Pipeline – B-raf

About B-raf

Many cancers have been shown to have mutations in the B-raf gene which cause a large increase in the enzyme activity of the B-raf protein kinase. These mutations have been observed in over 60% of malignant melanoma as well as colorectal, thyroid, cholangiocarcinoma, lung adenocarcinoma and glioblastoma. In addition, introduction of these mutant forms of B-raf into experimental models have reproduced and sustained tumourigenesis.

Sareum have inuitiated a discovery programme to produce inhibitors that reduce B-raf enzyme activity. Such small molecular weight inhibitors, in appropriate cancer patients, would be expected to reverse the harmful effects of cellular transformation and even lead to tumour eradication in combination with other existing therapies.