Exemestane (Aromasin)
ex-EM-eh-stayn
Category
Compound type
Phase / Status
FDA approved for breast cancer. Widely used off-label in performance contexts for estrogen management.
Standard Dose
Every other day
Half-life
Plasma elimination
Route(s)
Oral
Research Stage
Regulatory approval granted; post-market monitoring ongoing.
Overview
Exemestane works by inactivating aromatase, the enzyme involved in converting androgens to estrogen. Because estrogen suppression can cause symptoms and affect bone and lipid health, it should be used with appropriate medical monitoring when prescribed.
Plain-language summary
Exemestane works by inactivating aromatase, the enzyme involved in converting androgens to estrogen. Because estrogen suppression can cause symptoms and affect bone and lipid health, it should be used with appropriate medical monitoring when prescribed.
Administration Routes
- Oral
Also known as
Mechanisms
Steroidal suicide aromatase inhibitor - irreversibly deactivates aromatase (CYP19A1) via covalent binding. It's like throwing a brick through the enzyme's window.
Detailed mechanism
Steroidal suicide aromatase inhibitor - irreversibly inactivates aromatase (CYP19A1) enzyme via covalent binding. Modulates cellular pathways and enzyme activity to produce therapeutic effects at the molecular level.
Safety
Side effects
- Joint pain (but less than anastrozole)
- Hot flashes
- Fatigue
- Headache
- Nausea
Reported benefits
- Permanently deactivates aromatase - no estrogen rebound
- Safe for PCT - doesn't interfere with SERMs like Nolvadex
- Mildly androgenic - slightly boosts testosterone and IGF-1
- FDA-approved with solid safety data
- Doesn't mess with cortisol or aldosterone
- Can be stacked with tamoxifen (unlike anastrozole)
Safety profile
Well-characterized safety profile from extensive clinical use and trials.
Clinical trials
Completed clinical trials leading to FDA or regulatory approval.
Structure
Verified structure
Exemestane (Aromasin)
Exact 2D structure can be rendered from a PubChem-backed canonical SMILES string.
- Chemical Formula
- C20H24O2
- Molecular Weight
- 296.40 g/mol
- CAS Number
- 107868-30-4
- InChIKey
- BFYIZQONLCFLEV-DAELLWKTSA-N
Stack Context
Stacks with
References
- 1View source
A randomized trial of exemestane after two to three years of tamoxifen therapy in postmenopausal women with primary breast cancer (IES, NEJM)
2004
- 2View source
Exemestane for breast-cancer prevention in postmenopausal women (MAP.3, NEJM)
2011
- 3View source
Tamoxifen versus exemestane in adjuvant endocrine treatment of postmenopausal women with early breast cancer (TEAM trial, Lancet Oncol)
2011
This profile summarizes research literature for education only. It is not medical advice, and it does not diagnose, treat, or recommend a dose. Consult a qualified professional before changing a protocol.