Androgen receptor antagonist prostate cancer therapy

L. Gao, J. Alumkal

Research output: Contribution to journalReview articlepeer-review

2 Scopus citations


Prostate cancer is the most common cancer in men in the U.S. and the second most lethal. Nearly all prostate cancer deaths occur due to castration-resistant prostate cancer (CRPC) that has progressed despite androgen deprivation therapy (ADT). These therapies are designed to lower levels of androgens that can activate the androgen receptor (AR), the central protein in prostate cancer. We now know that androgens and androgen-dependent signaling pathways modulated by AR persist in CRPC cells despite ADT. However, until recently, effective agents to antagonize these persistent androgens and to disrupt AR signaling in CRPC cells were not available. MDV-3100 is a new antiandrogen that effectively inhibits androgen binding to and activation of AR in preclinical studies in CRPC cells. A phase I/II clinical trial with MDV-3100 in CRPC patients also showed encouraging results, which led to the initiation of two ongoing phase III clinical trials. In this review, we will focus on its preclinical development and summarize the clinical results to date.

Original languageEnglish (US)
Pages (from-to)371-376
Number of pages6
JournalDrugs of the Future
Issue number5
StatePublished - May 2011

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)


Dive into the research topics of 'Androgen receptor antagonist prostate cancer therapy'. Together they form a unique fingerprint.

Cite this