National Stroke Foundation

Erleada (apalutamide)

The following drug information is obtained from various newswires, published medical journal articles, and medical conference presentations.

Company:

Approval Status:

Approved February 2018

Specific Treatments:

prostate cancer

Therapeutic Areas

General Information

Erleada (apalutamide) is an androgen receptor inhibitor.

Erleada is specifically indicated for the treatment of 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. 

Clinical Results

FDA Approval

The FDA approval of Erleada 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).

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

 

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. 

Additional Information

For additional information regarding Erleada or non-metastatic castration-resistant prostate cancer, please visit https://www.erleada.com/