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

Authors Gupta N, Al Ustwani O, Shen L, Pili R

Received 25 August 2013

Accepted for publication 20 November 2013

Published 12 February 2014 Volume 2014:7 Pages 223—234

DOI https://doi.org/10.2147/OTT.S53524

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 3


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

Department of Medicine, Roswell Park Cancer Institute, Buffalo, NY, USA

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, quinoline-3-carboxamide, prostate adenocarcinoma, castration resistant

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