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What is the AI 6 pill? Understanding Exemestane (Aromasin)

4 min read

Approximately 70% of all breast cancers are hormone receptor-positive (ER-positive). For many postmenopausal women, treatment involves hormonal therapy. So, what is the AI 6 pill? It is a tablet of Exemestane, a potent medication used in this fight.

Quick Summary

The AI 6 pill is the medication Exemestane, a type of hormone therapy known as an aromatase inhibitor. It is primarily used to treat hormone-receptor-positive breast cancer in postmenopausal women.

Key Points

  • Identification: The 'AI 6' pill is a 25 mg tablet of Exemestane, an aromatase inhibitor also known by the brand name Aromasin®.

  • Primary Use: Its main approved use is treating hormone-receptor-positive breast cancer in postmenopausal women, often after initial treatment with tamoxifen.

  • Mechanism of Action: Exemestane is a steroidal, irreversible inhibitor that permanently deactivates the aromatase enzyme, significantly lowering the body's estrogen levels.

  • Key Risks: The most significant side effects are related to low estrogen and include a decrease in bone mineral density (risk of osteoporosis), joint pain, hot flashes, and fatigue.

  • Proper Administration: Exemestane is typically taken once daily, often after a meal to enhance absorption.

  • Unapproved Use Warning: Exemestane is misused in bodybuilding to control estrogenic side effects from steroids, but this is illegal for that purpose and banned by anti-doping agencies.

In This Article

Identifying the 'AI 6' Pill

When you see a pill with the imprint "AI 6," it's important to know you are handling a specific prescription medication. This pill is identified as a tablet of Exemestane, which is the generic name for the drug also sold under the brand name Aromasin®. The "AI" likely refers to the manufacturer, while the "6" is part of the specific identifier for this product. Exemestane belongs to a class of drugs called aromatase inhibitors, which are a cornerstone of modern hormone therapy for specific types of cancer.

How Does Exemestane Work?

The mechanism of action for Exemestane is highly specific and effective. It is a steroidal, irreversible aromatase inhibitor. To understand what this means, we must first look at the aromatase enzyme.

In postmenopausal women, the primary source of estrogen is the conversion of androgens (hormones produced by the adrenal glands) into estrogen. The enzyme responsible for this conversion is aromatase. Some breast cancers, known as hormone receptor-positive (HR+) cancers, use estrogen as a fuel to grow and spread.

Exemestane works by binding permanently to the aromatase enzyme, effectively deactivating it. This is why it's called a "suicidal" or irreversible inhibitor. By blocking this enzyme, Exemestane drastically reduces the amount of estrogen circulating in the body—by as much as 85-95%—thereby cutting off the fuel supply to the cancer cells.

Primary Medical Uses for the AI 6 Pill

Exemestane is not a general-purpose medication; it is prescribed for very specific conditions approved by regulatory bodies like the FDA.

  • Adjuvant Treatment for Early Breast Cancer: It is used in postmenopausal women who have estrogen-receptor-positive early breast cancer. Typically, these patients have already completed 2 to 3 years of treatment with another hormone therapy called tamoxifen and are then switched to Exemestane to complete a total of five years of hormonal treatment.
  • Treatment of Advanced Breast Cancer: It is also indicated for postmenopausal women with advanced breast cancer whose disease has progressed despite treatment with tamoxifen.

It is crucial to note that this medication is intended for postmenopausal women because their main source of estrogen is the one targeted by the drug.

Comparison of Aromatase Inhibitors

Exemestane is one of three common third-generation aromatase inhibitors. The others are Anastrozole (Arimidex) and Letrozole (Femara). While they all work to lower estrogen, there are key differences between them.

Feature Exemestane (Aromasin) Anastrozole (Arimidex) Letrozole (Femara)
Type Steroidal Non-steroidal Non-steroidal
Mechanism Irreversible ("suicidal") binder Reversible inhibitor Reversible inhibitor
Key Characteristic Has mild androgenic activity, which may result in a different side effect profile. Can be effective after non-steroidal AIs fail. Highly selective for the aromatase enzyme. Considered a potent estrogen suppressor.
Common Side Effects Hot flashes, fatigue, joint pain, risk of bone density loss. Hot flashes, joint pain, bone thinning, potential for increased cholesterol. Joint pain, hot flashes, fatigue, bone thinning.

