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

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.