Exemestane – Uses, Dosage, Side Effects, Interactions

Exemestane - Uses, Dosage, Side Effects, Interactions
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Article Summary

Exemestane is a steroidal inhibitor of aromatase that effectively blocks estrogen synthesis in postmenopausal women and is used as therapy for estrogen receptor-positive breast cancer, usually after resection and after the failure of tamoxifen. Exemestane has been associated with a low rate of serum enzyme elevations during therapy and rare instances of clinically apparent liver injury. Exemestane is an oral steroidal aromatase inhibitor used in...

Key Takeaways

  • This article explains Mechanism of Action in simple medical language.
  • This article explains Indications in simple medical language.
  • This article explains Contraindications in simple medical language.
  • This article explains Dosage in simple medical language.
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Definition

Exemestane is a steroidal inhibitor of aromatase that effectively blocks estrogen synthesis in postmenopausal women and is used as therapy for estrogen receptor-positive breast cancer, usually after resection and after the failure of tamoxifen. Exemestane has been associated with a low rate of serum enzyme elevations during therapy and rare instances of clinically apparent injury.

Exemestane is an oral steroidal aromatase inhibitor used in the adjuvant treatment of hormonally-responsive (also called hormone-receptor-positive, estrogen-responsive) breast cancer in postmenopausal women. It irreversibly binds to the active site of the enzyme resulting in permanent inhibition.

Mechanism of Action

Breast cancer cell growth may be estrogen-dependent. Aromatase (exemestane) 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 in premenopausal women, the principal source of circulating estrogens in postmenopausal women is from the conversion of adrenal and ovarian androgens (androstenedione and testosterone) to estrogens (estrone and estradiol) by the aromatase enzyme in peripheral tissues. Estrogen deprivation through aromatase inhibition is an effective and selective treatment for some postmenopausal patients with hormone-dependent breast cancer. Exemestane is an irreversible, steroidal aromatase inactivator, structurally related to the natural substrate androstenedione. It irreversibly binds to the active site causing permanent inhibition and necessitating de novo synthesis to restore enzymatic function. Exemestane significantly lowers circulating estrogen concentrations in postmenopausal women but has no detectable effect on the adrenal biosynthesis of corticosteroids or aldosterone. This reduction in serum and concentrations of estrogen delays tumor growth and . 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.

or

Estrogen deprivation through aromatase inhibition is an effective and selective treatment for some postmenopausal patients with hormone-dependent breast cancer. 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 the 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.

Indications

  • For the treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy.
  • Exemestane is a steroidal inhibitor of aromatase that effectively blocks estrogen synthesis in postmenopausal women and is used as therapy for estrogen receptor-positive breast cancer, usually after resection and after the failure of tamoxifen. Exemestane has been associated with a low rate of serum enzyme elevations during therapy and rare instances of clinically apparent liver injury.
  • Exemestane is an aromatase inhibitor used to treat breast cancer in postmenopausal women after treatment with tamoxifen.
  • Antineoplastic (hormonal).
  • Exemestane is indicated for the treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy
  • Use of exemestane in premenopausal women is not accepted
  • 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.
  • Early Breast Cancer
  • , advanced Breast cancer

Use in Cancer

Exemestane is approved to treat:

Exemestane is used in postmenopausal women who have already been treated with tamoxifen citrate.

Exemestane is also being studied in the treatment of other types of cancer.

Contraindications

The following conditions are with this drug. Check with your physician if you have any of the following:

  • This drug is not indicated for the treatment of breast cancer in premenopausal women.
  • low vitamin D levels
  • decreased calcification or density of bone
  • pregnancy
  • a patient who is producing milk and breastfeeding

Strengths: 25 mg

Breast Cancer

  • 25 mg orally once a day

Side Effects

The Most Common

  • hot flushes
  • sweating
  • muscle or joint
  • tiredness
  • feeling worried or anxious
  • depression
  • difficulty falling asleep or staying asleep
  • increased appetite
  • hair loss
  • red, itchy skin
  • changes in vision
  • of the arms, hands, feet, ankles, or lower legs

More Common

  • abdominal or
  • burning, , or prickly sensations
  • diarrhea
  • dizziness
  • a general feeling of tiredness or
  • headache
  • hot flashes
  • increased appetite
  • increased sweating
  • joint pain
  • loss of hair
  • or cramps
  • nausea
  • trouble sleeping
  • weight gain
  • flu-like symptoms (e.g., , , sore throat, fever, or chills)
  • increased blood pressure (e.g., shortness of breath, fatigue, dizziness, fainting, bluish color to lips, chest pain or pressure)
  • increased cholesterol

