Mechanism of action and clinical activity of tasquinimod in castrate-resistant prostate cancer

Neha Gupta, Omar Al Ustwani, Li Shen, Roberto Pili

Research output: Contribution to journalArticle

14 Citations (Scopus)

Abstract

Castrate-resistant prostate cancer (CRPC) is a disease where survival is poor and treatment is challenging. Over the past 3 years, significant advances in the field have been made with US Food and Drug Administration approval of new drugs for patients with CRPC. However, despite the presence of new approved drugs such as enzalutamide, abiraterone, sipuleucel-T, cabazitaxel, and alpharadin, there is still an unmet need for novel agents with different mechanisms of action to target CRPC. Based on earlier studies demonstrating therapeutic potential of a quinoline-3-carboxamide agent roquinimex as an anticancer drug, efforts were directed to identify other useful members in this class. Tasquinimod is a second-generation quinoline-3-carboxamide agent that is currently in final stages of clinical development as a treatment for CRPC. The preclinical studies of tasquinimod have formed the basis for its success as an antiangiogenic and immunomodulatory agent in this disease. Tasquinimod is an orally available agent that has shown efficacy and favorable safety profile as deduced by the results of Phase I and II clinical trials of this drug in prostate cancer. The place of tasquinimod in the treatment of CRPC patients is currently under examination in an ongoing Phase III clinical trial. In this review, we will discuss tasquinimod, starting from its discovery and current knowledge on potential mechanisms of action to its clinical potential in CRPC.

Original languageEnglish (US)
Pages (from-to)223-234
Number of pages12
JournalOncoTargets and Therapy
Volume7
DOIs
StatePublished - Feb 12 2014
Externally publishedYes

Fingerprint

Prostatic Neoplasms
Pharmaceutical Preparations
Drug Approval
Phase III Clinical Trials
Phase II Clinical Trials
Clinical Trials, Phase I
Angiogenesis Inhibitors
Therapeutics
tasquinimod
Action Potentials
Safety
Survival

Keywords

  • ABR-215050
  • Castration resistant
  • Prostate adenocarcinoma
  • Quinoline-3-carboxamide

ASJC Scopus subject areas

  • Oncology
  • Pharmacology (medical)

Cite this

Mechanism of action and clinical activity of tasquinimod in castrate-resistant prostate cancer. / Gupta, Neha; Ustwani, Omar Al; Shen, Li; Pili, Roberto.

In: OncoTargets and Therapy, Vol. 7, 12.02.2014, p. 223-234.

Research output: Contribution to journalArticle

@article{f570f9969c3e4a2c922949a6554a1902,
title = "Mechanism of action and clinical activity of tasquinimod in castrate-resistant prostate cancer",
abstract = "Castrate-resistant prostate cancer (CRPC) is a disease where survival is poor and treatment is challenging. Over the past 3 years, significant advances in the field have been made with US Food and Drug Administration approval of new drugs for patients with CRPC. However, despite the presence of new approved drugs such as enzalutamide, abiraterone, sipuleucel-T, cabazitaxel, and alpharadin, there is still an unmet need for novel agents with different mechanisms of action to target CRPC. Based on earlier studies demonstrating therapeutic potential of a quinoline-3-carboxamide agent roquinimex as an anticancer drug, efforts were directed to identify other useful members in this class. Tasquinimod is a second-generation quinoline-3-carboxamide agent that is currently in final stages of clinical development as a treatment for CRPC. The preclinical studies of tasquinimod have formed the basis for its success as an antiangiogenic and immunomodulatory agent in this disease. Tasquinimod is an orally available agent that has shown efficacy and favorable safety profile as deduced by the results of Phase I and II clinical trials of this drug in prostate cancer. The place of tasquinimod in the treatment of CRPC patients is currently under examination in an ongoing Phase III clinical trial. In this review, we will discuss tasquinimod, starting from its discovery and current knowledge on potential mechanisms of action to its clinical potential in CRPC.",
keywords = "ABR-215050, Castration resistant, Prostate adenocarcinoma, Quinoline-3-carboxamide",
author = "Neha Gupta and Ustwani, {Omar Al} and Li Shen and Roberto Pili",
year = "2014",
month = "2",
day = "12",
doi = "10.2147/OTT.S53524",
language = "English (US)",
volume = "7",
pages = "223--234",
journal = "OncoTargets and Therapy",
issn = "1178-6930",
publisher = "Dove Medical Press Ltd.",

