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The role of α1-adrenoceptor antagonists in the treatment of prostate and other cancers
International Journal of Molecular Sciences
  • Mallory Batty, Griffith University
  • Rachel Pugh, Griffith University
  • Ilampirai Rathinam, Griffith University
  • Joshua Simmonds, Griffith University
  • Edwin Walker, Griffith University
  • Amanda Forbes, Bond University
  • Shailendra Anoopkumar-Dukie, Griffith University
  • Catherine M McDermott, Bond University
  • Briohny Spencer, Griffith University
  • David Christie, Bond University
  • Russ Chess-Williams, Bond University
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Journal Article
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Batty, M., Pugh, R., Rathinam, I., Simmonds, J., Walker, E., Forbes, A., Anoopkumar-Dukie, S., McDermott, C. M., Spencer, B., Christie, D., & Chess-Williams, R. (2016). The role of α1-adrenoceptor antagonists in the treatment of prostate and other cancers. International Journal of Molecular Sciences, 17(8), 1-25.

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Copyright © 2016 by the authors. licensee MDPI, Basel, Switzerland.

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This review evaluates the role of α-adrenoceptor antagonists as a potential treatment of prostate cancer (PCa). Cochrane, Google Scholar and Pubmed were accessed to retrieve sixty-two articles for analysis. In vitro studies demonstrate that doxazosin, prazosin and terazosin (quinazoline α-antagonists) induce apoptosis, decrease cell growth, and proliferation in PC-3, LNCaP and DU-145 cell lines. Similarly, the piperazine based naftopidil induced cell cycle arrest and death in LNCaP-E9 cell lines. In contrast, sulphonamide based tamsulosin did not exhibit these effects. In vivo data was consistent with in vitro findings as the quinazoline based α-antagonists prevented angiogenesis and decreased tumour mass in mice models of PCa. Mechanistically the cytotoxic and antitumor effects of the α-antagonists appear largely independent of α 1-blockade. The proposed targets include: VEGF, EGFR, HER2/Neu, caspase 8/3, topoisomerase 1 and other mitochondrial apoptotic inducing factors. These cytotoxic effects could not be evaluated in human studies as prospective trial data is lacking. However, retrospective studies show a decreased incidence of PCa in males exposed to α-antagonists. As human data evaluating the use of α-antagonists as treatments are lacking; well designed, prospective clinical trials are needed to conclusively demonstrate the anticancer properties of quinazoline based α-antagonists in PCa and other cancers.

Citation Information
Mallory Batty, Rachel Pugh, Ilampirai Rathinam, Joshua Simmonds, et al.. "The role of α1-adrenoceptor antagonists in the treatment of prostate and other cancers" International Journal of Molecular Sciences Vol. 17 Iss. 8 (2016) p. 1 - 25 ISSN: 1422-0067
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