General Information

Erleada (apalutamide) is an androgen receptor inhibitor.

Erleada is specifically indicated for the treatment metastatic castration-sensitive prostate cancer as well as non-metastatic castration-resistant prostate cancer.

Erleada is supplied as a tablet for oral administration. The recommended dose of Erleada is 240 mg (four 60 mg tablets) administered orally once daily. Swallow the tablets whole. Erleada can be taken with or without food. Patients should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had a bilateral orchiectomy.

If a patient experiences a greater than or equal to Grade 3 toxicity or an intolerable side effect, hold dosing until symptoms improve to less than or equal to Grade 1 or original grade, then resume at the same dose or a reduced dose (180 mg or 120 mg), if warranted. 

Mechanism of Action

Erleada (apalutamide) is an androgen receptor inhibitor that binds directly to the ligand-binding domain of the AR. Apalutamide inhibits AR nuclear translocation, inhibits DNA binding, and impedes AR-mediated transcription.

Side Effects

Adverse effects associated with the use of Erleada may include, but are not limited to, the following:

• fatigue
• hypertension
• rash
• diarrhea
• nausea
• weight decreased
• arthralgia
• fall
• hot flush
• decreased appetite
• fracture
• peripheral edema

Clinical Trial Results

The FDA approval of Erleada for non-metastatic prostate cancer was based on SPARTAN, a Phase III, randomized, double-blind, placebo-controlled, multi-center study conducted in 1,207 subjects with non-metastatic castration-resistant prostate cancer. The subjects were randomized 2:1 to receive either Erleada orally at a dose of 240 mg once daily (n=806), or placebo once daily (n=401). All subjects received a concomitant gonadotropin-releasing hormone (GnRH) analog or had a bilateral orchiectomy. Erleada decreased the risk of distant metastasis or death by 72 percent compared to placebo (P<0.0001). The median MFS was 40.51 months for Erleada compared to 16.20 months for placebo, prolonging MFS by more than two years (difference of 24.31 months). The major efficacy outcome was supported by statistically significant improvements for the following secondary endpoints: time to metastasis (TTM), progression-free survival (PFS) and time to symptomatic progression. The median TTM was 40.51 months for Erleada compared to 16.59 months for placebo (P<0.0001) and the median PFS was 40.51 months compared to 14.72 months for placebo (P<0.0001).

The FDA approval of Erleada for metastatic prostate cancer was based on the phase III TITAN study that included 1,052 patients in 23 countries across 260 sites in North America, Latin America, South America, Europe, and Asia Pacific. The patients with mCSPC were randomized 1:1 and received either Erleada (240 mg) plus ADT or placebo plus ADT. Data showed that Erleada plus ADT significantly extended overall survival (OS) compared to placebo plus ADT, obtaining a 33% decrease in the risk of death. It also significant improved radiographic progression-free survival (rPFS) compared to the control group with a 52% lower risk of radiographic progression or death.