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Aromasin (exemestane)
Exemestane irreversibly inhibits aromatase, the enzyme that converts androgens to estrogen in postmenopausal women, thereby reducing circulating estrogen levels.
Exemestane irreversibly inhibits aromatase, the enzyme that converts androgens to estrogen in postmenopausal women, thereby reducing circulating estrogen levels. Used for Hormone receptor-positive breast cancer in postmenopausal women (adjuvant and metastatic settings), Extended adjuvant therapy following tamoxifen in postmenopausal women with early-stage breast cancer.
At a glance
| Generic name | Aromasin (exemestane) |
|---|---|
| Also known as | Aromasin, exemestane |
| Sponsor | Pfizer |
| Drug class | Aromatase inhibitor (steroidal) |
| Target | Aromatase (CYP19A1) |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
Mechanism of action
Aromatase is the primary source of estrogen production in postmenopausal women, and many breast cancers depend on estrogen for growth. By irreversibly binding to and inactivating aromatase, exemestane depletes systemic estrogen, starving estrogen-dependent breast cancer cells. This mechanism is distinct from reversible aromatase inhibitors and represents a steroidal approach to hormone deprivation therapy.
Approved indications
- Hormone receptor-positive breast cancer in postmenopausal women (adjuvant and metastatic settings)
- Extended adjuvant therapy following tamoxifen in postmenopausal women with early-stage breast cancer
Common side effects
- Hot flashes
- Fatigue
- Arthralgia/joint pain
- Headache
- Nausea
- Increased sweating
- Osteoporosis/bone loss
Key clinical trials
- A Study of Elacestrant Versus Standard Endocrine Therapy in Women and Men With ER+,HER2-, Early Breast Cancer With High Risk of Recurrence (PHASE3)
- Testing Whether Hormone Therapy With Ribociclib is as Effective as Chemotherapy Followed by Hormone Therapy With Ribociclib for the Treatment of High Anatomic Stage Breast Cancer With Low Recurrence Risk, The RxFINE-Low Trial (PHASE3)
- Hormone Therapy With or Without Combination Chemotherapy in Treating Women Who Have Undergone Surgery for Node-Negative Breast Cancer (The TAILORx Trial) (PHASE3)
- A Study of LOXO-783 in Patients With Breast Cancer/Other Solid Tumors (PHASE1)
- Tamoxifen Citrate, Letrozole, Anastrozole, or Exemestane With or Without Chemotherapy in Treating Patients With Invasive RxPONDER Breast Cancer (PHASE3)
- Study of Belzutifan (MK-6482) Plus Fulvestrant for ER+/HER2- Metastatic Breast Cancer (MK-6482-029/LITESPARK-029) (PHASE2)
- Ribociclib And Endocrine Treatment of Physician's Choice for Locoregional Recurrent, Resected Hormone Receptor Positive HER2 Negative Breast Cancer (PHASE2)
- A Study of Tersolisib (LY4064809/STX-478) With Other Anti-Cancer Treatments in Participants With Advanced Breast Cancer With a Genetic Change (PIK3CA) (PHASE3)
Primary sources
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| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |