apalutamide (Erleada)
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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]
More general terms
References
- ↑ 1.0 1.1 1.2 1.3 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 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/29420164 <Internet> http://www.nejm.org/doi/full/10.1056/NEJMoa1715546 - ↑ 2.0 2.1 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
- ↑ 3.0 3.1 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: https://www.ncbi.nlm.nih.gov/pubmed/31150574 https://www.nejm.org/doi/full/10.1056/NEJMoa1903307