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Exemestane
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DRUG INFO
Exemestane
Drug Name:
Exemestane
Indication: For the treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy.
Pharmacology: aromatase is an enzyme that converts hormones to estrogen in the body's adrenal glands. The aromatase inhibitors (AIs) are drugs that reduce estrogen levels by blocking the action of aromatase in the adrenal glands. The selective AIs (SAIs) selectively reduce levels of estrogen without interfering with levels of other steroid hormones that are produced by the adrenal gland. Drugs in this class include anastrozole (ArimidexÆ), letrozole (FemaraÆ) and exemestane (AromasinÆ).
Mechanism Of Action: Breast cancer cell growth may be estrogen-dependent. Aromatase (exemestane) is the principal enzyme that converts androgens to estrogens both in pre- and postmenopausal women. While the main source of estrogen (primarily estradiol) is the ovary in premenopausal women, the principal source of circulating estrogens in postmenopausal women is from conversion of adrenal and ovarian androgens (androstenedione and testosterone) to estrogens (estrone and estradiol) by the aromatase enzyme in peripheral tissues. Estrogen deprivation through aromatase inhibition is an effective and selective treatment for some postmenopausal patients with hormone-dependent breast cancer. 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". Exemestane significantly lowers circulating estrogen concentrations in postmenopausal women, but has no detectable effect on adrenal biosynthesis of corticosteroids or aldosterone. Exemestane has no effect on other enzymes involved in the steroidogenic pathway up to a concentration at least 600 times higher than that inhibiting the aromatase enzyme.
Drug Category: Antineoplastic Agents; ATC:L02BG06
Brand Names/Synonyms: Aromasin; EXEMESTANE; Exemestance; Exemestane; Exemestane [Inn]; Exemestane [Usan:Inn:Ban]; Exemestano [Inn-Spanish]; Exemestanum [Inn-Latin]
Dosage Forms: tablets
Absorption: 42%
Interactions:
DrugBank: Interactions for Exemestane
Interactions for Exemestane:
Exemestane is extensively metabolized by CYP 3A4, but coadministration of ketoconazole, a potent inhibitor of CYP
3A4, has no significant effect on exemestane pharmacokinetics. Significant pharmacokinetic interactions mediated by
inhibition of CYP isoenzymes therefore appear unlikely. Co-medications that induce CYP 3A4 (e.g., rifampicin,
phenytoin, carbamazepine, phenobarbital, or St. Johnís wort) may significantly decrease exposure to
exemestane. Dose modification is recommended for patients who are also receiving a potent CYP 3A4 inducer (see
DOSAGE AND ADMINISTRATION and CLINICAL
PHARMACOLOGY).
Drug/Laboratory Tests Interactions
No clinically relevant changes in the results of clinical laboratory tests have been observed.
Chemical IUPAC Name: 10,13-dimethyl-6-methylidene-7,8,9,10,11,12,13,14,15,16-decahydrocyclopenta[a]phenanthrene-3,17-dione
Chemical Formula: C20H24O2
Half Life: 24 hours
Drug Type: Approved Drug
# Accession No: APRD00144
CAS Registry Number: 107868-30-4
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Exemestane News
(When available)
Breast Cancer Prevention: Femara, Coffee Consumption Jan 6, 2006
KLAS-TV, ...another may not be the same because they have different hereditary factors or genetic risks.". The other two aromatase inhibitors are Arimidex and Aromasin. ...
Delay over top cancer treatment for women Dec 28, 2005
Times Online, ...disease returning. Access to the drug and its two close cousins, Aromasin and Arimidex, varies widely around the country. A survey ...
UPDATE 1-FDA OKs broader Novartis breast cancer drug use Dec 28, 2005
Reuters The two other aromatase inhibitors currently on the market are Arimidex, made by AstraZeneca (AZN.L: Quote, Profile, Research), and Aromasin, made by Pfizer Inc ...
Broader Novartis breast cancer drug use approved Dec 28, 2005
ABC News The two other aromatase inhibitors currently on the market are Arimidex, made by AstraZeneca , and Aromasin, made by Pfizer Inc. . ...
New Drugs For Breast Cancer Dec 20, 2005
WFtv.com, ...estrogen. There are three AIs approved by the FDA including anastrozole (Arimidex), exemestane (Aromasin) and letrozole (Femara). ...
2nd drug better at fighting breast cancer Dec 28, 2005
Washington Times, A third aromatase inhibitor, Pfizer Inc.'s Aromasin, also has shown promise for preventing recurrence when given after several years of tamoxifen. ...
Another drug added to breast cancer fight Dec 29, 2005
Fort Lauderdale Sun Sentinel, South Florida cancer doctors said they already have been using Femara, Arimidex and a third related drug, Aromasin, as a follow-up treatment for almost all post ...
FDA approves cancer drugs Dec 31, 2005
North Platte Telegraph, Femara is the latest aromatase inhibitor to be approved by the FDA. Other drugs in this class include Arimidex and Aromasin. "It ...
... Go to the Article Jan 4, 2006
CancerWise Some cancer treatments such as the aromatase inhibitors, Arimidex® (anastrozole), Aromasin® (exemestane) and Femara® (letrozole), may increase bone loss by ...
Fresh hopes for life-saving breast cancer drug Dec 28, 2005
The Observer, Trials have compared the performance of individual drugs in the class, anastrozole (Arimidex), exemestane (Aromasin) and letrozole (Femara) with tamoxifen. ...
Femara May Be Better Than Tamoxifen Dec 28, 2005
WebMD ...estrogen. Tamoxifen also blocks estrogen's effects, but not in the same way as Femara and its sister drugs Arimidex and Aromasin. ...
New hope for breast cancer patients Dec 29, 2005
Yorkshire Post Today, Institute for Clinical Excellence is expected to report next November on three aromatase inhibitors – Arimidex, Femara and Aromasin – as alternatives to ...
New drug fights breast cancer Dec 29, 2005
Danbury News Times, ...with breast cancer had been to give them tamoxifen for two or three years, then switch to an aromatase inhibitor — including Femara, Arimedex and Aromasin. ...
Researchers seek volunteers for breast cancer study Dec 14, 2005
Newark Star Ledger, ...responding to tamoxifen therapy, Lasser said. Exemestane is a hormonal drug sold under the brand Aromasin. It belongs to a newer ...
Cancer Center at center of treatment research Dec 24, 2005
Odessa American, The research has resulted in the approval of about 20 drugs such as Gemzar, a medication for lung patients, and Aromasin and Herceptin for breast cancer. ...
Hope lives for cancer patients Dec 18, 2005
Birmingham News, ...cancer lesions. I've taken Tamoxifen, Femara and Aromasin. When one drug quits working, Dr. Falkson switches me to another. On Friday ...
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