Selective, Resistant-Mutant Active
Selectively inhibits FGFR2/3 while sparing FGFR1/4, and retains activity against multiple resistance mutants, with potential for tissue-agnostic solid tumor therapy.
Aliper, Alexander M. · Yan, Feng · Ren, Feng · Ding, Xiao · Zhavoronkov, Alex A.
Journal of Medicinal Chemistry 2025
Potently inhibits FGFR2/3 and selectively spares FGFR1/4
Maintains strong activity against multiple FGFR2/3 mutants known to drive resistance to current drugs
Broad-spectrum antiproliferative potency in cancer cells harboring FGFR2/3 amplification, fusion, and mutation
Robust tumor growth suppression, favorable pharmacokinetic profile, and pharmacodynamic effects