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apalutamide (Erleada)
Indications:
- non-metastatic, castration-resistant prostate cancer [1,2]
- metastatic, castration-sensitive prostate cancer [3]
Adverse effects:
- generally well tolerated
- 11% discontinuation due to adverse events [1]
- rash (23.8% vs 5.5%)*
- hypothyroidism (8.1% vs 2.0%)
- bone fracture (11.7% vs 6.5%)
* vs placebo
Mechanism of action:
- androgen receptor antagonist (competitive inhibitor)
- blocks androgen binding to receptor
- blocks androgen receptor translocation to the nucleus
- blocks androgen receptor-mediated DNA transcription
- delays time to metastatic progression of prostate cancer [1]
General
androgen receptor antagonist; androgen receptor signaling inhibitor (ARSI)
antineoplastic agent (chemotherapeutic agent)
Database Correlations
PUBCHEM cid=24872560
References
- Bankhead C
Apalutamide Slows Metastasis in Prostate Cancer -
Two-year delay in metastatic progression with apalutamide.
MedPage Today. Feb 05, 2018
https://www.medpagetoday.com/meetingcoverage/mgucs/70966
- Small EJ, et al
SPARTAN, a phase III double-blind randomized study of
apalutamide vs placebo in patients with nonmetastatic
castration-resistant prostate cancer
Genitourinary Cancers Symposium (GUCS); Abstract 161.
- Smith MR, Saad F, Chowdhury S et al
Apalutamide Treatment and Metastasis-free Survival in Prostate
Cancer.
N Engl J Med. Feb 8, 2018
PMID: 29420164
http://www.nejm.org/doi/full/10.1056/NEJMoa1715546
- FDA News Release. Feb 14, 2018
FDA approves new treatment for a certain type of prostate
cancer using novel clinical trial endpoint.
https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm596768.htm
- Chi KN, Agarwal N, Bjartell A
Apalutamide for Metastatic, Castration-Sensitive Prostate Cancer.
N Engl J Med 2019; 381:13-24. July 4, 2019
PMID: 31150574
https://www.nejm.org/doi/full/10.1056/NEJMoa1903307