Exemestane
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| Clinical data | |
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| Trade names | Aromasin |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a607006 |
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| Routes of administration |
Oral |
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| Pharmacokinetic data | |
| Bioavailability | ~60% |
| Protein binding | 90% |
| Metabolism | Liver (CYP3A4, aldo-keto reductase) |
| Biological half-life | 24 hours |
| Duration of action | 4–5 days |
| Excretion | Urine and feces ~ 1:1 (mainly metabolites) |
| Identifiers | |
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| Synonyms | FCE-24304 |
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| ChEMBL | |
| ECHA InfoCard | 100.171.149 |
| Chemical and physical data | |
| Formula | C20H24O2 |
| Molar mass | 296.403 g/mol |
| 3D model (Jmol) | |
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  (what is this?)
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Exemestane (trade name Aromasin) is a drug used to treat breast cancer. It is a member of the class of drugs known as aromatase inhibitors. Some breast cancers require estrogen to grow. Those cancers have estrogen receptors (ERs), and are called ER-positive. They may also be called estrogen-responsive, hormonally-responsive, or hormone-receptor-positive. Aromatase is an enzyme that synthesizes estrogen. Aromatase inhibitors block the synthesis of estrogen. This lowers the estrogen level, and slows the growth of cancers.
Exemestane is indicated for the adjuvant treatment of postmenopausal women with estrogen-receptor positive early breast cancer who have received two to three years of tamoxifen and are switched to it for completion of a total of five consecutive years of adjuvant hormonal therapy. US FDA approval was in October 2005.
Exemestane is also indicated for the treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy.
The drug is contraindicated in premenopausal women, which of course includes pregnant and lactating women.
The most common side effects (more than 10% of patients) are hot flashes and sweating, which are typical of estrogen deficiency as caused by exemestane, and also insomnia, headache, and joint pain. Nausea and fatigue are mainly observed in patients with advanced breast cancer.
Exemestane has androgenic properties similarly to formestane and can produce androgenic side effects such as acne and weight gain, although these are generally associated with supratherapeutic dosages of the drug.
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Wikipedia