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A Bioluminescent and Fluorescent Orthotopic Syngeneic Murine Model of Androgen-dependent and Castration-resistant Prostate Cancer
07:25

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Published on: March 6, 2018

Endothelin receptor antagonists: rationale, clinical development, and role in prostate cancer therapeutics

Snehal G Thakkar1, Toni K Choueiri, Jorge A Garcia

  • 1Department of Hematology and Medical Oncology, Taussig Cancer Center, The Cleveland Clinic Foundation, 9500 Euclid Avenue, R-35, Cleveland, OH 44195, USA. choueit@ccf.org

Current Oncology Reports
|March 2, 2006
PubMed

Insights

Atrasentan, an endothelin receptor antagonist, shows promise in inhibiting tumor growth and metastasis. Clinical trials suggest it may be a new therapeutic strategy for prostate cancer and other solid tumors.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Endothelins (ETs) and their receptors (ET-A, ET-B) are implicated in tumor progression, including growth, proliferation, apoptosis, angiogenesis, and bone metastasis.
  • Targeting the endothelin pathway presents a potential therapeutic strategy for various cancers.

Purpose of the Study:

  • To evaluate the efficacy of atrasentan, a selective endothelin-1 and ET-A receptor inhibitor, in preclinical and clinical settings.
  • To explore atrasentan as a novel therapeutic agent for solid malignancies, particularly prostate cancer.

Main Methods:

  • In vitro and in vivo studies assessing the anti-tumor effects of atrasentan.
  • Phase I, II, and III clinical trials involving patients with refractory carcinoma and hormone-refractory prostate carcinoma.

Main Results:

  • Atrasentan demonstrated in vitro inhibition of tumor cells.
  • Clinical trials indicated potential therapeutic benefits in patients with advanced cancers.

Conclusions:

  • Atrasentan exhibits anti-tumor activity and warrants further investigation.
  • Targeting the endothelin pathway with atrasentan represents a promising therapeutic strategy for prostate cancer and other solid tumors.

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