GT818

GT818 is a first-in-class, orally available small molecule PROTAC (Proteolysis-targeting chimera) degrader designed to selectively target the ribosomal S6 kinase (RSK) protein family. Developed by Gluetacs Therapeutics, GT818 induces the ubiquitin-proteasome-mediated degradation of pathogenic RSK proteins, which are implicated in various oncogenic signaling pathways. Preclinical studies have demonstrated that GT818 possesses a high safety window, significant tumor enrichment across multiple solid tumor types, and moderate blood-brain barrier penetration. The drug is currently being developed for the treatment of advanced solid tumors, including breast cancer, prostate cancer, non-small cell lung cancer (NSCLC), pancreatic cancer, and colorectal cancer. As of late 2025, GT818 is in the IND-enabling phase, with clinical development expected to formally commence in early 2026.