Elevate Therapeutics, HLB Subsidiary, Presents Lerapugratinib Kinome Analysis Results at AACR

Elevate Therapeutics, a subsidiary of HLB, announced on the 19th (local time) the results of a 'Kinome analysis' conducted on four FGFR inhibitors, including Lerapugratinib. Kinome analysis refers to a comprehensive assessment of changes in the activity of kinases, which regulate cellular signal transduction, to evaluate the range of action and selectivity of a drug.

On the 19th (local time) at the American Association for Cancer Research (AACR 2026) in San Diego, USA, a representative from Elevate Therapeutics introduced a Kinome analysis poster of the FGFR2-targeted anticancer drug, Lirafugratinib. HLB

Lerapugratinib demonstrated high selectivity for FGFR2 through an analysis of a panel of 468 kinases. It also exhibited characteristics that may reduce off-target and isotype-related toxicity compared to other pan-FGFR inhibitors.

In particular, Lerapugratinib strongly inhibited FGFR2 while showing relatively low inhibition of FGFR1, FGFR3, and FGFR4, suggesting the potential to reduce adverse events such as hyperphosphatemia and diarrhea, which are common issues with pan-FGFR inhibitors. Elevate Therapeutics expects that this selectivity could become a differentiating factor for the drug in future clinical applications.

In contrast, the comparator drug, Futibatinib, inhibited FGFR1 through FGFR4 by more than 90%. Pemigatinib, Erdafitinib, and AZD4547 also showed patterns of broadly inhibiting multiple kinases.

Lerapugratinib is a targeted anticancer drug in development for patients with FGFR2 fusion or rearrangement. This analysis is interpreted as data supporting the drug's competitiveness in terms of selectivity and safety.

The additional analysis results, which demonstrated high selectivity for FGFR2, are expected to serve as a positive factor in the ongoing FDA approval review process for the cholangiocarcinoma indication, and to help secure competitiveness during commercialization in the future. Lerapugratinib has been designated for priority review, and a decision on approval is expected by September.

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