Antiandrogens: Uses, most common brand names, and safety information

Medically reviewed by  Jamie Winn, PharmD

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Prostate cancer is the most commonly diagnosed cancer and the second leading cause of cancer death in American men. It is estimated that 1 in 8 men will develop prostate cancer in their lifetime. The beneficial effects of androgen deprivation therapy on prostate cancer were discovered in 1941.

The steroidal antiandrogen Androcur (cyproterone acetate) was introduced in 1973 and is often described as the first antiandrogen to have been marketed.

Eulexin (flutamide) was introduced in 1983 as the first nonsteroidal antiandrogen marketed. Other first-generation nonsteroidal antiandrogens were approved and marketed over the next decade. In 2012, the first second-generation nonsteroidal antiandrogen Xtandi (enzalutamide) was approved, followed by Erleada (apalutamide) in 2018. The second-generation antiandrogens are more effective in preventing the biosynthesis of androgens in comparison to the earlier nonsteroidal antiandrogens.

The list below includes the best non-steroidal antiandrogens approved by the U.S. Food and Drug Administration (FDA) and their pricing:

List of Antiandrogens

Other examples include progesterone agents, steroidal antiandrogens, or 5-alpha reductase inhibitors such as:

• Androcur (cyproterone acetate)
• Provera (medroxyprogesterone acetate)
• Aldactone (spironolactone)
• Proscar (finasteride)

What are antiandrogens?

Androgens are a group of sex hormones such as testosterone and dihydrotestosterone (DHT). Typically people born with male sex characteristics have higher levels of androgens, while those born with female characteristics have higher levels of estrogen. Androgens are mainly made by the testicles but are also made by the adrenal glands and prostate cancer cells themselves.

Antiandrogen medications block the effects of these hormones by binding to androgen receptors. This group of medications is also called androgen receptor blockers or androgen receptor antagonists. They can be prescribed as part of treatment for metastatic prostate cancer. However, hormone therapy alone will not cure prostate cancer. Antiandrogens are typically used in addition to testosterone lowering therapies such as:

• Luteinizing hormone-releasing hormone (LHRH) agonist. Also called gonadotropin-releasing hormone (GnRH) agonists, LHRH agonists such as Lupron (leuprolide) are a type of medical castration used to reduce androgen levels. Clinical trials have shown that this combination of medications can increase the survival rate of advanced prostate cancer patients.
• Luteinizing hormone-releasing hormone (LHRH) antagonist. Medications such as Orgovyx (relugolix) inhibit the brain from signaling the testicles to produce testosterone.
• Surgical castration (orchiectomy). This surgical procedure involves the removal of the testes to lower androgen production.

How do antiandrogens work?

By blocking androgen hormones such as testosterone, antiandrogens can treat a number of androgen-dependent conditions. Some antiandrogens target the biosynthesis of testosterone through the inhibition of an enzyme produced in the testicles and adrenal glands. This inhibits androgen production which helps shrink tumors and slow down the spread of cancer cells. This can help prolong survival in conditions such as castration-resistant prostate cancer.

What conditions are antiandrogens used to treat?

Antiandrogens are a form of hormone therapy that is used in the treatment of prostate cancer. They are typically combined with surgical castration or other medications that lower testosterone levels. Antiandrogens are also treatment options for benign prostatic hyperplasia (BPH) and androgenic hair loss (alopecia).

In women, they are used as a treatment for polycystic ovary syndrome (PCOS), excessive hair growth (hirsutism), absence of menstrual periods (amenorrhea), and adrenal gland tumors. Antiandrogen therapy is also under investigation for the potential treatment of breast cancer.

Are antiandrogens safe?

When taken as prescribed, antiandrogens are safe and effective. You tell your healthcare provider if you have any of the following:

• Liver impairment
• Lung disease
• Kidney disease
• Diabetes
• Are pregnant, plan on becoming pregnant, or are breastfeeding

Can you take antiandrogens while you are pregnant or breastfeeding?

Antiandrogens may cause fetal harm so they are contraindicated for use during pregnancy.

There is limited information on whether antiandrogens are found in breast milk. Based on the potential for adverse events, antiandrogen use during lactation is not recommended.

What are the common side effects of antiandrogens?

Some common side effects of Antiandrogens include:

• Sexual dysfunction (loss of sex drive or erectile dysfunction)
• Diarrhea
• Nausea
• Vomiting
• Fatigue
• Hot flashes
• Dizziness
• Rash
• Loss of muscle mass
• Decreased facial or body hair
• Weight gain
• Increased cholesterol levels

Antiandrogens can sometimes cause severe adverse effects, including:

• Hepatic (liver) impairment
• Seizures
• Breast enlargement in men (gynecomastia)
• Anemia
• Loss of bone density (osteoporosis)

This is not a complete list of side effects and we encourage you to consult with your healthcare professional for medical advice about any possible side effects.

How much do antiandrogens cost?

Antiandrogens are very expensive with an average cost of around $10,000 per year, depending on the medication.

You can purchase antiandrogens for $49 per month from NiceRx if eligible for assistance. Prices at the pharmacy vary by location, strength, and quantity, as well as your insurance status.

Related resources for antiandrogens

• Antiandrogenic drugs. National Library of medicine
• What are anti-androgens? Healthline
• How do antiandrogens work? RxList
• Hormone therapy for prostate cancer. National Cancer Institute