TSL-1502

TSL-1502 is an oral small molecule prodrug developed as a targeted therapy for cancer. It is designed to be selectively converted in the tumor microenvironment by the enzyme beta-glucuronidase into its active metabolite, TSL-1502M. The active form, TSL-1502M, potently inhibits poly(ADP-ribose) polymerase 1 and 2 (PARP1/2), enzymes involved in DNA repair via the base-excision repair pathway. By inhibiting PARP-mediated DNA repair, TSL-1502M induces synthetic lethality in homologous recombination-deficient cancer cells and enhances sensitivity to chemotherapy. Preclinical studies have shown that TSL-1502 achieves higher localized concentrations at tumor sites with greater potency and a wider therapeutic window compared to existing PARP inhibitors, while minimizing systemic toxicity[1][3][5]. Clinical development includes phase I trials for advanced solid tumors and phase II trials for HER2-negative breast cancer[5].

Other names

TSL-1502TSL1502TSL 1502