Side Effects, and Risks

Administration

Exemestane is typically taken once daily. It is often recommended to take the tablet after a meal, as this can increase the drug's absorption in the body. If a dose is missed, it's generally advised to take it as soon as remembered, unless it is close to the time for the next scheduled dose, in which case the missed dose should be skipped.

Potential Side Effects

Like all powerful medications, Exemestane can cause side effects. These are largely related to the drastic reduction in estrogen.

Common side effects include:

  • Hot flashes
  • Fatigue or tiredness
  • Joint, muscle, or back pain (arthralgia)
  • Headache
  • Difficulty sleeping (insomnia)
  • Increased sweating

Serious risks and long-term effects:

  • Decreased Bone Mineral Density: A significant risk is the loss of bone density, which can lead to osteoporosis and an increased risk of fractures. Patients are often monitored for this and may be advised to take calcium and vitamin D supplements.
  • Cardiovascular Events: Some studies have noted a slightly higher incidence of cardiac events, like heart attacks, compared to tamoxifen.
  • Drug Interactions: Exemestane should not be taken with estrogen-containing medications. Its effectiveness can also be reduced by strong CYP3A4 inducers, such as St. John's wort or certain seizure medications like phenytoin.

Off-Label and Unapproved Uses

It is important to address the off-label use of Exemestane, particularly in bodybuilding. Some individuals use aromatase inhibitors to counteract the side effects of anabolic steroid use. Anabolic steroids can increase estrogen levels, leading to unwanted effects like gynecomastia (male breast development) and water retention. Exemestane is used to prevent this by suppressing estrogen.

This use is not medically approved and is considered misuse of the drug. The World Anti-Doping Agency (WADA) has banned aromatase inhibitors for use in sports. The health risks associated with using this powerful drug without medical supervision for non-approved purposes can be significant.

Conclusion

The AI 6 pill is correctly identified as Exemestane 25 mg, a potent steroidal aromatase inhibitor used primarily in the treatment of hormone-receptor-positive breast cancer in postmenopausal women. By irreversibly blocking the enzyme that produces estrogen, it plays a vital role in cutting off the fuel for certain cancers. While effective, it carries notable risks, including bone density loss and joint pain, and must be used strictly under medical supervision. Its unapproved use in contexts like bodybuilding is dangerous and strongly discouraged.

For more information, you can visit MedlinePlus, a service of the National Library of Medicine.

Frequently Asked Questions

The AI 6 pill is a 25 mg tablet of Exemestane, an oral medication belonging to a class of drugs called aromatase inhibitors. It's often known by its brand name, Aromasin®.

Exemestane is primarily used to treat hormone-receptor-positive breast cancer in women who have gone through menopause. It is often prescribed after 2-3 years of tamoxifen treatment or if the cancer has progressed after tamoxifen therapy.

They work differently. Exemestane is an aromatase inhibitor that stops estrogen production. Tamoxifen is a Selective Estrogen Receptor Modulator (SERM) that blocks estrogen's effects on cancer cells. They are often used sequentially in breast cancer treatment.

Taking Exemestane after a meal is recommended because it can significantly increase the body's absorption of the medication, making it more effective.

While Exemestane's primary approval is for postmenopausal women, it is sometimes used off-label in men to treat certain conditions or to illegally counteract side effects of steroid use in bodybuilding. This should only be done under strict medical guidance.

The most common side effects are related to low estrogen levels and include hot flashes, fatigue, joint pain, headaches, and trouble sleeping. A more serious long-term risk is decreased bone mineral density.

The duration of treatment can be several years. For early breast cancer, it's often used to complete a total of five consecutive years of adjuvant hormone therapy after a patient has already taken tamoxifen for 2-3 years.

References

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Medical Disclaimer

This content is for informational purposes only and should not replace professional medical advice.