DTS-108

DTS-108 is a water-soluble peptide-drug conjugate (PDC) consisting of SN-38, the active metabolite of the topoisomerase I inhibitor irinotecan, linked to a 20-amino acid human-derived oligopeptide via an esterase-sensitive cross-linker. Developed using Vectocell technology, the conjugate is designed to improve the solubility and delivery of SN-38. Upon administration, the linker is cleaved by endogenous esterases, releasing SN-38, which then inhibits DNA topoisomerase I, leading to DNA strand breaks and apoptosis in rapidly dividing cancer cells. DTS-108 was initially developed by Drais Pharmaceuticals and has been evaluated in Phase I clinical trials for the treatment of advanced solid tumors and malignancies.