T7-SN-38-rucaparib

T7-SN-38-rucaparib is a transferrin receptor (TfR)-targeted peptide-drug conjugate designed to deliver a combination of the cytotoxic agent SN-38 (the active metabolite of irinotecan) and the PARP inhibitor rucaparib specifically to glioblastoma cells. The conjugate utilizes the T7 peptide (sequence HAIYPRH) as a targeting ligand, which binds to TfR highly expressed on the blood-brain barrier (BBB) and glioblastoma cells, facilitating transcytosis into the brain. Once internalized by tumor cells, a cathepsin B-cleavable linker releases SN-38 and rucaparib, resulting in selective cytotoxicity in cancer cells and reduced toxicity to normal cells. This strategy directly enables the combination delivery of both agents to tumors, overcomes the BBB limitation for rucaparib, and is intended for the treatment of glioblastoma and other TfR-expressing malignancies[1][4].