Description
PLX4720 is an orally available ATP-competitive kinase inhibitor specific for mutant (V600E) B-Raf, which is present in a variety of cancer subtypes. PLX4720 is an analog of vemurafenib. This compound is being examined as a treatment for unresectable or metastatic melanomas. Inhibition of B-Raf by PLX4720 induces apoptosis and autophagy in tumor cells, resulting in decreased tumor growth and increased survival in vitro and in vivo. Additional downstream effects of B-Raf inhibition by PLX4720 include downregulation of expression of angiogenic factors, enhancement of surface expression of tumor-associated antigens on tumor cells, and alterations of trafficking of local immune cells such as CD8+ T lymphocytes.