Antineoplastic Agents  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D000970.html)
- Aromatase Inhibitors  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D047072.html)

## 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](https://trialight.com/data/trial/a-phase-iii-trial-comparing-hrs-8080-with-standard-endocrine-e2a57990-1f83-4ce5-bd36-8e94a49c52ad.md)
- 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](https://trialight.com/data/trial/a-study-of-camizestrant-in-er-her2-early-breast-cancer-after-2e9eb478-c398-409a-a2cc-81da5599f650.md)
- 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](https://trialight.com/data/trial/a-study-of-elacestrant-versus-standard-endocrine-therapy-in-dff6c6aa-c4b1-4a1b-95e0-992970dd2c2f.md)
- 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](https://trialight.com/data/trial/a-study-of-imlunestrant-versus-standard-endocrine-therapy-in-1fbe3844-7d64-40a8-8560-9100ec0b3d0f.md)

### Approved for (5)

- [Breast cancer](https://trialight.com/data/condition/breast-cancer-8ac10da3-93bd-54c5-a93b-265bc6699689.md)
- Breast carcinoma
- [Breast neoplasm](https://trialight.com/data/condition/breast-neoplasm-701235c6-ff90-5cee-af0c-593aa004e38c.md)
- [Cancer](https://trialight.com/data/condition/cancer-703b1dfc-4812-50eb-83f4-d7a205d16bdb.md)
- 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](https://trialight.com/data/condition/endometrial-cancer-4da2a0bc-7943-502b-a698-cc2beccbed8c.md) Phase 2
- Female breast carcinoma Phase 3
- [Lung cancer](https://trialight.com/data/condition/lung-cancer-c4ca1fe0-9b3d-5957-a668-2d6cf26bd16a.md) Phase 1
- [Lymphoma](https://trialight.com/data/condition/lymphoma-de4db685-7419-5e0e-b958-4591ffd69d43.md) Phase 1
- Male breast carcinoma Phase 3
- Maligant granulosa cell tumor of ovary Phase 2
- [Non-small cell lung carcinoma](https://trialight.com/data/condition/non-small-cell-lung-carcinoma-a86c1d60-523f-5ea7-a5e1-39ed4a2296f8.md) Phase 2
- [Ovarian cancer](https://trialight.com/data/condition/ovarian-cancer-f64f2018-55a5-553a-8960-76cb4906aa17.md) Phase 3
- [Prostate cancer](https://trialight.com/data/condition/prostate-cancer-3659fc70-617b-5868-a093-ae819ffc6755.md) Phase 2
- [Triple-negative breast carcinoma](https://trialight.com/data/condition/triple-negative-breast-carcinoma-059174a2-9b5f-5234-90b9-4a4fee6eb9bb.md) Phase 2

### Targets (1)

- [CYP19A1](https://trialight.com/data/target/cyp19a1-9682b33b-ed66-55a7-8155-bf00584059c7.md) Cytochrome P450 19A1 inhibitor

---

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