}

TY - JOUR

T1 - Mechanism of action and clinical activity of tasquinimod in castrate-resistant prostate cancer

AU - Gupta, Neha

AU - Ustwani, Omar Al

AU - Shen, Li

AU - Pili, Roberto

PY - 2014/2/12

Y1 - 2014/2/12

N2 - Castrate-resistant prostate cancer (CRPC) is a disease where survival is poor and treatment is challenging. Over the past 3 years, significant advances in the field have been made with US Food and Drug Administration approval of new drugs for patients with CRPC. However, despite the presence of new approved drugs such as enzalutamide, abiraterone, sipuleucel-T, cabazitaxel, and alpharadin, there is still an unmet need for novel agents with different mechanisms of action to target CRPC. Based on earlier studies demonstrating therapeutic potential of a quinoline-3-carboxamide agent roquinimex as an anticancer drug, efforts were directed to identify other useful members in this class. Tasquinimod is a second-generation quinoline-3-carboxamide agent that is currently in final stages of clinical development as a treatment for CRPC. The preclinical studies of tasquinimod have formed the basis for its success as an antiangiogenic and immunomodulatory agent in this disease. Tasquinimod is an orally available agent that has shown efficacy and favorable safety profile as deduced by the results of Phase I and II clinical trials of this drug in prostate cancer. The place of tasquinimod in the treatment of CRPC patients is currently under examination in an ongoing Phase III clinical trial. In this review, we will discuss tasquinimod, starting from its discovery and current knowledge on potential mechanisms of action to its clinical potential in CRPC.

AB - Castrate-resistant prostate cancer (CRPC) is a disease where survival is poor and treatment is challenging. Over the past 3 years, significant advances in the field have been made with US Food and Drug Administration approval of new drugs for patients with CRPC. However, despite the presence of new approved drugs such as enzalutamide, abiraterone, sipuleucel-T, cabazitaxel, and alpharadin, there is still an unmet need for novel agents with different mechanisms of action to target CRPC. Based on earlier studies demonstrating therapeutic potential of a quinoline-3-carboxamide agent roquinimex as an anticancer drug, efforts were directed to identify other useful members in this class. Tasquinimod is a second-generation quinoline-3-carboxamide agent that is currently in final stages of clinical development as a treatment for CRPC. The preclinical studies of tasquinimod have formed the basis for its success as an antiangiogenic and immunomodulatory agent in this disease. Tasquinimod is an orally available agent that has shown efficacy and favorable safety profile as deduced by the results of Phase I and II clinical trials of this drug in prostate cancer. The place of tasquinimod in the treatment of CRPC patients is currently under examination in an ongoing Phase III clinical trial. In this review, we will discuss tasquinimod, starting from its discovery and current knowledge on potential mechanisms of action to its clinical potential in CRPC.

KW - ABR-215050

KW - Castration resistant

KW - Prostate adenocarcinoma

KW - Quinoline-3-carboxamide

UR - http://www.scopus.com/inward/record.url?scp=84894247854&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84894247854&partnerID=8YFLogxK

U2 - 10.2147/OTT.S53524

DO - 10.2147/OTT.S53524

M3 - Article

AN - SCOPUS:84894247854

VL - 7

SP - 223

EP - 234

JO - OncoTargets and Therapy

JF - OncoTargets and Therapy

SN - 1178-6930

ER -