Rare

  • signs of carpal tunnel syndrome (pain or burning in the hands or wrists)
  • signs of depression (e.g., poor concentration, changes in weight, changes in sleep, decreased interest in activities, thoughts of suicide)
  • signs of a urinary tract infection (e.g., difficult or painful urination, blood in the urine, frequent urge to urinate, lower back or side pain)
  • swelling of hands, ankles, feet, or lower legs
  • symptoms of liver damage (e.g., yellow skin or eyes, dark urine, clay-colored stools, loss of appetite, nausea, and vomiting, or itching)
  • symptoms of a stomach ulcer (e.g., heartburn, burning stomach pain, nausea, vomiting)
  • unexplained broken bones
  • vaginal bleeding
  • signs of a heart attack (e.g., chest pain or pressure, pain extending through shoulder and arm, nausea and vomiting, sweating)
  • signs of a blood clot in blood vessels, such as sudden vision change or dizziness, chest pain, pain and swelling in one leg muscle
  • sudden development of breathing problems (e.g., shortness of breath, trouble breathing, wheezing, tightness in the chest, or fast or irregular breathing)
  • signs of a severe allergic reaction (e.g., hives; difficulty breathing; swelling of the face, lips, tongue, or throat)
  • signs of bleeding in the stomach or intestines (e.g., dark and tarry stools, blood coming from rectum, vomiting blood or material that looks like coffee grounds, fast heartbeat, weakness or fainting)

Drug Interactions

Pregnancy and Lactation

 US FDA pregnancy category: Not assigned

Pregnancy

Although the effect of exemestane is unclear, there is some evidence suggesting that taking this medication during pregnancy may cause harm to an unborn baby. Exemestane should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.

Breast-feeding

It is not known if exemestane passes into breast milk. If you are breastfeeding and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding. The safety and effectiveness of using this medication have not been established for children.

What special precautions should I follow?

Before taking exemestane,

  • tell your doctor and pharmacist if you are allergic to exemestane or any other medications.
  • tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, and nutritional supplements you are taking or plan to take. Be sure to mention any of the following: carbamazepine (Carbatrol, Epitol, Tegretol); medications that contain estrogens such as hormone replacement therapy and hormonal contraceptives (birth control pills, patches, rings, and injections); phenobarbital; phenytoin (Dilantin); and rifampin (Rifadin, in Rifater, in Rifamate). Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
  • tell your doctor what herbal products you are taking, especially St John’s wort.
  • tell your doctor if you have or have ever had osteoporosis (a condition in which the bones are fragile and break easily), liver or kidney disease.
  • tell your doctor if you are pregnant or plan to become pregnant. You will need to have a negative pregnancy test within 7 days before you begin to take exemestane. You should use birth control to avoid pregnancy during your treatment with exemestane and for 1 month after your final dose. If you become pregnant while taking exemestane, call your doctor immediately. Exemestane may harm the fetus.
  • tell your doctor if you are breastfeeding. You should not breastfeed during your treatment with exemestane and for 1 month after your final dose.

References

  1. https://pubchem.ncbi.nlm.nih.gov/compound/Exemestane
  2. https://pubchem.ncbi.nlm.nih.gov/compound/Exemestane-D2
  3. https://pubchem.ncbi.nlm.nih.gov/compound/17-beta-Hydroxy-Exemestane-Epoxide
  4. https://go.drugbank.com/drugs/DB00990
  5. https://www.drugs.com/exemestane.html
  6. https://medlineplus.gov/druginfo/meds/a607006.html
  7. https://www.webmd.com/drugs/2/drug-17764/exemestane-oral/details/list-contraindications
  8. https://www.medbroadcast.com/drug/getdrug/med-exemestane
  9. ChemIDplus Chemical Information Classification
  10. CompTox Chemicals Dashboard Chemical Lists
  11. 10,13-dimethyl-6-methylidene-7,8,9,10,11,12,13,14,15,16-decahydrocyclopenta[a]phenanthrene-3,17-dione
    10,13-dimethyl-6-methylidene-7,8,9,10,11,12,13,14,15,16-decahydrocyclopenta[a]phenanthrene-3,17-dione
  12. EXEMESTANE
    CCSbase Classification
  13. NCI Thesaurus Tree
  14. LICENSE
    Data: CC-BY 4.0; Code (hosted by ECI, LCSB): Artistic-2.0
    Exemestane
    NORMAN Suspect List Exchange Classification
  15. PubChem
  16. Therapeutic category of drugs in Japan
    Anatomical Therapeutic Chemical (ATC) classification
    Target-based classification of drugs
  17. Guide to Pharmacology Target Classification
  18. NCBI

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What to tell the doctor

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Avoid these mistakes

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Get urgent help if

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Doctor / service to discuss: Qualified healthcare provider; specialist depends on symptoms and examination.
  1. Step 1

    Check danger signs first

    If danger signs are present, seek emergency care and do not wait for online information.

  2. Step 2

    Record the symptom story

    Write when symptoms started, severity, medicines already taken, allergies, pregnancy status, and test results.

  3. Step 3

    Visit a qualified clinician

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  4. Step 4

    Do only useful tests

    Do tests after clinical assessment. Avoid unnecessary tests, random antibiotics, or repeated medicines without diagnosis.

  5. Step 5

    Follow up and return early if worse

    If symptoms worsen, new warning signs appear, or treatment is not helping, return for review quickly.

Rural patient practical tips
  • Take a written symptom diary and all previous prescriptions/test reports.
  • Do not hide medicines already taken, even herbal or over-the-counter medicines.
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