Erleada

Approved Indications

Erleada is used to treat two primary forms of prostate cancer:

• Non-metastatic castration-resistant prostate cancer (nmCRPC): This is prostate cancer that has not yet spread to other parts of the body on imaging tests, but no longer responds to medical or surgical treatments that lower testosterone levels.
• Metastatic castration-sensitive prostate cancer (mCSPC): This is prostate cancer that has already spread to other parts of the body, such as the bones or lymph nodes, but still responds to medical or surgical treatments that lower testosterone.

Treatment Context

This medication is typically used in patients who are also receiving androgen deprivation therapy (ADT). This may involve the use of other medications to lower testosterone levels or a history of surgery to remove the testicles. Erleada works by blocking the effect of hormones like testosterone to help slow the growth and spread of the cancer.

Mechanism of Action

Erleada belongs to a class of medications known as androgen receptor inhibitors. It is designed to treat prostate cancer by interfering with the way the body uses certain hormones.

Prostate cancer cells often rely on male hormones, called androgens (such as testosterone), to grow and multiply. Erleada works by targeting the androgen receptors on these cancer cells through several steps:

• Blocking hormone attachment: The medication binds to androgen receptors, which prevents hormones like testosterone from attaching to the cancer cells.
• Stopping receptor movement: It prevents the androgen receptors from moving into the nucleus of the cell, where they would normally trigger growth.
• Inhibiting DNA interaction: It stops the receptors from interacting with the cell's DNA, which effectively cuts off the signals that tell the cancer cell to divide and spread.

By disrupting these hormonal signals, Erleada helps to slow the progression of the disease and may help shrink tumors, even in cases where the cancer has become resistant to other types of hormone therapy.

Common Side Effects

Many people taking Erleada experience mild to moderate side effects. These may include:

• Fatigue or extreme tiredness
• Joint, muscle, or bone pain
• Skin rash
• Nausea or diarrhea
• Hot flashes
• High blood pressure
• Decreased appetite and weight loss

Serious Side Effects

Erleada may cause serious side effects that require prompt medical evaluation. These include:

• Seizures or loss of consciousness
• Increased risk of falls and bone fractures
• Heart disease, which may cause chest pain or shortness of breath
• Stroke or mini-stroke symptoms, such as sudden weakness or numbness
• Severe skin reactions, including peeling or blistering
• Hypothyroidism, or an underactive thyroid, which may cause weight gain or feeling cold

Seizure Risk

Treatment with Erleada has been associated with an increased risk of seizures. If a seizure occurs during treatment, the medication is typically discontinued permanently. Caution is often advised for individuals with a history of seizures or other factors that may increase seizure risk.

Falls and Bone Fractures

Patients taking this medication may have a higher risk of falling and experiencing bone fractures. Healthcare providers may monitor bone health and recommend treatments to help prevent bone loss or manage fracture risk during therapy.

Heart and Brain Circulation Issues

Serious heart problems, such as heart attacks or chest pain (ischemic heart disease), and strokes (ischemic cerebrovascular disorders) have occurred in patients taking Erleada. Some of these events have been fatal. Monitoring for signs and symptoms of cardiovascular or cerebrovascular issues is important during treatment.

Severe Skin Reactions

Serious skin reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis, have been reported with the use of this medication. Treatment should be stopped if a severe rash, skin peeling, or mucosal sores develop.

Thyroid Function

This medication can cause hypothyroidism, which is an underactive thyroid. Healthcare providers may check thyroid-stimulating hormone (TSH) levels periodically to monitor thyroid function while a patient is taking Erleada.

Reproductive Risks

Erleada can cause harm to an unborn baby and is not intended for use in women. Men with female partners who could become pregnant should use effective contraception during treatment and for three months after the final dose. Men should also avoid donating sperm during this period.

Pregnancy Risks

Erleada is not approved for use in women. Research indicates that the medication can cause fetal harm, including birth defects or loss of the pregnancy, if exposure occurs. Because the drug may be present in semen, it is important to prevent exposure to a partner who is pregnant or could become pregnant.

Precautions for Men

Men taking Erleada who have female partners of reproductive potential should follow these safety measures:

• Contraception: Use a condom and another form of highly effective birth control during treatment and for 3 months after the last dose.
• Sperm Donation: Do not donate sperm during treatment and for 3 months after the final dose to prevent potential exposure to others.

Breastfeeding

Erleada is not indicated for use in women. There is no information regarding its presence in human breast milk or its effects on a breastfed child. Women who are breastfeeding should consult their healthcare provider if they have concerns about environmental exposure.

Dosage Forms

Erleada is supplied as a tablet intended for oral use. The tablets are usually swallowed whole.

For individuals who have difficulty swallowing tablets, the medication may be administered by dispersing the tablets in specific liquids, such as water, apple juice, or orange juice. Alternatively, the tablets may be mixed with soft foods like applesauce. Patients should follow specific preparation instructions provided by their healthcare provider when using these alternative administration methods.

FDA Approval History

Erleada (apalutamide) received its initial FDA approval in February 2018. It was the first medication specifically approved for the treatment of patients with non-metastatic castration-resistant prostate cancer (nmCRPC). This condition occurs when the cancer has not spread to other parts of the body but no longer responds to medical or surgical treatments that lower testosterone.

Expanded Indications

In September 2019, the FDA expanded the approved use of Erleada to include the treatment of metastatic castration-sensitive prostate cancer (mCSPC). This indication applies to patients whose prostate cancer has spread to other areas of the body but still responds to hormone therapy.

Safety Communications and Labeling Updates

The FDA monitors the safety of Erleada through the FDA Adverse Event Reporting System (FAERS). In 2020, the FDA identified potential signals of serious risks based on adverse event reports, which led to updates in the drug's official labeling. These safety concerns include:

• Cerebrovascular accidents (such as stroke)
• Ischemic heart disease

There is currently no Risk Evaluation and Mitigation Strategy (REMS) program required for Erleada, and it does not carry a boxed warning. Patients are monitored for these and other potential side effects, such as seizures and fractures, as part of standard clinical care.

Insurance and Coverage

The out-of-pocket cost for Erleada is primarily determined by your health insurance plan. Most Medicare Part D and private insurance plans provide coverage for this medication, but it is often categorized as a specialty drug. This classification may result in higher copayments or coinsurance. Many insurance providers also require prior authorization, a process where your healthcare provider must confirm the medical necessity of the drug before the insurer will cover the cost.

Generic Availability

Erleada is a brand-name medication containing the active ingredient apalutamide. There is currently no generic version of apalutamide available. Brand-name drugs are typically more expensive than generics because they are protected by patents that prevent other companies from producing the same medication for a specific period.

Financial Assistance Programs

Several options may be available to help manage the cost of Erleada:

• Manufacturer Savings: The pharmaceutical company that produces Erleada may offer copay cards or savings programs for eligible patients with commercial insurance to help lower monthly expenses.
• Patient Assistance Programs: These programs are often available for individuals who are uninsured or underinsured and meet specific income requirements. They may provide the medication at a reduced cost or for free.
• Non-profit Organizations: Some independent foundations provide grants to help patients cover the costs of cancer treatments and related medications.