Clinical Information
Gen. Code and Des.
44186 exemestane ORAL TABLET 25 MG
GCN and Des.
92896 exemestane ORAL TABLET 25 MG
Strength
25MG
Dose Form
TABLET
Product Category
RX Pharmaceuticals
Fine Line Class
850085008510 All Rx Products
DEA Class
NC
OMP Family
AHFS Class
10000000 ANTINEOPLASTIC AGENTS
68160800 ANTIESTROGENS
Active Ingredients
7997 exemestane 107868304
Inactive Ingredients
2272 mannitol 69658
2537 povidone 9003398
2598 sucrose 57501
3203 paraben 99967
7230 magnesium carbonate
FDA NDA Approved
DESCRIPTION
AROMASIN? Tablets for oral administration contain 25 mg of exemestane, an irreversible, steroidal aromatase inactivator. Exemestane is chemically described as 6-methylenandrosta-1,4-diene-3,17-dione. Its molecular formula is C20 H24 O2
The active ingredient is white to slightly yellow crystalline powder with molecular weight of 296.41. Exemestane is freely soluble in N, N-dimethylformamide, soluble in methanol, and practically insoluble in water.
Each AROMASIN Tablet contains the following inactive ingredients: mannitol, crospovidone, polysorbate 80, hypromellose, colloidal silicon dioxide, microcrystalline cellulose, sodium starch glycolate, magnesium stearate, simethicone, polyethylene glycol 6000, sucrose, magnesium carbonate, titanium dioxide, methylparaben, and polyvinyl alcohol.
Mechanism of Action
Breast cancer cell growth may be estrogen-dependent. Aromatase 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.
INDICATIONS AND USAGE
1.1 Adjuvant Treatment of Postmenopausal Women
AROMASIN is indicated for 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 AROMASIN for completion of total of five consecutive years of adjuvant hormonal therapy
1.2 Advanced Breast Cancer in Postmenopausal Women
AROMASIN is indicated for the treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy
2 DOSAGE AND ADMINISTRATION
2.1 Recommended Dose
The recommended dose of AROMASIN in early and advanced breast cancer is one 25 mg tablet once daily after meal.
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 AROMASIN for completion of total of five consecutive years of adjuvant hormonal therapy.
the treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy.
Dose Modifications
? Concomitant use of strong CYP 3A4 inducers decreases exemestane exposure, For patients receiving AROMASIN with strong CYP 3A4 inducer such as rifampicin or phenytoin, the recommended dose of AROMASIN is 50 mg once daily after mea
DOSAGE FORMS AND STRENGTHS
AROMASIN Tablets are round, biconvex, and off-white to slightly gray. Each tablet contains 25 mg of exemestane. The tablets are printed on one side with the number ?7663? in black.
Pregnancy
AROMASIN may cause fetal harm when administered to pregnant woman. Based on its mechanism of action AROMASIN is expected to result in adverse reproductive effects. In non-clinical studies in rats and rabbits, exemestane was embryotoxic, fetotoxic, and abortifacient.
AROMASIN is contraindicated in women who are or may become pregnant. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus.
AROMASIN Tablets should not be administered to premenopausal women
WARNINGS AND PRECAUTIONS
5.1 Administration with Estrogen-Containing Agents
AROMASIN should not be coadministered with estrogen-containing agents as these could interfere with its pharmacologic action.
DRUG INTERACTIONS
Drugs That Induce CYP 3A4
Co-medications that induce CYP 3A4 (e.g., rifampicin, phenytoin, carbamazepine, phenobarbital, or St. John?s wort) may significantly decrease exposure to exemestane. Dose modification is recommended for patients who are also receiving strong CYP 3A4 induce