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Irinotecan liposome (nal-irinotecan) is a nanoliposomal encapsulated formulation of the topoisomerase I inhibitor irinotecan. It is designed to improve the pharmacokinetic profile and therapeutic index of irinotecan by prolonging drug circulation time and enhancing accumulation within tumor tissues through the enhanced permeability and retention (EPR) effect. Once inside the tumor microenvironment, the liposomes are taken up by macrophages and the active drug is released. Irinotecan and its active metabolite, SN-38, bind to the topoisomerase I-DNA complex, preventing the religation of single-strand DNA breaks, which leads to lethal double-strand DNA damage during replication. It is primarily approved for the treatment of metastatic pancreatic adenocarcinoma in combination with 5-fluorouracil and leucovorin, and is being investigated in various other solid tumors and neoadjuvant settings.
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