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Irinotecan liposomal is a formulation of irinotecan encapsulated within a lipid bilayer vesicle known as a liposome. It functions as a topoisomerase I inhibitor. Irinotecan and its active metabolite SN-38 bind reversibly to the topoisomerase I-DNA complex and prevent re-ligation of single-strand breaks, leading to exposure time-dependent double-strand DNA damage and cell death. The liposomal formulation extends plasma levels of irinotecan and prolongs exposure of SN-38, resulting in increased antitumor activity. In animal models, irinotecan liposome produced similar intratumor SN-38 exposure at doses 5-fold lower than irinotecan hydrochloride.
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