Enzalutamide: A Novel Antiandrogen for Patients with Castrate-Resistant Prostate Cancer
ABSTRACT Enzalutamide (MDV3100, Xtandi, Medivation\Astellas) is an oral inhibitor of androgen receptor signaling which blocks androgen-receptor interaction; inhibits translocation of the androgen receptor to the nucleus; impairs androgen receptor binding to DNA; and inhibits co-activator recruitment and receptor mediated DNA transcription. In a Phase III randomized study comparing Enzalutamide to placebo in men with progressive castration resistant prostate cancer (CRPC) who were previously treated with docetaxel, Enzalutamide showed an improvement in overall survival (18.4 vs. 13.6 months, hazard ratio 0.63, p<0.001). In addition, all secondary endpoints including proportion of patients with PSA decline; soft tissue response; quality of life response; time to PSA progression; radiographic progression free survival; and the time to the first radiographic skeletal event all significantly favored patients treated with enzalutamide. Fatigue, diarrhea and hot flashes were common in patients treated with enzalutamide, with seizures reported in 5 (0.6%) of the patients. Enzalutamide is a novel therapy which very potently blocks the androgen signaling pathway that is unregulated during the development of CRPC. The preclinical studies along with the pivotal trials which led to its approval by the FDA in September of 2012 will be reviewed.
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ABSTRACT: To develop a nomogram predictive of current bone scan positivity in patients receiving androgen-deprivation therapy (ADT) for advanced prostate cancer; to augment clinical judgment and highlight patients in need of additional imaging investigations.Frontiers in Oncology 10/2014; 4:296. DOI:10.3389/fonc.2014.00296
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ABSTRACT: Radium-223 dichloride (radium-223) is an important therapeutic option for the treatment of patients with castration-resistant prostate cancer, symptomatic bone metastases, and no visceral disease. The unique mechanism of action of this first-in-class alpha-emitting radiopharmaceutical underlies its favorable safety profile and low incidence of myelosuppression. In the pivotal phase 3 ALpharadin in SYMptomatic Prostate CAncer Patients study, radium-223 reduced the risk of death by 30% and prolonged time to first symptomatic skeletal event by 5.8 months. This article summarizes current guidelines and clinical studies that led to the approval of radium-223 as an overall survival therapy, and discusses the urologist's perspective on using radium-223 in clinical practice. Copyright © 2015 Elsevier Inc. All rights reserved.Urology 02/2015; 85(4). DOI:10.1016/j.urology.2014.11.031 · 2.13 Impact Factor
Dataset: AM-I2PP2A and prostate cancer