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SERMs: Underused and under the radar

The selective estrogen receptor modulators tamoxifen and raloxifene have been shown to reduce the risk for breast cancer in women at high risk by as much as 50%. With an accumulation of years of clinical trial data testing both drugs, a high rate of efficacy in the target population and highly favorable adverse effects profiles, these two drugs are considered two of the bigger success stories among chemopreventive methods.

“I have worked with tamoxifen for 20 years and raloxifene for almost a decade, and I don’t think that it is an exaggeration to say that tamoxifen is probably the most important cancer drug yet to be discovered,” said Victor G. Vogel, MD, director of the Geisinger Cancer…

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 The Secrets of SERMs

Raloxifene has also proven effective in the prevention of breast cancer without raising the risk of endometrial cancer after scientists tested it in post-menopausal women who, aside from their age, had no other apparent risk factors. A large-scale clinical trial called the Study of Tamoxifen and Raloxifene (STAR) demonstrated that both compounds showed a decrease in breast cancer in high-risk women, and raloxifene produced fewer adverse effects.

Articles of Interest

Is there still a role for SERMs in menopause management?

Selective Estrogen Receptor Modulators (SERMs) are non-hormonal compounds that can act as estrogen-agonist or antagonist according to the different target tissues. For instance, a SERM may be an estrogen agonist on bone tissue and, conversely, a potent estrogen antagonist on breast tissue.

Selective Estrogen Receptor Modulators

Selective estrogen receptor modulators (SERMs) are now being used as a treatment for breast cancer, osteoporosis and postmenopausal symptoms, as these drugs have features that can act as an estrogen agonist and an antagonist, depending on the target tissue. After tamoxifen, raloxifene, lasofoxifene and bazedoxifene SERMs have been developed and used for treatment. The clinically decisive difference among these drugs (i.e., the key difference) is their endometrial safety.

SERMs & Aromatase Inhibitors

SERMs, such as Tamoxifen and Raloxifene, compete with estrogen for receptor binding thereby inhibiting tumor growth. However, it's important to note that SERMs aren't pure antagonists and exhibit partial agonist activity on the endometrium, skeletal, and cardiovascular systems.

SERMs May Be Healthier Choice Than HRT

'Designer estrogens' don't increase breast cancer risk.

SERMs: Meeting the Promise of Multifunctional Medicines

The successful development and clinical evaluation of the selective estrogen receptor modulators in the Study of Tamoxifen and Raloxifene trial provides an occasion to reflect on the milestone that has been achieved and the potential for further progress in the chemoprevention of breast cancer.

The Effect of Selective Estrogen Receptor Modulators (SERMs) on the Tamoxifen Resistant Breast Cancer Cells

Selective estrogen receptor modulators (SERMs) are synthetic molecules which bind to estrogen receptors (ER) and can modulate its transcriptional capabilities in different ways in diverse estrogen target tissues. Tamoxifen, the prototypical SERM, is extensively used for targeted therapy of ER positive breast cancers. Unfortunately, the use of tamoxifen is associated with acquired resistance and some undesirable side effects.

Resources

BreatCancer.org

Selective estrogen receptor modulators (SERMs) are one of three types of hormonal therapy medicines used to treat estrogen receptor-positive breast cancer in women — both pre- and post-menopausal — and men. There are three SERMs doctors use to treat breast cancer: tamoxifen in pill form, also called tamoxifen citrate (brand name Nolvadex), and in liquid form (brand name: Soltamox). Evista (chemical name: raloxifene), Fareston (chemical name: toremifene).