Fadrozole (marketed as Afema by Novartis) for the treatment of breast cancer.

 

Fadrozole (INN, marketed as Afema by Novartis) is an aromatase inhibitor^[1] that has been introduced in Japan for the treatment of breast cancer.

It is selective.^[2]

1. Raats JI, Falkson G, Falkson HC (January 1992). "A study of fadrozole, a new aromatase inhibitor, in postmenopausal women with advanced metastatic breast cancer". J. Clin. Oncol. 10 (1): 111–6. PMID 1530798.
2. Browne LJ, Gude C, Rodriguez H, Steele RE, Bhatnager A (February 1991). "Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease". J. Med. Chem. 34 (2): 725–36.doi:10.1021/jm00106a038. PMID 1825337.

Aromatase inhibitors (AIs) are a class of drugs used in the treatment of breast cancer and ovarian cancer inpostmenopausal women. AIs may also be used off-label to treat or prevent gynaecomastia in men.

Aromatase is the enzyme that synthesizes estrogen. As breast and ovarian cancers require estrogen to grow, AIs are taken to either block the production of estrogen or block the action of estrogen on receptors.

Types of AIs

There are 2 types of aromatase inhibitors (AIs) approved to treat breast cancer:

• Irreversible steroidal inhibitors, such as exemestane (Aromasin), forms a permanent and deactivating bond with the aromatase enzyme.

• Non-steroidal inhibitors, such as anastrozole (Arimidex), inhibit the synthesis of estrogen via reversible competition for the aromatase enzyme.

Aromatase inhibitors work by inhibiting the action of the enzyme aromatase, which converts androgens into estrogens by a process called aromatization. As breast tissue is stimulated by estrogens, decreasing their production is a way of suppressing recurrence of the breast tumor tissue. The main source of estrogen is the ovaries inpremenopausal women, while in post-menopausal women most of the body's estrogen is produced in peripheral tissues (outside the CNS), and also a few CNS sites in various regions within the brain. Estrogen is produced and acts locally in these tissues, but any circulating estrogen, which exerts systemic estrogenic effects in men and women, is the result of estrogen escaping local metabolism and spreading to the circulatory system.