Estrogen blockers are a common medical treatment used to treat gynecomastia symptoms. Gynecomastia is when men who have a female appearance of the chest due to an enlargement of the breast gland behind the nipple-areola complex. Most gynecomastia cases need surgery, but there are certain non-surgical treatments that can be used to minimize or improve the symptoms associated with gynecomastia.


Gynecomastia is usually caused by a hormone imbalance that occurs during puberty. Estrogen, the predominant sex hormone in women, is formed when testosterone is converted to estrogen by an enzyme called aromatase found in the fat cells of the body. During puberty, testosterone levels increase dramatically and subsequently estrogen due to the high levels of testosterone that is converted by the aromatase enzyme. This higher level of estrogen is what causes the development of breast glands in males. When testosterone levels return back to normal levels following the end of puberty, estrogen levels should also return down to normal levels. Unfortunately, if the exposure to high estrogen levels was long enough, the formation of the breast glands becomes permanent.
Knowing this basic physiology of how gynecomastia develops, there is a great interest in the use of medications to help block the effect of estrogen onto the breast gland. Doing this may prevent its progression and to shrink the breast gland enough to a point where surgery is not necessary.

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What are some common medications used to treat gynecomastia?


In general, there are two types of medications that can decrease the effect of messaging on a male.

  • One class of drugs are aromatase inhibitors. Aromatase inhibitors work by stopping the function of the aromatase enzyme that turns testosterone into estrogen. Anastrozole is the most well known aromatase inhibitor.
  • The second class are estrogen receptor blockers. Estrogen receptor blockers block the estrogen receptor on the breast gland tissue, preventing the estrogen from acting on the tissue. Tamoxifen is the well known medication of this class.

Flare ups of gynecomastia occurs when exposure of the breast gland causes enlargement, sensitivity, and tenderness of the nipple-areola complex. In instances where an increase in estrogen is expected, such as in testosterone replacement therapy, estrogen blockers may be used in conjunction with testosterone to prevent the development or progression of gynecomastia.


How does the use of estrogen blockers help with gynecomastia?


The primary use of estrogen blockers in gynecomastia are to treat “flare ups” and prevent worsening of the disease. Estrogen blockers can help decrease the size of the breast gland and prevent further symptoms from occurring. But once the breast gland has formed it is permanent.


Why is estrogen important in men?

Estrogen serves an important function in men as it maintains bone and heart health. Estrogen also balances the mood, preventing over-aggression that can be stimulated by testosterone.

Estrogen levels that are too low in men can lead to many health issues including:

  • Osteoporosis
  • Heart disease
  • Mood disorders
  • Sexual dysfunction
  • Sleep disturbances

Estrogen blockers are not a permanent solution. It may help with the treatment of gynecomastia symptoms. Long term use of these medications are not recommended due to the effects of low estrogen levels in men. Occasional use can help someone who has gynecomastia and is symptomatic. The only permanent treatment of gynecomastia requires surgery to remove the breast gland.

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