Exemestane

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

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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)