Letrozole (also known as Femara) is an oral non-steroidal aromatase inhibitor for the treatment of hormonally responsive breast cancer after surgery. Letrozole has been used for ovarian stimulation by fertility doctors since 2001 due to less chance of multiple gestations. It also shows promise in studies as a treatment for early-onset gynecomastia.
Estrogens are produced by the conversion of androgens through the activity of the aromatase enzyme. Estrogens then bind to an estrogen receptor, which causes cells to divide. Letrozole prevents the aromatase from producing estrogens by competitive, reversible binding to the heme of its cytochrome P450 unit. The action is specific, and letrozole does not reduce the production of minerals- or corticosteroids.