pexidartinib + vemurafenib

**Pexidartinib + vemurafenib** is an investigational combination regimen utilizing two targeted small molecule inhibitors: pexidartinib, a colony-stimulating factor 1 receptor (CSF-1R) inhibitor, and vemurafenib, a BRAF inhibitor. Pexidartinib selectively inhibits CSF-1R as well as kinases such as KIT and FLT3, leading to suppression of tumor-associated macrophage recruitment and survival. Vemurafenib specifically inhibits the activity of BRAF with the V600E mutation, blocking the MAPK pathway in tumors such as melanoma. This combination has been studied in early-phase clinical trials for advanced solid tumors, particularly melanoma, but is not an approved fixed-dose combination. Most experience with both drugs comes from their individual use. The rationale for combining these agents is to simultaneously target tumor cells harboring BRAF mutations and modulate the tumor microenvironment through macrophage inhibition. There is a noted risk for hepatotoxicity with this regimen, requiring careful monitoring.

Other names

pexidartinib and vemurafenib combination