Apalutamide (Erleada)

From HemOnc.org - A Hematology Oncology Wiki
Jump to: navigation, search

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

Also known as

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

References

  1. 1.0 1.1 1.2 Apalutamide (Erleada) package insert
  2. Apalutamide (Erleada) package insert (locally hosted backup)
  3. Erleada manufacturer's website
  4. Apalutamide (Erleada) patient drug information (Chemocare)
  5. Apalutamide (Erleada) patient drug information (UpToDate)