In patients with stage IV melanoma with distant metastases, what is the response rate to an oral inhibitor of the protein kinase BRAF?
Explore this issue:April 2011
Background: There are few effective therapies for patients with stage IV metastatic melanoma. Response rates to standard therapy (interleukin-2 or dacarbazine) are 10 to 20 percent, and complete responses are exceedingly rare. The activating V600E mutation in the BRAF gene is found in 40 to 60 percent of melanomas. The oral agent PLX4032 is a potent inhibitor of mutated BRAF signaling.
Study design: Phase I dose-escalation trial followed by extension phase. The dose-escalation phase included 55 patients. The recommended phase II dose was then administered to 32 patients with metastatic melanoma testing positive for the V600E mutation in the BRAF gene.