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What is tamoxifen? How does it work?

Tamoxifen citrate has been the most commonly prescribed drug to treat breast cancer, since the approval of the drug by the U.S. Food and Drug Administration (FDA) in the 1970s. Tamoxifen is taken orally in pill form. The brand name of tamoxifen citrate is Nolvadex.

Tamoxifen citrate is an example of a type of drug called a selective estrogen receptor modulator (SERM). Tamoxifen works by binding to estrogen receptors on estrogen-dependent breast cancer cells, thereby competitively blocking their ability to absorb estrogen, preventing their ability to "turn on" estrogen-sensitive signals in DNA, suppressing DNA synthesis of the cancer cells, and blocking multiplication of the cancer cells. Without having bound estrogen to stimulate their growth, the breast cancer cells “starve” and die.

Also, tamoxifen blocks the production of insulin-like growth factor-1 (IGF-1), a molecule that otherwise could help cancer cells multiply. Furthermore, tamoxifen stimulates the synthesis of transforming growth factor B (TGF-b), a molecule that suppresses the multiplication of cancer cells.

Tamoxifen reduces the risk of recurrence and metastasis of estrogen receptor-positive (ER-positive) breast cancer. Use of tamoxifen for 5 years in post-menopausal women who had been treated for ER-positive breast cancer resulted in an 81.4% rate of disease-free survival (i.e., survival with no evidence of recurrence of disease).

If a woman who has had ER-positive breast cancer has taken tamoxifen for 5 years, however, it generally is recommended that she consider taking an aromatase inhibitor.

In 1998, Tamoxifen became the first drug to be approved by the FDA for the prevention of breast cancer. Research showed that tamoxifen reduced the chances of developing breast cancer by 50% in women at high risk for the disease.

As tamoxifen blocks the action of estrogen, some side effects are possible.

Questions Related to Tamoxifen
If my cancer does recur, how will I be treated?
I’ve just been diagnosed with breast cancer. What should I do, including deciding on treatment?
Should I get a second opinion from another doctor about my breast cancer?
What are the treatment options for breast cancer?
What things should I consider when deciding on a type of treatment for my breast cancer?
What does a cancer’s histological grade have to do with selecting a type of treatment?
What treatments are usually associated with the different stages of breast cancer?
What is a bone scan? Why do I need one?
What is the difference between breast cancer and recurrent breast cancer? How do the treatments differ?
What are breast-conserving surgeries?
Why do I need so many doctors involved in my treatment for breast cancer? What do all the doctors do?
What is the difference between local and systemic treatment of breast cancer?
How is hypercalcemia treated?
What is the difference between a lumpectomy and a mastectomy?
When would I choose a mastectomy over a lumpectomy?
When is radiation added after a mastectomy?
What is a lumpectomy?
What is a partial mastectomy?
What is a radical mastectomy?
What is a modified radical mastectomy?
What is a total mastectomy?
What is a segmental mastectomy?
What is a skin-sparing mastectomy?
What is involved with a lumpectomy surgery? How long will it take?
What is involved with a mastectomy surgery? How long will it take to recover?
What is radiation therapy?
When is radiation therapy appropriate for breast cancer?
When is radiation therapy not an option for breast cancer?
Does the procedure for external radiation therapy hurt?
Will external radiation therapy make me radioactive?
Does radiation therapy increase my risk of my breast cancer recurring?
Does radiation therapy increase my risk of developing cancer in my other breast?
Who is a dosimetrist?
What happens during your radiation setup?
What happens during the actual treatments with external radiation?
What is brachytherapy?
How long will my external radiation therapy take?
What is a boost dose of radiation?
What is intraoperative radiation therapy?
What is hyperfractionated radiation therapy?
What is radiosurgery ablation?
Can I take vitamins during radiation treatment?
What is chemotherapy? How does it work? How is the treatment taken?
What are SERMs? How do they work?
What are aromatase inhibitors? How do they work?
What is Arimidex?
What is Taxol?
What are the different classes of chemotherapy (chemo) drugs used to treat breast cancer?
What are adjuncts?
What is bone marrow transplantation?

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