tagarafdeg

Tagarafdeg (CFT1946) is an orally bioavailable, small-molecule targeted protein degrader (TPD) designed to selectively target and degrade BRAF V600 mutant proteins. Developed by C4 Therapeutics using its proprietary TORPEDO platform, tagarafdeg functions by recruiting an E3 ubiquitin ligase to the mutant BRAF protein, leading to its ubiquitination and subsequent degradation by the proteasome. This approach is intended to overcome the limitations of traditional BRAF inhibitors, such as the development of resistance through pathway reactivation or paradoxical activation of the MAPK pathway. Tagarafdeg is currently being investigated in Phase 1/2 clinical trials for the treatment of BRAF V600-mutant solid tumors, including melanoma, colorectal cancer, and non-small cell lung cancer, both as a monotherapy and in combination with other targeted therapies like cetuximab or trametinib.

Other names

Tagarafdeg