Exemestane

Exemestane
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

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Overview

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Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

There is limited information regarding Exemestane FDA-Labeled Indications and Dosage (Adult) in the drug label.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Exemestane in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Exemestane in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

There is limited information regarding Exemestane FDA-Labeled Indications and Dosage (Pediatric) in the drug label.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Exemestane in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Exemestane in pediatric patients.

Contraindications

There is limited information regarding Exemestane Contraindications in the drug label.

Warnings

There is limited information regarding Exemestane Warnings' in the drug label.

Adverse Reactions

Clinical Trials Experience

There is limited information regarding Exemestane Clinical Trials Experience in the drug label.

Postmarketing Experience

There is limited information regarding Exemestane Postmarketing Experience in the drug label.

Drug Interactions

There is limited information regarding Exemestane Drug Interactions in the drug label.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): There is no FDA guidance on usage of Exemestane in women who are pregnant.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Exemestane in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Exemestane during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Exemestane in women who are nursing.

Pediatric Use

There is no FDA guidance on the use of Exemestane in pediatric settings.

Geriatic Use

There is no FDA guidance on the use of Exemestane in geriatric settings.

Gender

There is no FDA guidance on the use of Exemestane with respect to specific gender populations.

Race

There is no FDA guidance on the use of Exemestane with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Exemestane in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Exemestane in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Exemestane in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Exemestane in patients who are immunocompromised.

Administration and Monitoring

Administration

There is limited information regarding Exemestane Administration in the drug label.

Monitoring

There is limited information regarding Exemestane Monitoring in the drug label.

IV Compatibility

There is limited information regarding the compatibility of Exemestane and IV administrations.

Overdosage

There is limited information regarding Exemestane overdosage. If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.

Pharmacology

There is limited information regarding Exemestane Pharmacology in the drug label.

Mechanism of Action

There is limited information regarding Exemestane Mechanism of Action in the drug label.

Structure

There is limited information regarding Exemestane Structure in the drug label.

Pharmacodynamics

There is limited information regarding Exemestane Pharmacodynamics in the drug label.

Pharmacokinetics

There is limited information regarding Exemestane Pharmacokinetics in the drug label.

Nonclinical Toxicology

There is limited information regarding Exemestane Nonclinical Toxicology in the drug label.

Clinical Studies

There is limited information regarding Exemestane Clinical Studies in the drug label.

How Supplied

There is limited information regarding Exemestane How Supplied in the drug label.

Storage

There is limited information regarding Exemestane Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Exemestane Patient Counseling Information in the drug label.

Precautions with Alcohol

Alcohol-Exemestane interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

There is limited information regarding Exemestane Brand Names in the drug label.

Look-Alike Drug Names

There is limited information regarding Exemestane Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

Exemestane

Clinical data
ATC code	L02BG06 (WHO)
Pharmacokinetic data
Bioavailability	~60%
Protein binding	90%
Elimination half-life	27 hours
Identifiers
IUPAC name 10,13-dimethyl-6-methylidene- 7,8,9,10,11,12,13,14,15,16- decahydrocyclopenta[a] phenanthrene- 3,17-dione
CAS Number	107868-30-4
PubChem CID	60198
DrugBank	APRD00144
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C20H24O2
Molar mass	296.403 g/mol

WikiDoc Resources for Exemestane
Articles
Most recent articles on Exemestane Most cited articles on Exemestane Review articles on Exemestane Articles on Exemestane in N Eng J Med, Lancet, BMJ
Media
Powerpoint slides on Exemestane Images of Exemestane Photos of Exemestane Podcasts & MP3s on Exemestane Videos on Exemestane
Evidence Based Medicine
Cochrane Collaboration on Exemestane Bandolier on Exemestane TRIP on Exemestane
Clinical Trials
Ongoing Trials on Exemestane at Clinical Trials.gov Trial results on Exemestane Clinical Trials on Exemestane at Google
Guidelines / Policies / Govt
US National Guidelines Clearinghouse on Exemestane NICE Guidance on Exemestane NHS PRODIGY Guidance FDA on Exemestane CDC on Exemestane
Books
Books on Exemestane
News
Exemestane in the news Be alerted to news on Exemestane News trends on Exemestane
Commentary
Blogs on Exemestane
Definitions
Definitions of Exemestane
Patient Resources / Community
Patient resources on Exemestane Discussion groups on Exemestane Patient Handouts on Exemestane Directions to Hospitals Treating Exemestane Risk calculators and risk factors for Exemestane
Healthcare Provider Resources
Symptoms of Exemestane Causes & Risk Factors for Exemestane Diagnostic studies for Exemestane Treatment of Exemestane
Continuing Medical Education (CME)
CME Programs on Exemestane
International
Exemestane en Espanol Exemestane en Francais
Business
Exemestane in the Marketplace Patents on Exemestane
Experimental / Informatics
List of terms related to Exemestane

Exemestane (trade name Aromasin) is an oral steroidal aromatase inhibitor (but also known uniquely as an aromatase inactivator) 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, the 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).

References

• Extensive information, including trial statistics from the National Institutes of Health
• Aromasin official website
• Profile of exemestane for use as an anti-estrogen by athletes and bodybuilders
• Coombes RC; et al. (2007). "Survival and safety of exemestane versus tamoxifen after 2–3 years' tamoxifen treatment (Intergroup Exemestane Study): a randomised controlled trial". Lancet. 369 (9561): 559–70. doi:10.1016/S0140-6736(07)60200-1. PMID 17307102. CS1 maint: Explicit use of et al. (link)