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

Abstract:

:The endothelins (ETs), which include ET-1, ET-2, ET-3, and their receptors ET-A and ET-B, play a major role in tumor growth, proliferation, apoptosis, angiogenesis, and bone metastasis. Atrasentan is a novel and selective inhibitor of ET-1 and ET-A. In vitro and in vivo data show that this oral agent is capable of inhibiting tumor cells in vitro. More recently, this agent was studied in several phase I trials with refractory carcinoma patients. Subsequently, phase II and III clinical trials evaluating atrasentan in patients with hormone-refractory prostate carcinoma have suggested that targeting this pathway may be a new therapeutic strategy in the treatment of solid malignancies, specifically, prostate cancer.

journal_name

Curr Oncol Rep

journal_title

Current oncology reports

authors

Thakkar SG,Choueiri TK,Garcia JA

doi

10.1007/s11912-006-0045-1

keywords:

subject

Has Abstract

pub_date

2006-03-01 00:00:00

pages

108-13

issue

2

eissn

1523-3790

issn

1534-6269

journal_volume

8

pub_type

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