RG1534

RG1534 is a small molecule inhibitor developed by Reglagene that targets the mutated hTERT (human Telomerase Reverse Transcriptase) promoter, a common genetic driver in glioblastoma (GBM). Mutations in the TERT promoter occur in over 80% of GBM cases, leading to the upregulation of TERT and subsequent telomere maintenance and cancer cell immortality. RG1534 is designed to interfere with the functionality of this mutated promoter, likely by stabilizing G-quadruplex (G4) DNA structures within the promoter region. Preclinical studies have demonstrated that RG1534 selectively suppresses the viability of glioma cells while sparing normal astrocytes. The compound induces rapid apoptosis and increases the generation of reactive oxygen species (ROS), effects that appear to be independent of traditional telomere shortening, suggesting that RG1534 also disrupts non-canonical functions of TERT, such as its role in mitochondrial pathobiology.