Drug intelligence / Profile preview

irinotecan liposome (Ipsen, 045525)

Development stage
Approved
Lead developer
Ipsen
Modality
Small Molecules, Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

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.

Brand names
Onivyde
Other names
nal-irinotecannal-IRInanoliposomal irinotecanliposomal irinotecan
02

Targets

TOP1 (DNA Topoisomerase I)

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