plixorafenib

Plixorafenib is an investigational, orally available, small-molecule inhibitor of mutated BRAF. It selectively binds to and inhibits dimeric BRAF mutants (including fusions and splice variants) as well as BRAFV600 monomers, while sparing wild-type RAF function in normal cells. This mechanism blocks the proliferation of tumor cells harboring these BRAF alterations by disrupting the MAPK/ERK signaling pathway. Unlike first-generation RAF inhibitors, plixorafenib does not induce paradoxical activation of the pathway (“paradox breaker”), potentially reducing toxicities and resistance seen with earlier drugs. Plixorafenib is being developed primarily for solid tumors with BRAF mutations or fusions—including melanoma, thyroid cancer, central nervous system tumors (such as primary CNS tumors), and other rare cancers—and has reached phase 2 clinical trials[1][3][5][6][8].

Brand names

plixorafenib

Other names

plixorafenib