What is the mechanism of action for Erleada?

Erleada is an oral medicine for prostate cancer that works by blocking the effects of androgen. Androgens are male hormones (like testosterone) that are needed for prostate function but can also stimulate cancer growth. Blocking androgens can help stop the growth and spread of prostate cancer cells.

Specifically, Erleada belongs to a class of medications called androgen receptor (AR) inhibitors and blocks AR signaling at multiple sites of action. It binds directly to the ligand-binding domain of the AR, inhibits AR nuclear translocation, inhibits DNA binding and impedes AR-mediated transcription. It is not considered a chemotherapy treatment.

Erleada (apalutamide) is approved by the FDA for the treatment of patients with:

• Metastatic castration-sensitive prostate cancer (mCSPC) - mCSPC is prostate cancer that has spread in the body (metastatic) but still responds to a medical or surgical treatment that lowers testosterone (castration-sensitive).
• Non-metastatic castration-resistant prostate cancer (nmCRPC)- nmCRPC is prostate cancer that has not spread in the body (non-metastatic), after surgery or other treatments that did not fully work or have stopped working (castration-resistant).

Erleada is not approved for use in women or children.

Other second-generation anti-androgen options used in the treatment of prostate cancer include:

• enzalutamide (Xtandi)
• darolutamide (Nubeqa)

How is Erleada taken?

Erleada is taken by mouth, once a day (either as one 240 mg tablet or four 60 mg tablets). It can be taken with or without food.

If you have trouble swallowing tablets, let your doctor know. You can also take Erleada mixed in orange juice, applesauce or non-carbonated water, but ask your doctor or pharmacist for directions on how to do this first.

Do I take other medicines with Erleada?

Patients taking Erleada should also receive either a GnRH analog hormonal drug treatment (an androgen deprivation therapy or ADT) or should have had a bilateral orchiectomy (surgical removal of both testicles).

In the U.S., androgen deprivation therapy using medications (“medical castration”) is usually preferred over surgical castration (surgical removal of the testicles). Examples of the medicines used for ADT include:

Gonadotropin-releasing hormone (GnRH) agonists

GnRH agonists work by lowering the amount of testosterone made by the testicles. This causes the prostate to shrink. They are given as injections every 1 to 6 months, as a long-lasting (12 month) depot injection, or as an implant (under the skin) depending on the drug and prescribed dosage.

• leuprolide (Lupron Depot, Eligard)
• leuprolide mesylate (Camcevi)
• goserelin (Zoladex)
• triptorelin (Trelstar)

When GnRH agonist treatment is first started, there may be a temporary increase of androgen production (a "flare") before levels start to decline. Thus can temporarily worsen symptoms, like bone pain, spinal cord compression and urinary problems​​​​ for days to weeks​​​​.

Your doctor may prescribe another medicine, called an antiandrogen, to help reduce your symptoms during this flare. Examples of antiandrogens include flutamide and bicalutamide (Casodex), both given as oral medicines.

Related questions

• Erleada vs. Xtandi: What's the difference?
• How long do you have to take Erleada (apalutamide) for?
• How effective is Erleada (apalutamide)?

Gonadotropin-releasing hormone (GnRH) antagonists

GnRH antagonists can be used for more advanced prostate cancer faster and may be faster-acting than GnRH agonists. Like GnRH agonists, they also stop production of androgens from the testicles, but without causing an initial testosterone surge. Firmagon is given as an injection, while Orgovyx is available as an oral tablet.

• degarelix (Firmagon)
• relugolix (Orgovyx)

What kind of side effects can occur with Erleada?

The most common side effects you might experience with Erleada treatment include:

• feeling very tired or exhausted
• joint pain
• rash (tell your doctor if you develop a rash)
• decreased appetite
• a fall
• decreased weight
• high blood pressure
• hot flush or “flash”
• diarrhea
• bone fracture.

More serious side effects can happen too. These might include heart disease, a stroke or mini-stroke, fractures and falls, seizures, and severe skin reactions that can be life-threatening or may lead to death.

Learn more: Erleada side effects (in more detail)

This is not all the information you need to know about Erleada (apalutamide) for safe and effective use and does not take the place of your healthcare provider’s directions. Review the full product information and discuss this information and any questions you have with your doctor or other health care provider.