Abstract

Importance of the field: The endothelin (ET) axis, which includes the biologicalfunctions of ETs and their receptors, has played a physiological role innormal tissue, acting as a modulator of vasomotor tone, tissue differentiationand development, cell proliferation and hormone production. Interestingly, italso functions in the growth and progression of various tumors. Severalresearchers have identified the blockade of the ET-1 receptor as a promisingtherapeutic approach.Areas covered in this review: The clinical investigation of an orally bioavailableET antagonist, atrasentan, in prostate cancer, is encouraging. In thisneoplasia, it has shown antitumor activity, bone metastasis control andamelioration of cancer-related pain but improvement in time to progressionand overall survival has still not been demonstrated. The clinical trials of otherET antagonists are reported. Literature research was performed by Pubmedand Pharmaprojects.What the reader will gain: A comprehensive view about the use of atrasentanin the treatment of castration-resistant prostate cancer (CRPC) is providedtogether with the scientific rationale based on the function of ET and itsreceptor in various cancer development mechanisms.Take home message: Atrasentan seems to be active in CRPC, althoughstrong scientific evidence is still to be found. Interesting clinical findingsregard zibotentan.
Lingua originaleEnglish
pagine (da-a)27-40
Numero di pagine14
RivistaDefault journal
Volume15
Stato di pubblicazionePublished - 2010

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Endothelins
Prostatic Neoplasms
Castration
Pharmaceutical Preparations
Endothelin A Receptors
Neoplasms
Cell Proliferation
Clinical Trials
Hormones
Neoplasm Metastasis
Bone and Bones
Growth
Research
atrasentan
Therapeutics

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Pharmacology (medical)

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@article{3687ea0a94a84c91903768c08309dc5b,
title = "Anti-endothelin drugs in solid tumors",
abstract = "Importance of the field: The endothelin (ET) axis, which includes the biologicalfunctions of ETs and their receptors, has played a physiological role innormal tissue, acting as a modulator of vasomotor tone, tissue differentiationand development, cell proliferation and hormone production. Interestingly, italso functions in the growth and progression of various tumors. Severalresearchers have identified the blockade of the ET-1 receptor as a promisingtherapeutic approach.Areas covered in this review: The clinical investigation of an orally bioavailableET antagonist, atrasentan, in prostate cancer, is encouraging. In thisneoplasia, it has shown antitumor activity, bone metastasis control andamelioration of cancer-related pain but improvement in time to progressionand overall survival has still not been demonstrated. The clinical trials of otherET antagonists are reported. Literature research was performed by Pubmedand Pharmaprojects.What the reader will gain: A comprehensive view about the use of atrasentanin the treatment of castration-resistant prostate cancer (CRPC) is providedtogether with the scientific rationale based on the function of ET and itsreceptor in various cancer development mechanisms.Take home message: Atrasentan seems to be active in CRPC, althoughstrong scientific evidence is still to be found. Interesting clinical findingsregard zibotentan.",
author = "Antonio Russo and Viviana Bazan and Daniele Fanale and Nicolo' Gebbia and Giuseppe Bronte and {Di Gaudio}, Francesca and Sergio Rizzo",
year = "2010",
language = "English",
volume = "15",
pages = "27--40",
journal = "Default journal",

}

TY - JOUR

T1 - Anti-endothelin drugs in solid tumors

AU - Russo, Antonio

AU - Bazan, Viviana

AU - Fanale, Daniele

AU - Gebbia, Nicolo'

AU - Bronte, Giuseppe

AU - Di Gaudio, Francesca

AU - Rizzo, Sergio

PY - 2010

Y1 - 2010

N2 - Importance of the field: The endothelin (ET) axis, which includes the biologicalfunctions of ETs and their receptors, has played a physiological role innormal tissue, acting as a modulator of vasomotor tone, tissue differentiationand development, cell proliferation and hormone production. Interestingly, italso functions in the growth and progression of various tumors. Severalresearchers have identified the blockade of the ET-1 receptor as a promisingtherapeutic approach.Areas covered in this review: The clinical investigation of an orally bioavailableET antagonist, atrasentan, in prostate cancer, is encouraging. In thisneoplasia, it has shown antitumor activity, bone metastasis control andamelioration of cancer-related pain but improvement in time to progressionand overall survival has still not been demonstrated. The clinical trials of otherET antagonists are reported. Literature research was performed by Pubmedand Pharmaprojects.What the reader will gain: A comprehensive view about the use of atrasentanin the treatment of castration-resistant prostate cancer (CRPC) is providedtogether with the scientific rationale based on the function of ET and itsreceptor in various cancer development mechanisms.Take home message: Atrasentan seems to be active in CRPC, althoughstrong scientific evidence is still to be found. Interesting clinical findingsregard zibotentan.

AB - Importance of the field: The endothelin (ET) axis, which includes the biologicalfunctions of ETs and their receptors, has played a physiological role innormal tissue, acting as a modulator of vasomotor tone, tissue differentiationand development, cell proliferation and hormone production. Interestingly, italso functions in the growth and progression of various tumors. Severalresearchers have identified the blockade of the ET-1 receptor as a promisingtherapeutic approach.Areas covered in this review: The clinical investigation of an orally bioavailableET antagonist, atrasentan, in prostate cancer, is encouraging. In thisneoplasia, it has shown antitumor activity, bone metastasis control andamelioration of cancer-related pain but improvement in time to progressionand overall survival has still not been demonstrated. The clinical trials of otherET antagonists are reported. Literature research was performed by Pubmedand Pharmaprojects.What the reader will gain: A comprehensive view about the use of atrasentanin the treatment of castration-resistant prostate cancer (CRPC) is providedtogether with the scientific rationale based on the function of ET and itsreceptor in various cancer development mechanisms.Take home message: Atrasentan seems to be active in CRPC, althoughstrong scientific evidence is still to be found. Interesting clinical findingsregard zibotentan.

UR - http://hdl.handle.net/10447/58939

M3 - Article

VL - 15

SP - 27

EP - 40

JO - Default journal

JF - Default journal

ER -