Exemestane

Exemestane was shown to protect against oxidation activity, hypoxia, damage from UV radiation, and also displayed anti-inflammatory properties similar to that of sulforaphane. The combination of the two agents was more potent than each alone, although the mechanism for this synergy remains to be explored.

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Description

Introduction

Exemestane lowers estrogen levels in postmenopausal women, which may slow the growth of certain types of breast tumors that need estrogen to grow in the body.

Exemestane is used to treat breast cancer in postmenopausal women. It is often given to women whose cancer has progressed even after surgery, radiation, or other cancer medications have been tried without success.

Exemestane may also be used for purposes not listed in this medication guide.

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How it works?

Breast cancer cell growth may be estrogen-dependent. Aromatase is the principal enzyme that converts androgens to estrogens both in pre-and postmenopausal women. While the main source of estrogen (primarily estradiol) is the ovary in premenopausal women, the principal source of circulating estrogens in postmenopausal women is from conversion of adrenal and ovarian androgens (androstenedione and testosterone) to estrogens (estrone and estradiol) by the aromatase enzyme in peripheral tissues.

Exemestane is an irreversible, steroidal aromatase inactivator, structurally related to the natural substrate androstenedione. It acts as a false substrate for the aromatase enzyme, and is processed to an intermediate that binds irreversibly to the active site of the enzyme, causing its inactivation, an effect also known as “suicide inhibition.” Exemestane significantly lowers circulating estrogen concentrations in postmenopausal women, but has no detectable effect on adrenal biosynthesis of corticosteroids or aldosterone. Exemestane has no effect on other enzymes involved in the steroidogenic pathway up to a concentration at least 600 times higher than that inhibiting the aromatase enzyme.

Side Effects

Call your doctor at once if you have:
● new or unusual bone pain;
● swelling in your hands or feet;
● feeling short of breath, even with mild exertion; or
● chest pain, sudden numbness or weakness, sudden headache, confusion, problems with vision, speech, or balance.
Common side effects may include:
● hot flashes;
● headache, tired feeling;
● joint pain;
● nausea, increased appetite;
● sleep problems (insomnia); or
● increased sweating.

More information

You should not use exemestane if you have not started menopause, or if you are pregnant or able to become pregnant.
Do not use exemestane if you are pregnant. It could harm the unborn baby.

Dosages

Usual Adult Dose for Breast Cancer:
25 mg orally once a day
Comment:
-This drug should be administered after a meal.
Uses:
-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 exemestane for completion of a total of five consecutive years of adjuvant hormonal therapy.
-Treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy.

Conclusion

Exemestane is an irreversible, steroidal aromatase inhibitor, structurally related to the natural substrate androstenedione. In post-menopausal women, oestrogens are produced primarily from the conversion of androgens into oestrogens through the aromatase enzyme in peripheral tissues.

User reviews

Review 1
I have to say I feel very lucky reading all these reviews. I have been on exemestane for just under 2 years. I started following 23 rounds of radiation after my lumpectomy. While is do have sore feet occasionally and some mild tiredness I feel pretty lucky compared to other people who have posted. I guess I just want people who are new to the drug to know that not everyone has terrible experiences with it. Yes, it does affect your libido as well but sometimes you just have to learn to make adjustments in what you want to do and what you can do. It has not completely got rid of my sex life but it has definitely made me appreciate the times I am up for it more. It does seem to be getting less of an issue the more I am on it but the trade off is rare occurrences of anxiety. I guess after losing more people than I care to count to cancer I am just lucky there are drugs like this to give us hope

Review 2
Stage 3 infiltrating ductal carcinoma breast cancer survivor twice over 20 years (single mastectomy). I’ve already had high dose chemo & radiation treatments. They also found a brain tumor in 2018. Turning 60 next month, I need to take an estrogen prohibitor and exemestane aka Aromasin is my 3rd AI to try! After 3 months on this drug I’ve had hot flashes, watery eyes, bad foot pain, headaches, falling asleep in the afternoon at work, but the worst for me has been hip/joint pain I never had before. My primary care doctor gave me a cortisone shot in the hip for the pain. He thinks it’s bursitis? (I’m going to try taking high dose vitamin D 50,000 units per week for joint pain someone else suggested in here). Not sure if I can do my time of 5 years on this drug, but oncologist said if I want 10 more years I should try. Comes down to quality of life vs duration of life? I’m running out of options!

Review 3

I was diagnosed with stage 3 invasive ductal carcinoma in early 2017. After one dose of chemo I developed sepsis and almost died – 2 weeks in ICU in a coma, followed by 2 months in hospital. I had to learn how to walk again, etc. Thanks to excellent medical care I am back at work, and about 85% “back to normal”. I am 61 years old and started this adventure as a pretty fit, outdoorsy woman, confident I could manage chemo. However, post sepsis, they won’t give me chemo again. I did 6 weeks of radiation, took letrizole for a year to suppress estrogen, and switched to exemestane in July 2018. My most concerning side effect is lack of vaginal lubrication and interest in sex, which sounds trivial but is wreaking emotional havoc in my 27 year marriage. Medical professionals seem to have no knowledge of the safety of using topical estrogen and it’s a risk my husband doesn’t want me to take. Had anyone had this problem? I feel dropped by the medical system.

Review 4

I just took my first dose of Exemestane. I’m 2 weeks post radiation therapy for breast cancer. I’m wondering if there is a patient Facebook group for this med.? There is a support group on this website https://www.drugs.com/answers/support-group/exemestane/

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