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.	?
Legal status
Routes	?

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
Businness
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. Retrieved on 2007-07-22.

v • d • e Sex hormones and related agents (primarily G03, also L02, H01C) - human endogenous in CAPS
Progestogens: (receptor)	PROGESTERONE,Dienogest, Desogestrel, Drospirenone, Dydrogesterone, Ethisterone, Etonogestrel, Ethynodiol diacetate, Gestodene, Gestonorone, Levonorgestrel, Lynestrenol, Medroxyprogesterone, Megestrol, Norelgestromin, Norethisterone, Norethynodrel, Norgestimate, Norgestrel, Norgestrienone, Tibolone Selective progesterone receptor modulator: Asoprisnil, CDB-4124 Antiprogestogen: Mifepristone
Androgens: (receptor)	TESTOSTERONE, Androstanolone, Fluoxymesterone, Mesterolone, Methyltestosterone, (see also anabolic steroids) Antiandrogens: Bicalutamide, Cyproterone, Dienogest, Flutamide, Nilutamide, Spironolactone
Estrogens: (receptor)	ESTRADIOL, ESTRIOL, ESTRONE, Chlorotrianisene, Dienestrol, Diethylstilbestrol, Ethinylestradiol, Fosfestrol, Mestranol, Polyestradiol phosphate Selective estrogen receptor modulator: Afimoxifene, Arzoxifene, Bazedoxifene, Clomifene, Fulvestrant, Lasofoxifene, Raloxifene, Tamoxifen, Toremifene Aromatase inhibitor: Aminogluthetimide, Anastrozole, Atamestane, Exemestane, Formestane, Letrozole, Vorozole
Gonadotropins: (FSHR/LHCGR)	ovulation stim.: Clomifene, Urofollitropin Antigonadotropins: Danazol, Gestrinone
GnRH: (receptor)	agonist: Buserelin, Goserelin, Histrelin, Leuprorelin, Nafarelin, Triptorelin antagonist: Abarelix, Cetrorelix, Ganirelix

v • d • e WikiDoc Research Resources for Exemestane (Click show to right to view)
Articles on Exemestane	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 (Slides, Video, Images, MP3) on Exemestane	Powerpoint slides on Exemestane • Images of Exemestane • Photos of Exemestane • Podcasts & MP3s on Exemestane • Videos on Exemestane
Evidence Based Medicine Regarding Exemestane	Cochrane Collaboration on Exemestane • Bandolier on Exemestane • TRIP on Exemestane
Cost Effectiveness of Exemestane	Cost Effectiveness of Exemestane
Clinical Trials Involving Exemestane	Ongoing Trials on Exemestane at Clinical Trials.gov • Trial results on Exemestane • Clinical Trials on Exemestane at Google
Guidelines / Policies / Government Resources (FDA/CDC) Regarding Exemestane	US National Guidelines Clearinghouse on Exemestane • NICE Guidance on Exemestane • NHS PRODIGY Guidance • FDA on Exemestane • CDC on Exemestane
Textbook Information on Exemestane	Books and Textbook Information on Exemestane
Pharmacology Resources on Exemestane	Dosing of Exemestane • Drug interactions with Exemestane • Side effects of Exemestane • Allergic reactions to Exemestane • Overdose information on Exemestane • Carcinogenicity information on Exemestane • Exemestane in pregnancy • Pharmacokinetics of Exemestane •
Genetics, Pharmacogenomics, and Proteinomics of Exemestane	Genetics of Exemestane • Pharmacogenomics of Exemestane • Proteomics of Exemestane
Newstories on Exemestane	Exemestane in the news • Be alerted to news on Exemestane • News trends on Exemestane
Commentary on Exemestane	Blogs on Exemestane
Patient Resources on Exemestane	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 on Exemestane	Symptoms of Exemestane • Causes & Risk Factors for Exemestane • Diagnostic studies for Exemestane • Treatment of Exemestane
Continuing Medical Education (CME) Programs on Exemestane	CME Programs on Exemestane
International Resources on Exemestane	Exemestane en Espanol • Exemestane en Francais
Business Resources on Exemestane	Exemestane in the Marketplace • Patents on Exemestane
Informatics Resources on Exemestane	List of terms related to Exemestane

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Acknowledgement and Attribution Regarding Sources of Content

Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .