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Anti-endothelin drugs in solid tumors

Antonio Russo1, Giuseppe Bronte, Sergio Rizzo

  • 1Università di Palermo, Section of Medical Oncology, Department of Surgical and Oncological Sciences, Via del Vespro 129, 90127 Palermo, Italy. lab-oncobiologia@usa.net

Expert Opinion on Emerging Drugs
|January 28, 2010
PubMed
Abstract

Insights

Endothelin receptor blockade, including with atrasentan, shows promise for castration-resistant prostate cancer (CRPC). While active, further evidence is needed to confirm its efficacy in improving survival for CRPC patients.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • The endothelin (ET) axis regulates normal tissue functions and is implicated in tumor growth and progression.
  • ET-1 receptor blockade is a potential therapeutic strategy for various cancers.
  • The ET axis plays a role in cancer development mechanisms.

Purpose of the Study:

  • To provide a comprehensive view of atrasentan for castration-resistant prostate cancer (CRPC) treatment.
  • To present the scientific rationale for ET receptor blockade in cancer.
  • To review clinical trials of ET antagonists.

Main Methods:

  • Literature research using PubMed and Pharmaprojects.
  • Review of clinical investigations of atrasentan in prostate cancer.
  • Analysis of ET antagonist clinical trials.

Main Results:

  • Atrasentan demonstrates antitumor activity, bone metastasis control, and pain amelioration in CRPC.
  • Improvement in time to progression and overall survival with atrasentan is yet to be demonstrated.
  • Clinical findings regarding zibotentan are also noted.

Conclusions:

  • Atrasentan appears active in CRPC, but robust scientific evidence is still required.
  • The ET axis is a relevant target for CRPC therapy.
  • Further research is warranted to establish the role of ET antagonists in CRPC.

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