SERMs (Selective Estrogen Receptor Modulators)

Selective estrogen receptor modulators, called SERMs for short, block the effects of estrogen in the breast tissue. SERMs work by sitting in the estrogen receptors in breast cells. If a SERM is in the estrogen receptor, there is no room for estrogen and it can't attach to the cell. If estrogen isn't attached to a breast cell, the cell doesn't receive estrogen's signals to grow and multiply.

Cells in other tissues in the body, such as bones and the uterus, also have estrogen receptors. But each estrogen receptor has a slightly different structure, depending on the kind of cell it is in. So breast cell estrogen receptors are different from bone cell estrogen receptors and both of those estrogen receptors are different from uterine estrogen receptors. As their name says, SERMs are "selective" – this means that a SERM that blocks estrogen's action in breast cells can activate estrogen's action in other cells, such as bone, liver, and uterine cells.

There are three SERMs:

• tamoxifen (also called tamoxifen citrate; brand name: Nolvadex)
• Evista (chemical name: raloxifene)
• Fareston (chemical name: toremifene)

Each is a pill, usually taken once a day. Tamoxifen is the oldest, most well-known, and most-prescribed SERM.

SERMs can be used to treat women both before and after menopause.

Benefits of SERMs

Because tamoxifen is the most commonly used SERM, most of the studies comparing SERMs to aromatase inhibitors have looked at tamoxifen versus aromatase inhibitors. Several studies have compared tamoxifen with aromatase inhibitors to see which type of medicine was more effective in treating early-stage, hormone-receptor-positive breast cancer in post-menopausal women. Based on the results, most doctors go by the following recommendations:

• An aromatase inhibitor is the best type of hormonal therapy to start with for post-menopausal women. When treating early-stage, hormone-receptor-positive breast cancer, aromatase inhibitors have more benefits and fewer serious side effects than tamoxifen.
• Switching to an aromatase inhibitor after taking tamoxifen for 2 to 3 years (for a total of 5 years of hormonal therapy) offers more benefits than 5 years of tamoxifen. Taking an aromatase inhibitor for 5 years after taking tamoxifen for 5 years continues to reduce the risk of the cancer coming back, compared to no treatment after tamoxifen.
• Taking an aromatase inhibitor for 5 years after taking tamoxifen for 5 years continues to reduce the risk of the cancer coming back, compared to no treatment after tamoxifen.

For pre-menopausal women diagnosed with hormone-receptor-positive breast cancer, the SERM tamoxifen is the hormonal therapy treatment standard.

Side effects of SERMs

SERMs may cause some serious side effects, including blood clots, stroke, and endometrial cancer. If you and your doctor are considering tamoxifen or another SERM as part of your treatment plan, tell your doctor if you smoke or have a history of blood clots or heart attack. If you're taking a SERM, call your doctor immediately if you have any of these symptoms:

• abnormal vaginal bleeding or discharge
• pain or pressure in the pelvis
• leg swelling or tenderness
• chest pain
• shortness of breath
• weakness, tingling, or numbness in your face, arm, or leg
• sudden difficulty seeing
• dizziness
• sudden severe headache

The most common side effects of SERMs are:

• fatigue
• hot flashes
• night sweats
• vaginal discharge
• mood swings

Hot flashes or night sweats from taking a SERM can be troubling. But a 2008 British study suggests that women who experienced hot flashes and night sweats while taking hormonal therapy medicine were less likely to have the breast cancer come back (recur). Knowing that this side effect might indicate a reduced risk of the cancer coming back may help some women stick with treatment despite the side effects.

As a benefit, SERMs also can improve bone density, which reduces the risk of osteoporosis.

See the pages on tamoxifen, Evista, and Fareston for more information on each medicine.