Lifirafenib (BGB-283) is an investigational novel small molecule inhibitor of the RAF protein. As opposed to other agents which inhibit RAF in its monomeric form, lifirafenib was designed to inhibit both monomeric and dimeric RAF inhibition activities. Lifirafenib has demonstrated antitumor activity in preclinical models and in cancer patients with tumors harboring BRAF V600E mutations and non-V600E BRAF mutations, in which the monomeric form of RAF is implicated, as well as KRAS/NRAS mutations, in which the dimeric form of RAF is implicated. 

Lifirafenib Clinical Trials 

We are studying lifirafenib in Phase 1 trials for the treatment of cancers with aberrations in the mitogen-activated protein kinase (MAPK) pathway, including BRAF gene mutations and KRAS/NRAS gene mutations where first generation BRAF inhibitors are not effective. 

For more clinical trial information please visit CLINICALTRIALS.GOV.

The MAPK Pathway 

The mitogen-activated protein kinase (MAPK) pathway consists of proteins in the cell that transmit a signal from a receptor on the surface of the cell to the DNA in the nucleus of the cell. This pathway plays an essential role in regulating cell proliferation and survival. We believe that lifirafenib as monotherapy or in combination with other agents may have a potential for treating various malignancies, such as melanoma, non-small cell lung cancer, and endometrial cancer.