NVP BGJ398 phosphate

China [CN]

1. Core Uses

Clinical Research: Used in targeted therapy research for advanced cholangiocarcinoma (FDA-approved), bladder cancer, gastric cancer, liver cancer, and other solid tumors with FGFR2/3 fusion/mutation.

Mechanism: Inhibits FGFR kinase activity, blocking downstream RAS/MAPK and PI3K/AKT signaling pathways, thereby inhibiting tumor cell proliferation, angiogenesis, and metastasis.

R&D Applications: Used as an FGFR target tool compound for cell experiments, animal models, drug screening, and mechanism studies.

2. Key Clinical Information

Approved Indication: Previously treated, unresectable locally advanced or metastatic cholangiocarcinoma (with FGFR2 fusion/rearrangement).

Dosage Form: Oral capsule (phosphate form, higher bioavailability).

Core Advantages: High selectivity (selectivity for FGFR1/2/3 > 40 times that of FGFR4 and VEGFR2), and still potently inhibits FGFR3 mutants (such as K650E).