H3B-6527

H3B‑6527 is an orally bioavailable, highly selective covalent inhibitor of human fibroblast growth factor receptor 4 (FGFR4), developed as a small molecule with potential antineoplastic activity. It specifically binds to and blocks FGFR4, preventing its activation and downstream signaling. This inhibition leads to reduced cell proliferation and induces apoptosis in tumor cells that overexpress FGFR4—particularly relevant in hepatocellular carcinoma (HCC), where FGF19-driven activation of FGFR4 is implicated in tumorigenesis. Preclinical studies demonstrated robust anti-tumor effects in HCC models with high FGF19 expression. Clinical trials have shown that H3B‑6527 is well tolerated and exhibits encouraging clinical activity in heavily pretreated patients with advanced HCC[1][5][7].

Other names

N-[2-[[6-[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl-methylamino]pyrimidin-4-yl]amino]-5-(4-ethylpiperazin-1-yl)phenyl]prop-2-enamideN-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin‑4‑yl)amino)-5-(4‑ethylpiperazin‑1‑yl)phenyl)acrylamide