Exemestane
- Atc Codes:L02BG06
- CAS Codes:107868-30-4
- PHARMGKB ID:107868-30-4
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Aromasin; Belgium: Aromasin; Bulgaria: Aromasin; Cyprus: Aromasin; Czech Republic: Aromasin; Denmark: Aromasin; Estonia: Aromasin; Finland: Aromasin; France: Aromasine; Germany: Aromasin; Greece: Aromasin; Hungary: Aromasin; Ireland: Aromasin; Italy: Aromasin; Latvia: Aromasin; Malta: Aromasin; Netherlands: Aromasin; Portugal: Aromasin; Romania: Aromasin; Slovakia: Aromasin; Spain: Aromasil; Sweden: Aromasin; UK: Aromasin.
North America
Canada: Aromasin; USA: Aromasin.
Latin America
Argentina: Aromasin, Noxetol; Brazil: Aromasin; Mexico: Aromasin.
Asia
Japan: Aromasin.
Drug combinations
Chemistry
Exemestane: C~20~H~24~O~2~. Mw: 296.40. (1) Androsta-1,4-diene-3,17-dione, 6-methylene-; (2) 6-Methyleneandrosta-1,4-diene-3,17-dione. CAS-107868-30-4 (1999).
Pharmacologic Category
Antineoplastic Agents; Endocrine Therapy; Aromatase Inactivator. (ATC-Code: L02BG06).
Mechanism of action
Exemestane is an irreversible, steroidal aromatase inactivator. Prevents conversion of androgens to estrogens by tying up the enzyme aromatase. In breast cancers where growth is estrogen-dependent, it lowers circulating estrogens.
Therapeutic use
Used in treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy. Adjuvant treatment of postmenopausal estrogen receptor-positive early breast cancer following 2-3 years of tamoxifen (for a total of 5 years of adjuvant therapy.)
Pregnancy and lactiation implications
Possible fetal harm. Embryotoxic in rats and embryotoxic and abortifacient in rabbits.
Unlabeled use
Contraindications
Hypersensitivity to exemestane or any component of the formulation.
Warnings and precautions
Hazardous agent. Possible fetal harm. Not recommended for use in premenopausal women. Do not administer concomitantly with estrogenic agents. Risk of grade 3 or 4 lymphocytopenia. Should not be administered concurrently with estrogen-containing drugs.