Tamoxifen: A Comprehensive Review of its Mechanisms and Clinical Applications

 

Tamoxifen is a medication that has played a pivotal role in the treatment of hormone receptor-positive breast cancer for several decades. It is classified as a selective estrogen receptor modulator (SERM), and its main mechanism of action involves blocking the estrogen receptors in breast cancer cells, thereby inhibiting estrogen-driven tumor growth. This comprehensive review aims to explore the mechanisms of tamoxifen and its diverse clinical applications beyond breast cancer.

Mechanisms of Action: Tamoxifen exerts its effects primarily through its active metabolite, endoxifen, which competes with estrogen for binding to estrogen receptors (ERs). By binding to the ERs, tamoxifen prevents estrogen from activating the transcription of genes involved in cell proliferation and survival. Consequently, this impedes the growth of hormone receptor-positive breast cancer cells and reduces the risk of cancer recurrence.

Clinical Applications in Breast Cancer Treatment: Tamoxifen has become a cornerstone in the management of hormone receptor-positive breast cancer. It is commonly prescribed as adjuvant therapy after primary treatment, such as surgery, to reduce the risk of cancer recurrence. Studies have demonstrated that long-term tamoxifen therapy significantly improves disease-free and overall survival rates in these patients. Additionally, tamoxifen may be used as neoadjuvant therapy to shrink tumors before surgery, making them more manageable for surgical removal.

Adjuvant Therapy: Typically, tamoxifen is prescribed for five to ten years, depending on the patient's risk profile and menopausal status. For premenopausal women, tamoxifen is the preferred option, whereas postmenopausal women may opt for aromatase inhibitors as an alternative endocrine therapy.

Neoadjuvant Therapy: In some cases, especially when the tumor is large or locally advanced, tamoxifen may be given before surgery to reduce tumor size and facilitate a more conservative surgical approach.

Metastatic Breast Cancer: Tamoxifen also plays a role in the treatment of metastatic breast cancer, where it can help control tumor growth and alleviate symptoms. However, resistance to tamoxifen can develop over time, leading to disease progression.

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