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Letrozole, sold under the brand name Femara among others, is an aromatase inhibitor medication that is used in the treatment of breast cancer for post-menopausal women. [ 1 ] It was patented in 1986 and approved for medical use in 1996. [ 4 ]
Ovarian stimulation with the aromatase inhibitor letrozole has been proposed for ovulation induction in order to treat unexplained female infertility. In a multi-center study funded by the National Institute of Child Health and Development, ovarian stimulation with letrozole resulted in a significantly lower frequency of multiple gestation (i.e., twins or triplets) but also a lower frequency ...
AIs inhibit the enzyme aromatase that converts testosterone to estrogen and that is used clinically in treatments of breast cancer in postmenopausal women. Currently, two types of NSAIs are used for breast cancer, anastrozole and letrozole. They are used as first-line therapy in metastatic breast cancer and also in adjuvant treatment. [1]
The most common side effects (more than 10% of patients) are hot flashes and sweating, which are typical of estrogen deficiency as caused by exemestane, and also insomnia, headache, and joint pain. Nausea and fatigue are mainly observed in patients with advanced breast cancer. [7] [8]
The mechanism of action of SERDs involves binding to the estrogen receptor, leading to a conformational change that facilitates recruitment of cellular machinery to degrade the receptor protein. By promoting degradation of the estrogen receptor, SERDs effectively inhibit estrogen signaling within cancer cells, thereby suppressing tumor growth.
Staging breast cancer is the initial step to help physicians determine the most appropriate course of treatment. As of 2016, guidelines incorporated biologic factors, such as tumor grade, cellular proliferation rate, estrogen and progesterone receptor expression, human epidermal growth factor 2 (HER2) expression, and gene expression profiling into the staging system.
Another remaining question surrounding CDK inhibitors as a therapy is if certain cancers will evade or be resistant to treatment. One study showed that 20% of the patients being treated for metastatic ER+ HER2-breast cancer did not respond at all to treatment with a CDK4/6 inhibitor due to preexisting mutations allowing the cancer cells to continue proliferating despite treatment with the drug ...
It has also been used to prevent breast cancer in those at high risk. [7] It is taken by mouth. [7] Common side effects of anastrozole include hot flashes, altered mood, joint pain, and nausea. [7] [6] Severe side effects include an increased risk of heart disease and osteoporosis. [7] Use during pregnancy may harm the baby. [7]