LUT014

LUT014 is a topically bioavailable small molecule inhibitor of serine/threonine-protein kinase B-Raf (BRAF), developed as a gel formulation for the treatment of dermatologic toxicities associated with cancer therapies. Its primary mechanism involves paradoxical activation of the mitogen‑activated protein kinase (MAPK) pathway in healthy keratinocytes by inhibiting BRAF, which counteracts the skin toxicity (notably acneiform rash) induced by epidermal growth factor receptor (EGFR) inhibitors such as cetuximab and panitumumab. This effect leads to proliferation and migration of healthy skin cells, improving rash symptoms and patient quality of life during EGFR-targeted therapy. Clinical trials have also explored its use in radiation-induced dermatitis among breast cancer patients[1][2][4][5][6][8].

Other names

N5-(3-(7H-Purin-6-yl)pyridin-2-yl)-6-methyl-N1-(3-(trifluoromethoxy)phenyl)isoquinoline-1,5-diamine