NCIt definition : An orally available v-raf murine sarcoma viral oncogene homolog B1 (B-raf) serine/threonine
protein kinase inhibitor with potential antineoplastic activity. Agerafenib specifically
and selectively inhibits the activity of the mutated form (V600E) of B-raf kinase.
This inhibits the activation of the RAF/mitogen-activated protein kinase kinase (MEK)/extracellular
signal-related kinase (ERK) signaling pathway and may result in a decrease in the
proliferation of tumor cells expressing the mutated B-raf gene. The Raf mutation BRAF
V600E, in which valine is substituted for glutamic acid at residue 600, is frequently
found in a variety of human tumors and results in the constitutive activation of the
RAF/MEK/ERK signaling pathway that regulates cellular proliferation and survival.;