- Side Effects
- Drug Interactions
- Pregnancy & Breastfeeding
- What Else to Know
Generic Name: exemestane
Brand Name: Aromasin
Drug Class: Antineoplastics, Aromatase Inhibitor
What is exemestane, and what is it used for?
Exemestane is a medication approved for the treatment of advanced breast cancer in postmenopausal women, and is also used off-label to prevent breast cancer in high-risk premenopausal women.
Exemestane belongs to a drug class known as aromatase inhibitors which work by blocking the activity of aromatase, an enzyme that plays an important role in the biosynthesis of estrogens, the female sex hormones.
Estrogens are steroid hormones that come in three forms, estrone (E1), estradiol (E2), and estriol (E3). Estrogens are essential for normal sexual development and function, and in addition, have many other important functions in the body. On the other hand, the growth of the majority of breast cancers is stimulated and maintained by estrogens. Exemestane helps prevent, halt or slow down the progression of estrogen-dependent breast cancers.
In postmenopausal women, the ovaries stop producing estrogens and the primary source of estrogens are those derived from the male sex hormones (androgens) androstenedione and testosterone produced by the adrenal gland. Aromatase is responsible for the conversion of the two androgens into estrone and estradiol. By inhibiting aromatase, exemestane reduces the availability of estrogens that cancer cells require to grow.
The uses of exemestane include:
- Treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy
- Adjuvant treatment of estrogen receptor (ER)-positive early breast cancer in postmenopausal patients who have received 2 to 3 years of tamoxifen, to complete a total of 5 consecutive years of adjuvant hormonal therapy
- Adjuvant therapy in combination with ovarian function suppression, for high-risk hormone-positive breast cancer in premenopausal women
- First-line adjuvant treatment for early ER-positive breast cancer in postmenopausal women
- Risk-reduction for invasive breast cancer in postmenopausal women
- Do not use in patients with known hypersensitivity to exemestane or any of its components.
- Do not use exemestane to treat women who are pregnant or who may become pregnant, the drug can cause loss of a pregnancy or fetal harm.
- Exemestane is indicated for breast cancer in postmenopausal women, and if it must be used in premenopausal women:
- Verify the pregnancy status of women before initiation of therapy and do not administer it to pregnant women.
- In case pregnancy occurs during treatment, apprise the patient of potential hazards to the fetus and the potential risk of pregnancy loss.
- Exemestane should not be administered concurrently with estrogen-containing agents as they can interfere with the effects of exemestane.
- Assess the levels of 25-hydroxyvitamin D before the start of exemestane therapy, due to the high prevalence of vitamin D deficiency in women with early breast cancer, and administer vitamin D to those who are deficient.
- Exemestane reduces bone mineral density over time. Assess patient’s bone mineral density before starting treatment, monitor the patient for loss of bone mineral density, and treat appropriately.
- Low lymphocyte count (Grade 3 or 4 lymphopenia) was observed with exemestane therapy, although most patients had preexisting lower grade lymphopenia. Some patients improved or recovered while continuing exemestane, however, there was no significant increase in viral infections, and no opportunistic infections.
- Rarely, elevations of AST, ALT, alkaline phosphatase, and gamma glutamyl transferase enzymes were observed, which may be from liver or bone metastases. In patients with early breast cancer, elevations of bilirubin, alkaline phosphatase, and serum creatinine were more common with exemestane treatment than with tamoxifen or placebo.
What are the side effects of exemestane?
