Targeting FGFR Abnormalities: The Therapeutic Efficacy of TAS-120 in Cancer

3 June 2024
The study explores the impact of TAS-1201, a potent and selective FGFR inhibitor, on various cancer types characterized by FGFR gene anomalies. FGFs and FGFRs are integral to cell processes such as proliferation and differentiation. Abnormalities in FGFR genes are linked to several cancers, prompting the development of TAS-1201 to target all four FGFR subtypes.

In vitro tests on tumor cells with FGFR gene mutations demonstrated TAS-1201's efficacy, as it selectively hindered the growth of affected cancer cells without impacting those without the mutations. The compound also effectively blocked cellular FGFR phosphorylation and downstream signaling pathways.

Further, in vivo experiments using xenograft models showed that TAS-1201 significantly reduced tumor growth in a dose-dependent manner and confirmed the compound's target engagement through the inhibition of FGFR phosphorylation in tumors.

The findings indicate TAS-1201's potential as a therapeutic agent for cancers with FGFR gene abnormalities, as it has exhibited both selective antitumor activity and pharmacodynamic effects in preclinical models.

The research was presented at the 24th EORTC-NCI-AACR Symposium and published in the Molecular Cancer Therapeutics journal, with Hiroaki Ochiiwa and colleagues detailing the inhibitor's effectiveness in abstract A270.

How to Use Synapse Database to Search and Analyze Translational Medicine Data?

The transational medicine section of the Synapse database supports searches based on fields such as drug, target, and indication, covering the T0-T3 stages of translation. Additionally, it offers a historical conference search function as well as filtering options, view modes, translation services, and highlights summaries, providing you with a unique search experience.

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Taking obesity as an example, select "obesity" under the indication category and click search to enter the Translational Medicine results list page. By clicking on the title, you can directly navigate to the original page.

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By clicking the analysis button, you can observe that GLP-1R treatment for obesity has gained significant attention over the past three years, with preclinical research still ongoing in 2023. Additionally, there are emerging potential targets, such as GDF15, among others.

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Click on the image below to go directly to the Translational Medicine search interface.

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