Aromatase Inhibitors: What You Need to Know! (Updated 2022)

Aromatase is an enzyme that converts testosterone and other male sex hormones called androgens into estrogen, the primary female sex hormone. This conversion process is why men don’t have as much estrogen as women. Aromatase inhibitors are drugs that reduce estrogen production in men and women by limiting the number of aromatase enzymes available to convert androgens into estrogens.

In doing so, aromatase inhibitors can help treat a variety of conditions, including breast cancer in postmenopausal women. Because both men and women have aromatase enzymes, this treatment is not recommended for both genders unless it’s part of another treatment plan. Read on to learn more about aromatase inhibitors and how they may be able to help you manage your specific condition.

What is an Aromatase Inhibitor?

An aromatase inhibitor is a drug that reduces the amount of estrogen produced by the body. Aromatase inhibitors treat men with breast cancer and women with breast cancer who have gone through menopause. Aromatase inhibitors work in a few different ways. Some work by inhibiting the production of the aromatase enzyme.

Others work by blocking the receptor site that binds to estrogen and prevents the conversion of androgens into estrogen. Aromatase inhibitors are often prescribed to men and postmenopausal women with breast cancer to reduce the risk of breast cancer recurrence.

How do Aromatase Inhibitors Work?

There are two primary ways aromatase inhibitors work:

Inhibiting the Production of the Aromatase Enzyme: This is done by drugs like letrozole, anastrozole, exemestane, and letrozole. When the body absorbs these drugs, they bind to the aromatase enzyme, inhibiting the production of more. Down-regulating aromatase enzymes are the primary way aromatase inhibitors reduce estrogen levels in the body. 

Blocking the Receptor Site that Binds to Estrogen: Drugs like aminoglutethimide, metformin, and clomifene do not inhibit aromatase enzyme production. Instead, they bind to estrogen receptors in the body and prevent estrogen from attaching to those receptors.

This way, estrogen production is still blocked, but the body is not deprived of estrogen entirely. Breast cancer cells need estrogen to grow, so blocking estrogen receptors can be used as a type of breast cancer treatment called “endocrine therapy.”

Uses of Aromatase Inhibitors

  • Treating Breast Cancer: Aromatase inhibitors are commonly used to reduce the risk of breast cancer recurrence in men and postmenopausal women. This is because breast cancer is driven by estrogen, so reducing estrogen levels in a person’s body can help to prevent breast cancer from coming back. 
  • Treating Gynecomastia: Aromatase inhibitors are also sometimes used to treat gynecomastia (unusual development of breast tissue in men) and reduce the risk of gynecomastia in breast cancer patients. 
  • Preventing Osteoporosis: Aromatase inhibitors may also be prescribed as part of a treatment plan to prevent osteoporosis in postmenopausal women.

Side Effects of Aromatase Inhibitors

Hot Flashes: Hot flashes are one of the most common side effects experienced by men taking aromatase inhibitors. Hot flashes are often described as feeling like intense bursts of heat or sudden flashes of heat that come on without warning. They can be so severe that they interrupt daily activities and sleep. 

Weakness: Reduced muscle mass and strength are other common side effect of aromatase inhibitors. This can lead to difficulty getting around and performing normal activities of daily living. 

Weakening of the Bones: Aromatase inhibitors can also lead to weaker bones and a higher risk of fractures because estrogen plays a key role in bone health.

Important notes regarding aromatase inhibitors

Existing Medical Conditions: Aromatase inhibitors can greatly reduce estrogen levels in the body, which is why they are recommended for some people with breast cancer. But this is also why they are not recommended for everyone with breast cancer. People who have existing medical conditions that rely on a certain amount of estrogen should not take aromatase inhibitors. Examples of these conditions include people with diabetes, epilepsy, or depression

Pregnant and Breastfeeding Women: Pregnant and breastfeeding women should not take aromatase inhibitors. This is because the drugs can be transferred through the placenta and breast milk and negatively affect the baby.

Final Words: Understanding Aromatase Inhibitors

Aromatase inhibitors are a treatment option for breast cancer patients and are often used to reduce the risk of breast cancer recurrence in men and postmenopausal women. These drugs work by lowering estrogen levels in the body and are often prescribed as part of an endocrine therapy treatment plan.

These drugs can also be very helpful for those with gynecomastia (unusual development of breast tissue in men) or other conditions that are estrogen-driven. Although aromatase inhibitors can be helpful, they come with various side effects, and they are not advised for everyone with breast cancer.


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