Common side effects of exemestane include:
- Hot flashes
- Joint pain (arthralgia)
- Low count of lymphocyte white blood cells (lymphocytopenia)
- Increase in serum alkaline phosphatase
- High blood pressure (hypertension)
- Chest pain
- Chest pain associated with coronary artery disease (angina pectoris)
- Reduced blood flow to the heart (ischemic heart disease)
- Heart attack (myocardial infarction)
- Swelling (edema)
- Peripheral edema
- Hair loss (alopecia)
- Excessive sweating (hyperhidrosis)
- Skin reactions including:
- Itching (pruritus)
- Abdominal pain
- Loss of appetite (anorexia)
- Indigestion (dyspepsia)
- Increased appetite
- Weight gain
- Increase in gamma-glutamyl transferase enzyme
- Increase in serum bilirubin
- Increase in serum creatinine
- Urinary tract infection
- Swelling due to lymph fluid buildup (lymphedema)
- Reduced skin sensation (hypoesthesia)
- Tingling and numbness (paresthesia)
- Tumor pain
- Carpal tunnel syndrome
- Visual disturbance
- Back pain
- Limb pain
- Skeletal pain
- Weakness (asthenia)
- Muscle pain (myalgia)
- Muscle cramps
- Brittle bones (osteoporosis)
- Pathological fracture
- Shortness of breath (dyspnea)
- Flu-like symptoms
- Upper respiratory tract infection
- Nasal inflammation (rhinitis)
- Throat inflammation (pharyngitis)
- Sinus inflammation (sinusitis)
- Bronchial inflammation (bronchitis)
Less common side effects of exemestane include:
- Hypersensitivity reaction
- Heart failure
- Blood vessel block from blood clot (thromboembolism)
- Gastric ulcer
- Elevated liver enzymes (transaminases)
- Liver inflammation (hepatitis)
- Liver inflammation due to impaired bile flow (cholestatic hepatitis)
- Overgrowth of the inner uterine membrane (endometrial hyperplasia)
- Endometrial polyps
- Nerve disease (neuropathy)
- Trigger finger (stenosing tenosynovitis)
- Decreased bone mineral density
- Abnormal bone growth (osteochondrosis)
- Hives (urticaria)
- Acute generalized exanthematous pustulosis, a severe skin disorder
Call your doctor immediately if you experience any of the following symptoms or serious side effects while using this drug:
- Serious heart symptoms include fast or pounding heartbeats, fluttering in your chest, shortness of breath, and sudden dizziness;
- Severe headache, confusion, slurred speech, severe weakness, vomiting, loss of coordination, feeling unsteady;
- Severe nervous system reaction with very stiff muscles, high fever, sweating, confusion, fast or uneven heartbeats, tremors, and feeling like you might pass out; or
- Serious eye symptoms include blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.
This is not a complete list of all side effects or adverse reactions that may occur from the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may also report side effects or health problems to the FDA at 1-800-FDA-1088.
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What are the dosages of exemestane?
- 25 mg
Postmenopausal ER-Positive Breast Cancer
- 25 mg orally once/day; continue until tumor progression
Breast Cancer Adjuvant Treatment
- Switch to exemestane after 2-3 years of tamoxifen treatment
- 25 mg orally once/day; continue until tumor progression
- Take after meals
Breast Cancer Prevention (Off-label)
- 2013 American Society of Clinical Oncology (ASCO) guidelines suggest exemestane as an alternative to tamoxifen or raloxifene to prevent invasive breast cancer in high-risk women
- 25 mg orally once/day for 5 years
- Coadministration with potent CYP3A4 inducers: 50 mg orally once/day
- High risk of breast cancer is defined as at least 1 breast biopsy showing lobular carcinoma in situ (LCIS) or atypical hyperplasia, 1 or more first-degree relatives with breast cancer, or a 5-year predicted risk of breast cancer greater than 1.66% (based on the modified Gail model)
- Safety and efficacy not established
- In clinical trials, dosages of up to 800 mg single dose in healthy women volunteers, and up to 600 mg daily for 12 weeks in postmenopausal women with breast cancer were well tolerated. In animal studies, convulsions and death occurred at extremely high doses.
- There is no specific antidote for exemestane, overdose is treated with symptomatic and supportive care, including monitoring of vital signs.
What drugs interact with exemestane?
Inform your doctor of all medications you are currently taking, who can advise you on any possible drug interactions. Never begin taking, suddenly discontinue, or change the dosage of any medication without your doctor’s recommendation.
- Exemestane has no known severe interactions with other drugs.
- Serious interactions of exemestane include:
- Exemestane has moderate interactions with at least 56 different drugs.
- Mild interactions of exemestane include:
- bazedoxifene/conjugated estrogens
- conjugated estrogens
- conjugated estrogens, vaginal
The drug interactions listed above are not all of the possible interactions or adverse effects. For more information on drug interactions, visit the RxList Drug Interaction Checker.
It is important to always tell your doctor, pharmacist, or health care provider of all prescription and over-the-counter medications you use, as well as the dosage for each, and keep a list of the information. Check with your doctor or health care provider if you have any questions about the medication.
