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Understanding Antiandrogen Medicines as a Treatment Option for Your Prostate Cancer

Understanding Antiandrogen Medicines as a Treatment Option for Your Prostate Cancer

This article is for people who have prostate cancer, their care partners, and anyone who wants to learn more about prostate cancer. The goal of this patient education activity is to increase your knowledge about newer antiandrogen medicines as a treatment option for prostate cancer.

You will learn about:

  • Different types of prostate cancer

  • Antiandrogen medicines that may be used to treat prostate cancer and how to take them

  • The most common side effects of antiandrogen medicines and serious side effects that may happen

  • Questions to ask your doctor and healthcare team

All medicines listed in this activity may not be approved by the US Food and Drug Administration (FDA) for prostate cancer but are recommended by the National Comprehensive Cancer Network (NCCN).

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What Is Prostate Cancer?

Prostate cancer develops in the cells of the prostate gland, an organ in men that forms a ring around the urethra (the tube that carries urine from the bladder to outside the body).

When you have prostate cancer, hormones that are normally found in your body, such as testosterone, can cause cancer to grow. So hormone treatment, such as surgery and/or medicine, may be recommended to lower your amount of hormones and help slow prostate cancer growth or shrink it.

Types of Prostate Cancer

There are different types of prostate cancer, depending on:

1. If it gets better from hormone treatment

  • If yes, then it's called castration-sensitive prostate cancer (CSPC)

  • If no, then it's called castration-resistant prostate cancer (CRPC)

2. If it has spread to other parts of your body

  • If no, then it's called non-metastatic (nm or M0)

  • If yes, then it's called metastatic (m or M1)

Both CSPC and CRPC can be either non-metastatic or metastatic.

Androgens and Antiandrogen Medicines

Androgens are a type of hormone that affect features such as having a lower voice and growing facial hair in men. The 2 main androgens that can cause prostate cancer to grow are testosterone and dihydrotestosterone (DHT), which is made from testosterone.

In most prostate cancers, androgens attach to a protein in cancer cells called an androgen receptor. Antiandrogen medicines are a type of hormone treatment that work by blocking these receptors and stopping the androgen from attaching. This can help stop androgens like testosterone from causing prostate cancer cells to grow.

Antiandrogen Medicines to Help Treat Prostate Cancer

Apalutamide (ERLEADA®), darolutamide (NUBEQA®), and enzalutamide (XTANDI®) are the most recent, or newer, antiandrogen medicines that may be used to help treat prostate cancer. Abiraterone acetate (YONSA® or ZYTIGA®) is a type of hormone treatment called an androgen synthesis inhibitor that may also be used and helps block androgens from being made. These medicines are be taken with another medicine called a gonadotropin-releasing hormone (GnRH) analog, unless you've had a bilateral orchiectomy (surgery to remove both testicles).

Other antiandrogen medicines that are older and may be used to help treat prostate cancer include bicalutamide, flutamide, and nilutamide.

Who Are Antiandrogen Medicines For?

Prostate Cancer Type


Non-metastatic CRPC (nmCRPC)





Metastatic CRPC (mCRPC)

Abiraterone acetate (YONSA®, ZYTIGA®)


Metastatic CSPC (mCSPC)

Abiraterone acetate (ZYTIGA®)



How Should Antiandrogen Medicines Be Taken?


How It’s Taken

Abiraterone acetate (YONSA®)

500 mg once daily (with methylprednisolone 4 mg twice daily) with or without food and swallowed whole

Abiraterone acetate (ZYTIGA®)

1000 mg once daily (with prednisone 5 mg once or twice daily, depending on your cancer type) without food and on an empty stomach at least 1 hour before or 2 hours after a meal or snack and swallowed whole


240 mg once daily with or without food and swallowed whole


600 mg twice daily with food and swallowed whole


160 mg once daily with or without food and swallowed whole

Possible Common Side Effects of Antiandrogen Medicines


Most Common Side Effects

Abiraterone acetate

Fatigue (tiredness), joint pain, high blood pressure, nausea, swelling in your legs or feet due to fluid buildup, hot flashes, diarrhea, vomiting, headache, cough, infected nose, sinuses, or throat


Lab test abnormalities: low blood potassium or red blood cells and high cholesterol, triglycerides, or blood sugar


Fatigue, joint pain, decreased appetite, falls, weight loss, high blood pressure, hot flashes, diarrhea, fracture, rash (tell your doctor if you get a rash)


Fatigue, pain in your arm, leg, hand, or foot, rash


Fatigue or weakness, back or joint pain, hot flashes, constipation, decreased appetite, diarrhea, high blood pressure

Possible Serious Side Effects of Antiandrogen Medicines


Serious Side Effects

Abiraterone acetate

High blood pressure, low blood potassium, fluid buildup, irregular heartbeat, adrenal or liver problems


There may be a greater chance of bone fracture and death when ZYTIGA® plus prednisone is used together with a type of radiation called radium Ra 223 dichloride


Heart disease, fractures with falls, seizures


Blood in your urine or being unable to empty your bladder, pneumonia


A condition called posterior reversible encephalopathy syndrome (PRES), seizure, allergic reactions, heart disease, fractures with falls


Serious side effects are not as common, but can happen, so be sure to talk to your doctor and cancer care team if you have questions about them.

Managing Your Side Effects

Be sure to talk to you doctor and care team about any side effects that may happen. Together, you will make a plan to help manage them. Your doctor may recommend medicines to help, lowering your treatment dose, or stopping your medicine for a while. But don't change or stop taking any treatments without talking to your doctor first.

Not all possible side effects are included in this activity, so be sure to ask your doctor for a complete list.

Questions to Ask Your Doctor and Healthcare Team

  • Why are you recommending an antiandrogen medicine for me?

  • Are there any medicines I should not take at the same time?

  • How will my side effects be checked and managed?

  • What can I do to help manage my side effects?

  • How often do my follow-up appointments need to be?

Test Your Knowledge

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You have successfully completed the program Understanding Antiandrogen Medicines as a Treatment Option for Your Prostate Cancer.

View Additional Materials on this topic that you may find useful:

Prostate Cancer

How Is Prostate Cancer Treated?

Hormone Therapy for Prostate Cancer -- National Cancer Institute

Authors and Disclosures

Clinician Reviewer

Karen Badal, MD, MPH

Senior Medical Education Director, Medscape, LLC.

Disclosure: Karen Badal, MD, MPH, has disclosed no relevant financial relationships.


Anita A. Galdieri, PharmD, RPh

Associate Director, Content Development, Medscape, LLC.

Disclosure: Anita A. Galdieri, PharmD, RPh has disclosed no relevant financial relationships.


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