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Exemestane

 
Drug Info: Exemestane

Brand names: Aromasin®

Chemical formula:



Exemestane tablets

What are exemestane tablets?

EXEMESTANE (Aromasin®) blocks the production of the hormone estrogen. Some types of breast cancer depend on estrogen to grow, and exemestane can stop tumor growth by blocking estrogen production. Exemestane is for the treatment of breast cancer in postmenopausal women only. Generic exemestane tablets are not available.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• osteoporosis
• an unusual or allergic reaction to exemestane, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I take this medicine?

Take exemestane tablets by mouth at the same time each day after a meal. Follow the directions on the prescription label. Swallow the tablets with a drink of water. Do not take your medicine more often than directed. Do not stop taking except on your prescriber's advice.

What if I miss a dose?

If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses. If you vomit after taking a dose, call your prescriber or health care professional for advice.

What drug(s) may interact with exemestane?

androstenedione
• any medicine containing estrogens (This may include some herbal products and some birth control pills)
• DHEA

Tell your prescriber or health care professional about all other medicines that you are taking, including nonprescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking exemestane?

Visit your prescriber or health care professional for regular checks on your progress.

Do not treat yourself for diarrhea, nausea, vomiting or other side effects. Ask your prescriber or health care professional for advice.

What side effects may I notice from taking exemestane?

Side effects that you should report to your prescriber or health care professional as soon as possible:
• any new or unusual symptoms
• fever
• leg or arm swelling
• pain in bones, joints, or muscles
• pain in hips, back, ribs, arms, shoulders, or legs
• skin rash or itching
• visual changes

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• anxiety
• constipation
• cough, or throat infection
• depression
• diarrhea
• difficulty sleeping
• dizziness
• headache
• hot flashes
• increase or decrease in appetite
• nausea
• numbness or tingling in hands or feet
• stomach pain
• sweating
• weakness and tiredness
• weight gain

Where can I keep my medicine?

Keep out of the reach of children in a container that small children cannot open.

Store at room temperature between 20 and 25 degrees C (68 and 77 degrees F). Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

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Wikipedia: Exemestane
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Exemestane
Systematic (IUPAC) name
10,13-dimethyl-6-methylidene- 7,8,9,10,11,12,13,14,15,16- decahydrocyclopenta[a] phenanthrene- 3,17-dione
Identifiers
CAS number 107868-30-4
ATC code L02BG06
PubChem 60198
DrugBank APRD00144
Chemical data
Formula C20H24O2 
Mol. mass 296.403 g/mol
Pharmacokinetic data
Bioavailability ~60%
Protein binding 90%
Metabolism  ?
Half life 27 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat.

D

Legal status

Rx only

Routes Oral
 Yes check.svgY(what is this?)  (verify)

Exemestane (trade name Aromasin) 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. An aim in the treatment of hormone-receptor-positive patients in preventing recurrence is to lower estrogen levels that this breast cancer thrives on.

The main source of estrogen is the ovaries in premenopausal women, while in post-menopausal women most of the body's estrogen is produced in the adrenal gland from the conversion of androgens into estrogen by the aromatase enzyme. 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." In other words, Exemestane, by being structurally similar to the target of the enzymes, permanently binds to those enzymes, thereby preventing them from ever completing their task of converting androgens into estrogens.

The estrogen suppression rate for exemestane varies from 85% for estradiol (E2) to 95% for estrone (E1).

Clinical uses

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.

Exemestane is indicated for the treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy.

External links

References


 
 
Learn More
Exemestane tablets
Exemestane Oral tablet
Aromatase Inhibitors

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Would natural progesterone help to balance the antiaging hormone when one is taking exemestane to block all estrogen?

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Wikipedia. This article is licensed under the Creative Commons Attribution/Share-Alike License. It uses material from the Wikipedia article "Exemestane" Read more