Difference between revisions of "Apalutamide (Erleada)"

Revision as of 15:48, 16 September 2018

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

Prostate cancer

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

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

References

[insert-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)

[1]

[2]

[3]

[4]

[5]

@@ Line 1: / Line 1: @@
-==Mechanism of action==
+==General information==
-Competitive androgen receptor (AR) inhibitor
+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.<ref name="insert">[http://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/ERLEADA-pi.pdf Apalutamide (Erleada) package insert]</ref><ref>[[Media:Apalutamide.pdf | Apalutamide (Erleada) package insert (locally hosted backup)]]</ref><ref>[https://www.erleadahcp.com Erleada manufacturer's website]</ref>
+<br>Route: PO
+<br>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 [http://www.thomsonhc.com/home/dispatch Micromedex], [http://online.lexi.com/ Lexicomp], [http://www.utdol.com/online/content/search.do UpToDate (courtesy of Lexicomp)], or the prescribing information.<ref name="insert"></ref>
 ==Diseases for which it is used==
@@ Line 6: / Line 11: @@
 # 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. [https://www.ncbi.nlm.nih.gov/pubmed/28213364 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. [https://www.ncbi.nlm.nih.gov/pubmed/28144693 PubMed]
+==Patient drug information==
+*[http://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/ERLEADA-pi.pdf Apalutamide (Erleada) package insert]<ref name="insert"></ref>
+*[https://chemocare.com/chemotherapy/drug-info/apalutamide.aspx Apalutamide (Erleada) patient drug information (Chemocare)]<ref>[https://chemocare.com/chemotherapy/drug-info/apalutamide.aspx Apalutamide (Erleada) patient drug information (Chemocare)]</ref>
+*[http://www.uptodate.com/contents/apalutamide-patient-drug-information Apalutamide (Erleada) patient drug information (UpToDate)]<ref>[http://www.uptodate.com/contents/apalutamide-patient-drug-information Apalutamide (Erleada) patient drug information (UpToDate)]</ref>
 ==History of changes in FDA indication==
-*2/14/2018: FDA approved "for patients with [[prostate cancer|non-metastatic castration-resistant prostate cancer (NM-CRPC)]]."
+*2/14/2018: [https://www.fda.gov/newsevents/newsroom/pressannouncements/ucm596768.htm FDA approved] "for patients with [[prostate cancer|non-metastatic castration-resistant prostate cancer (NM-CRPC)]]."
 ==Also known as==
 *'''Code name:''' ARN-509
 *'''Brand name:''' Erleada
+==References==
+<references/>
 [[Category:Drugs]]