These drugs treat estrogen receptor-positive (ER+) breast tumors, as they require estrogen to grow. By blocking estrogen production or its action on receptors, these tumors can be treated. These drugs also have action on ovarian tumors in postmenopausal women.
These drugs are often used to treat systemic metastases of ER-positive breast tumors, which preferentially spread to the liver, lungs, brain and bones. Other uses include treating ovarian cancers and preventing gynecomastia in men.
Non-steroidal inhibitors, such as anastrozole and letrozole, inhibit the synthesis of estrogen via reversible competition for the aromatase enzyme.
Letrozole is a non-steroidal aromatase inhibitor for the treatment of hormonally-responsive breast cancer after surgery. It works via reversible inhibition.
Anastrozole is an aromatase-inhibiting drug indicated for treatment of breast cancer after surgery, as well as for metastasis in both pre and post menopausal women. It is non-steroidal and works via reversible inhibition.
Irreversible steroidal inhibitors, such as exemestane, forms a permanent and deactivating bond with the aromatase enzyme.
Exemestane is an oral steroidal aromatase inhibitor that is used in ER-positive breast cancer in addition to surgery and/or radiation in postmenopausal women.
Estrogens have a positive effect on bone metabolism by stimulating bone growth and inhibiting bone resorption, so their depletion in patients with endocrine-responsive breast cancer leads to increased bone demineralization and finally osteoporosis occurs.
The use of aromatase inhibitors is also linked with the development of arthritis, while also causing arthralgias and arthrosis.
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