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.
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.
Diseases for which it is used
- Rathkopf DE, Antonarakis ES, Shore ND, Tutrone RF, Alumkal JJ, Ryan CJ, Saleh M, Hauke RJ, Bandekar R, Maneval EC, de Boer CJ, Yu MK, Scher HI. Safety and Antitumor Activity of Apalutamide (ARN-509) in Metastatic Castration-Resistant Prostate Cancer with and without Prior Abiraterone Acetate and Prednisone. Clin Cancer Res. 2017 Jul 15;23(14):3544-3551. Epub 2017 Feb 17. PubMed
- Rexer H, Graefen M. Phase III study for local or locally advanced prostate cancer : Randomized, double-blind, placebo-controlled phase 3 study of apalutamide in patients with local high-risk prostate cancer or locally advanced prostate cancer receiving primary radiotherapy (ATLAS) - study AP 90/15 of the AUO. Urologe A. 2017 Feb;56(2):243-244. German. PubMed
Patient drug information
- Apalutamide (Erleada) package insert
- Apalutamide (Erleada) patient drug information (Chemocare)
- Apalutamide (Erleada) patient drug information (UpToDate)
History of changes in FDA indication
- 2/14/2018: FDA approved "for patients with non-metastatic castration-resistant prostate cancer (NM-CRPC)."
Also known as
- Code name: ARN-509
- Brand name: Erleada