Enzalutamide: A novel antiandrogen for patients with castrate-resistant prostate cancer

Jean Hoffman-Censits, Wm Kevin Kelly

Research output: Contribution to journalReview article

Abstract

Enzalutamide (MDV3100, Xtandi, Medivation\Astellas) is an oral inhibitor of androgen receptor signaling that blocks androgen receptor interaction, inhibits translocation of the androgen receptor to the nucleus, impairs androgen receptor binding to DNA, and inhibits coactivator recruitment and receptor-mediated DNA transcription. In a phase III randomized study comparing enzalutamide with placebo inmen 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, HR, 0.63; P < 0.001). In addition, all secondary endpoints including proportion of patients with prostate-specific antigen (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 that very potently blocks the androgen signaling pathway, which is unregulated during the development of CRPC. The preclinical studies along with the pivotal trials that led to its approval by the U.S. Food and Drug Administration (FDA) in September 2012 will be reviewed.

Original languageEnglish (US)
Pages (from-to)1335-1339
Number of pages5
JournalClinical Cancer Research
Volume19
Issue number6
DOIs
StatePublished - Mar 15 2013
Externally publishedYes

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Androgen Antagonists
Prostatic Neoplasms
Androgen Receptors
Castration
docetaxel
Prostate-Specific Antigen
Hot Flashes
United States Food and Drug Administration
MDV 3100
Androgens
Reaction Time
Disease-Free Survival
Fatigue
Diarrhea
Seizures
Placebos
Quality of Life
Survival
DNA

ASJC Scopus subject areas

  • Oncology
  • Cancer Research

Cite this

Enzalutamide : A novel antiandrogen for patients with castrate-resistant prostate cancer. / Hoffman-Censits, Jean; Kelly, Wm Kevin.

In: Clinical Cancer Research, Vol. 19, No. 6, 15.03.2013, p. 1335-1339.

Research output: Contribution to journalReview article

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