Apalutamide (Erleada)

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General information

Class/mechanism: Antiandrogen; androgen receptor inhibitor (ARI). Apalutamide competitively inhibits activity mediated by the androgen receptor (AR) by binding directly to the AR ligand-binding domain, nuclear translocation, DNA binding, and AR-mediated transcription. A metabolite of apalutamide, N-desmethyl apalutamide, also exhibits some AR inhibiting activity, about 1/3 that of apalutamide.[1][2][3]
Route: PO
Extravasation: n/a

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1]

Diseases for which it is used

Patient drug information

History of changes in FDA indication

  • 2/14/2018: FDA approved for patients with non-metastatic castration-resistant prostate cancer (NM-CRPC). (Based on SPARTAN)
  • 9/17/2019: Approved for patients with metastatic castration-sensitive prostate cancer (mCSPC). (Based on TITANprostate)

History of changes in EMA indication

  • 1/14/2019: Initial marketing authorization as Erleada.

Also known as

  • Code name: ARN-509
  • Brand name: Erleada