Pregnancy and breastfeeding
- There are no studies of exemestane use in pregnant women, however, animal reproductive studies show it can cause fetal harm if used during pregnancy.
- Exemestane may impair fertility in both males and females.
- Women of pregnancy potential should be tested for pregnancy 7 days before initiating exemestane, and the drug should be avoided in pregnant women.
- Women of pregnancy potential should practice effective contraception during exemestane therapy and for one month following the final dose.
- It is not known if exemestane is present in breast milk, however, many drugs are excreted in breast milk. Women should not breastfeed while on exemestane therapy and for one month following the final dose, because of the potential for serious adverse reactions in the breastfed infant.
What else should I know about exemestane?
- Take exemestane exactly as prescribed.
- Store safely out of reach of children.
- In case of overdose, seek medical help or contact Poison Control.
Subscribe to MedicineNet's Cancer Report Newsletter
Exemestane is a medication approved for the treatment of advanced breast cancer in postmenopausal women, and is also used off-label to prevent breast cancer in high-risk premenopausal women. Common side effects of exemestane include fatigue, hot flashes, pain, headache, insomnia, depression, joint pain (arthralgia), low count of lymphocyte white blood cells (lymphocytopenia), nausea, high blood pressure (hypertension), chest pain, and others. Do not take if pregnant or breastfeeding.
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Tests used to detect cancer vary depending on the type of cancer, and can help to diagnose the disease, monitor how well cancer treatment is working or check if the cancer has come back.
How Can You Detect Breast Cancer Early?
Breast cancer develops from the cells of the breasts and can spread to other parts of the body (metastasis). It is one of the most common cancers diagnosed in women in the United States. A lump in the breast or armpit is often the first sign. Treatment success depends largely on early detection.
How to Manage Menopause Symptoms After Breast Cancer
Breast cancer treatment can cause menopausal symptoms due to the way certain therapies affect the ovaries. Learn about how you can find relief.
What Does Breast Cancer in a Man Feel Like?
Male breast cancer is rare and affects 2.7 out of 100,000 African American men and 1.9 out of 100,000 Caucasian men in the United States.
Guide for COVID-19 Vaccine for Cancer Patients
The authorities have jointly agreed that patients on active cancer treatment are at a higher risk of COVID-19 infection and complications. Hence, there is a necessity to prioritize patients with cancer for the COVID-19 vaccine.
What Are the Risk Factors for Developing Breast Cancer?
Breast cancer refers to the uncontrolled growth of cells within the breast. The risk factors for developing breast cancer include age, genetics, family history, personal history, menstrual history, breast density, previous radiation therapy, ethnicity, body weight, physical activity level, reproductive history, alcohol consumption and hormone pill use.
What Is the Newest Treatment for Breast Cancer?
Targeted therapies are a newer form of breast cancer treatment. They can be used alone or along with other therapies. Targeted therapies directly target cancer cells or specific processes that contribute to the growth of cancer cells. Target therapy often has fewer side effects.
How Can Cancer Be Diagnosed?
Along with your medical history and a physical exam, multiple diagnostic tests can be used to help your doctor confirm or eliminate the presence of cancer.
What Is the Survival Rate of Localized Breast Cancer?
The 5-year survival rate for localized breast cancer is 99%, and the condition is very treatable. Learn about symptoms and treatment for early stage breast cancer.
What Is Breast Cancer Screening?
Breast cancer screening is a process of examining the breasts to detect any signs or symptoms of cancer. Check out the center below for more medical references on breast cancer, including multimedia (slideshows, images, and quizzes), related disease conditions, treatment and diagnosis, medications, and prevention or wellness.
What Is the Risk of Breast Cancer by Age?
Age is the most significant risk factor for breast cancer, with the risk increasing with age. The risk peaks during menopause and remains constant or reduces afterwards.
Genetic Testing: Families With Breast Cancer
Breast cancer can be a killer and the decision to get tested to see if a patient is prone to the disease should be discussed with a doctor -- particularly if the woman has a history of breast cancer in her family. Genetic testing can only tell so much about breast cancer risk, however.
How Does Breast Cancer Start?
Breast cancer develops in the cells of the breasts and can spread to other parts of the body (metastasis). It is one of the most common cancers diagnosed in women in the US. Although extremely rare, breast cancer can sometimes occur in men. Breast cancer forms when there are changes or mutations in the deoxyribonucleic acid (DNA), which can cause normal breast cells to become cancerous.
