TR100

TR100 is a first-in-class small molecule inhibitor designed to selectively disrupt the actin cytoskeleton of tumor cells by targeting the cancer-associated tropomyosin isoform Tm5NM1 (encoded by the TPM3 gene). Unlike traditional anti-actin agents, which are often limited by severe cardiotoxicity due to their effects on muscle sarcomeres, TR100 demonstrates high specificity for cytoskeletal tropomyosin over muscle-specific isoforms. By binding to tropomyosin, TR100 disables the actin-tropomyosin filament assembly, leading to the induction of the intrinsic (mitochondrial) apoptotic pathway. This mechanism appears to be independent of the pro-apoptotic factors BAX and BAK. Preclinical studies in neuroblastoma and melanoma models have demonstrated that TR100 inhibits cell growth, motility, and tumor progression in vivo without evidence of cardiac damage, as measured by troponin levels and heart morphology.