Exemestane is a drug belonging to a class of oral steroidal aromatose inhibitors used in the treatment of hormone-receptor positive, or hormonally responsive breast cancer in postmenopausal women. The main goal of hormone receptor positive patients to prevent the recurrence of the cancer is to lower their estrogen levels that the cancer thrives on.
For premenopausal women, the primary source of estrogen is the ovaries. As for post-menopausal women, the body’s estrogen is derived from the adrenal gland via the conversion of androgens into estrogen with the help of the aromatase enzyme.
Exemestane is an irreversible aromatase inactivator, whose main function is to bind to their similarly structured aromatase enzymes, preventing the conversion of androgens into estrogen.
Exemestane is marketed under the brand name Aromasin, is indicated as the adjuvant treatment of postmenopausal women with estrogen-receptor positive early breast cancer who received around two to three years of tamoxifen, and switched to exemestane therapy for a completion of a five consecutive years of adjuvant hormonal therapy.
Exemestane is used for the treatment of advanced breast cancer for postmenopausal women whose conditions progressed after tamoxifen therapy.
The recommended dosage for Exemestane for early and advanced breast cancer is one 25mg tablet, taken once a day after a meal.
For patients taking a potent CYP 3A4 inhibitor such as the likes of rifampicin or phenytoin, the dosage of exemestane is 50mg once a day taken after a meal.
Exemestane is a well-tolerated drug, with side effects only ranging from mild to moderate. The serious side effects have been reported, however, they are very rarely occurring.
Common side effects of the drug may include hot flashes, fatigue, nausea, increase in appetite, and increase in sweating. Emergency medical attention is required if these effects persist. Some unlikely, yet serious side effects may also occur: swelling of feet and legs, signs of infections such as fever, dark urine, sore throat, stomach pains.
Other side effects may occur which affects the psychological and physical state of the patient. These side effects may include insomnia, depression, mood changes, fatigue, back and muscle pain, problems with vision, and unexplained fatigue.
Exemestane is found to be contraindicated in patients who have a known hypersensitivity to the drug or to any of its components. Exemestane should not be given to premenopausal women, and should not be used concomitantly with other medicines containing estrogen as it could interfere with the action of the drug.
Prior to the usage of the drug, a detailed medical history of the patient must be given. This includes past and present conditions, including allergic reactions, including other medications. Since exemestane is used for postmenopausal women, no known effects of the drug have been reported on pregnant women. A consultation with the doctor is necessary prior to taking the drug for pregnant women.
It is not known whether the drug is passed onto breast milk. In unlikely cases, the use of the drug for nursing mothers should be weighed based on the potential benefits and risks it poses.
Exemestane has the following structural formula:
• Molecular formula of exemestane is C20H24O2
• Chemical IUPAC Name is 10,13-dimethyl-6-methylidene-7,8,9,10,11,12,13,14,15,16- decahydrocyclopenta[a]phenanthrene-3,17-dione
• Molecular weight is 296.403 g/mol
• Exemestane available : 25mg tablets
Brand name(s): Aromasin, Exemestance, Exemestano, Exemestanum
Review published on: 06 August 2009
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