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IHL-305 is an investigational PEGylated liposomal formulation of irinotecan, co-developed by Yakult Honsha and Terumo Corporation. It encapsulates irinotecan within PEG-modified liposomes composed of cholesterol and hydrogenated soybean phosphatidylcholine, with a mean particle diameter of approximately 100 nm. This lipid nanoparticle delivery system is designed to improve the therapeutic index of conventional irinotecan by prolonging drug exposure in plasma and enhancing accumulation in tumor tissues via the enhanced permeability and retention (EPR) effect. Once released, irinotecan is converted into its active metabolite, SN-38, which inhibits DNA topoisomerase I, leading to DNA strand breaks and cell death. IHL-305 was evaluated in Phase I clinical trials for patients with advanced solid tumors but has not progressed to later-stage development.
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