Article
Mechanisms of clinical resistance to selective FGFR2 inhibition by lirafugratinib.
Annals of oncology : official journal of the European Society for Medical Oncology - 1 Jun 2026
Ellis H, Balasooriya E R, Varkaris A, Hajian B, Wan J, Shekhar M, Gritti I, Vijay V, Albertelli L, Piot S, Lau K, Kehlmann A, Chevalier N, Nugent F W, Zhen Y, Silveira V S, Sellers W R, Corcoran R B, Juric D, Bardeesy N
Abstract excerpt
BACKGROUND: Pan-fibroblast growth factor receptor (FGFR) inhibitors, targeting FGFR1-3 or FGFR1-4, are Food and Drug Administration-approved for FGFR2-driven cholangiocarcinoma. However, acquired resistance and dose-limiting toxicities from systemic FGFR inhibition constrain efficacy. Lirafugratinib (RLY-4008), a first-in-class FGFR2-selective inhibitor with activity against resistance-associated FGFR2 kinase...
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