How Is Breast Cancer Cured?
Surgery is the main treatment option for treating stage I breast cancer. Otherwise, the treatment options for breast cancer are determined by the following.
How Common Is Breast Cancer in Men?
Breast cancer is more common in women. However, men can get breast cancer too. The chances of occurrence of breast cancer in men are rare. Out of every 100 breast cancer diagnosed in the United States, 1 is found in a man.
What Are the Reasons for Breast Cancer?
Breast cancer is a multifactorial disease that can be caused by genetic and environmental factors. Experts are not yet fully aware of what may be the exact reason for breast cancer. The chances of getting breast cancer depend on the person’s age, personal history, genetic factors, and diet.
What Age Can a Male Get Breast Cancer?
Breast cancer risk in men increases with age, and most men with breast cancer are diagnosed in their 60s and 70s. Learn about causes and risk factors for breast cancer in men.
Treatment & Diagnosis
- Is a Breast Ultrasound or Mammogram Better?
- What Percentage of Abnormal Mammograms Are Cancer?
- What Age Should a Woman Get a Mammogram?
- Bone Marrow Transplantation for Breast Cancer
- Can Mammograms Detect Cancer?
- Genetic Testing for Breast Cancer
- Radiation Therapy for Breast Cancer
- Role of Estrogen Receptors in Breast Cancer
- Breast Cancer Follow-Up Self-Exam
- Breast Cancer
- Breast Cancer Husband
- Breast Cancer: A Feisty Women's Discussion
- Breast Cancer: Mother-daughter relationships
- Nutrition: Fighting Cancer With Food
- Breast Cancer
- Cancer: Confronting Cancer with Humor
- Cancer Survival and Attitude with Hamilton Jordan
- Cancer: The Importance of Joining a Cancer Support Group with Selma Schimmel
- Breast Cancer: Early Stage Treatments
- Cancer and Green Tea
- Cancer Patients Need Proper Diet and Exercise
- Cancer Pain Management with Ann Reiner
- Cancers: Children's Cancers
- Cancer: Childhood Cancer Survivors
- Cancer: Living Well Despite with Win Boerckel
- Cancer Treatment: Writing to Heal with Margie Davis
- Breast Cancer, Taking Control: Self-Advocacy 101
- Breast Cancer: The Male View on Survival and Support
- Cancer: Journaling to Save Your Life
- Breast Cancer: Early Diagnosis and Prevention
- Breast Cancer Treatment Update
- Cancer Research: Going the Distance
- Breast Cancer: Clinical Trials - Today's Cutting Edge
- Breast Cancer, Metastatic: Treatment Goals and Therapy Options -- Harold J. Burstein, MD
- Breast Cancer FAQs
- Cancer FAQs
- Breast Cancer Risk - Reduced With Exercise
- Cancer,Stroke & Heart Attack Risks- ReducedThrough Walking
- Herceptin Metastatic Breast Cancer Treatment
- Hormone Therapy in Survivors of Breast Cancer
- Breast Cancer: Types of Breast Cancer
- Cancer Survivor?
- Cancer Care in the Elderly
- Breastfeeding -- Protection from Breast Cancer?
- Exercise Improves Breast Cancer Survival
- Stress and Aggressive Breast Cancer: Cause or Effect?
- Advanced Breast Cancer in Young Women Increasing
- Angelina Jolie's Mastectomy
- Does Positive Additude Affect Breast Cancer?
- How Common and Dangerous Is Male Breast Cancer?
- How Many Breast Cancer Deaths Are there Each Year?
- Where Can Breast Cancer Spread To?
- Why Is Breast Cancer More Common in Females than Males?
- How Much Breast Cancer is Genetic?
- How Long Can Breast Cancer Patients Live?
- Who Does Breast Cancer Affect?
- How Does Breast Cancer Form?
- How Many Breast Cancer Stages Are There?
- Facts on Breast Cancer Causes, Risk Factors, and Types
- Breast Cancer Symptoms and Signs
- Complementary and Alternative Cancer Treatments
- Breast Cancer Detection
- Breast Cancer Treatment
- 10 Cancer Symptoms That Men Ignore
- Cancer Prevention: The Anticancer Diet
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