Apalutamide: the established and emerging roles in the treatment of advanced prostate cancer. (3rd June 2018)

• Record Type: Journal Article
• Authors: Dellis, Athanasios E.; Papatsoris, Athanasios G.
• Is Part Of: Expert opinion on investigational drugs. Volume 27:Number 6(2018)
• Page Start: 553
• Page End: 559
• Publication Date: 2018-06-03
• Subjects: Apalutamide -- ARN-509 -- anti-androgen -- androgen receptor -- antagonist -- prostate cancer -- drug evaluation; Drugs -- Design -- Periodicals; Drugs, Investigational -- Bibliography; Drugs, Investigational -- Periodicals; 615.1
• DOI: 10.1080/13543784.2018.1484107
• Languages: English
• ISSNs: 1354-3784

Abstract

ABSTRACT: Introduction : Prostate cancer (PCa) is the most common cancer in elderly males. Androgen deprivation therapy (ADT) is still the cornerstone of initial treatment; however, the vast majority of patients develop castration-resistant prostate cancer (CRPC). Several studies with numerous androgen receptor (AR)-directed agents have emerged since the approval of abiraterone acetate and enzalutamide. One of these agents is apalutamide, which seems to be a promising AR antagonist for the treatment of CRPC. Areas covered : The authors review Phase I, II, and III studies for apalutamide, in a large spectrum of PCa (from low-risk to metastatic CRPC [mCRPC]) patients as sole treatment or in the setting of combined therapy. Expert opinion : Apalutamide is an oral, investigational, AR antagonist that targets the AR ligand-binding domain and prevents AR nuclear translocation, DNA binding, and transcription of AR gene targets. It has shown favorable safety profile and therapeutic index in Phase I studies, good tolerance and efficacy in patients with high-risk CRPC in Phase II studies. Also, results were promising in a recent phase III study in patients with non-mCRPC who were at high risk for the development of metastasis. These data may offer potential advantages over the second-generation antiandrogens.