Lirafugratinib

DB18300ApprovedInvestigationalSmall molecule

Lirafugratinib is an oral kinase inhibitor of FGFR2 indicated for adults with previously treated, unresectable, locally advanced or metastatic cholangiocarcinoma harboring an FGFR2 fusion or other rearrangement. Lirafugratinib is an oral small molecule kinase inhibitor that inhibits and covalently binds fibroblast growth factor receptor 2 (FGFR2).

Mechanism: Lirafugratinib is a small molecule kinase inhibitor that inhibits FGFR2 and covalently binds FGFR2. Constitutive FGFR signaling can support the proliferation and survival of malignant cells. Lirafugratinib inhibited FGFR2 phosphorylation and downstream signaling and decreased cell viability in cancer cell lines with FGFR2 alterations, including FGFR fusions/rearrangements, amplifications, and mutations. It showed anti-tumor activity in human cell line-derived and patient-derived xenograft mouse models of various tumors with FGFR2 genetic alterations.
Curator reviewed · 4 references
Primary indication: Lirafugratinib is indicated for the treatment of adults with previously treated, unresectable, locally advanced or metastatic cholangiocarcinoma harboring a fibroblast growth factor receptor 2 (FGFR2) fusion or other rearrangement.Curator reviewed · 2 structured indications
Formula / weight: C₂₈H₂₄FN₇O₂ · 509.545 g/mol (avg)
Also known as: 2-Propenamide, N-[4-[4-amino-5-[3-fluoro-4-[(4-methyl-2-pyrimidinyl)oxy]phenyl]-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenyl]-2-methyl- · N-(4-(4-amino-5-(3-fluoro-4-((4-methylpyrimidin-2-yl)oxy)phenyl)-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl)phenyl)methacrylamide · N-[4-(4-amino-5-{3-fluoro-4-[(4-methylpyrimidin-2- yl)oxy]phenyl}-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-6- yl)phenyl]-2-methylprop-2-enamide
Code names: RLY-4008