Structure-Based Design and Optimization of Novel, Potent and Selective Covalent FGFR2/3 Inhibitors with a Tricyclic Core

Key Points

This research aims to design and optimize novel covalent inhibitors targeting FGFR2 and FGFR3.
Designed inhibitors with a tricyclic core based on structural biology principles.
Tested compounds for oral bioavailability and efficacy in an SNU-16 gastric cancer xenograft model.
Evaluated pharmacokinetics in rats to measure absorption and tumor response.
Inhibitors showed oral bioavailability of 56% in rats.
Achieved significant tumor growth inhibition in the SNU-16 model, with notable efficacy.

Study demonstrated tumor growth inhibition in gastric cancer using novel FGFR2/3 inhibitors, indicating therapeutic potential.

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Lu et al. (2026) studied this question.

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