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Letrozole is an aromatase inhibitor, which means it works by blocking the enzyme aromatase. Aromatase is responsible for converting androgens (like testosterone) into estrogens in the body. By inhibiting this enzyme, letrozole effectively lowers estrogen levels.
In postmenopausal women, estrogen mainly comes from the conversion of androgens. Tumor growth in certain types of breast cancer is driven by estrogen. By reducing estrogen production, letrozole decreases the availability of this hormone, thereby limiting cancer cell growth and proliferation.
The use of letrozole is grounded in its ability to target estrogen synthesis, making it a valuable therapy in estrogen receptor-positive breast cancer cases. Its efficacy has been investigated in combination with other therapies, such as in clinical trial NCT01231659, evaluating its use with everolimus for treating locally advanced or metastatic breast cancer.
Although some studies have investigated its formulation, such as letrozole incorporated into Eudragit® nanoparticles (PMID: 42522303), the primary mechanism remains focused on the inhibition of aromatase to manage conditions like breast cancer and tackle hormone dysregulation in situations like polycystic ovarian syndrome (PMID: 42524428).
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