TR128

TR128 is a small molecule, orally administered pan-RAF kinase inhibitor developed for the treatment of advanced malignant solid tumors. It acts as a dual inhibitor targeting both RAS (RAS type GTPase family) and RAF kinases (RAF serine/threonine protein kinases), with strong inhibitory activity against BRAF, CRAF, and the BRAF-V600E mutant. This mechanism allows it to overcome the "paradoxical activation" effect seen with some current BRAF inhibitors. Preclinical studies have shown that TR128 inhibits cell proliferation and induces apoptosis in tumor cells harboring RAS or RAF mutations—including colorectal cancer, pancreatic cancer, non-small cell lung cancer, and melanoma—and significantly suppresses tumor growth in animal models. The drug is currently being evaluated in Phase 1 clinical trials for safety, tolerability, pharmacokinetics, and preliminary anti-tumor activity in patients with advanced solid tumors[1][2][3][4][5].