Drug intelligence / Profile preview

irinotecan liposome + fluorouracil + leucovorin

Development stage
Phase 3
Lead developer
Ipsen
Modality
Small Molecules, Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

Irinotecan liposome in combination with fluorouracil and leucovorin is a pharmaceutical regimen used primarily for the treatment of metastatic pancreatic adenocarcinoma. Irinotecan liposome (marketed as Onivyde) is a topoisomerase 1 inhibitor encapsulated in a lipid bilayer vesicle (liposome), which enhances drug delivery to tumors and prolongs systemic exposure. Upon administration, irinotecan is converted to its active metabolite SN-38, which binds reversibly to the topoisomerase 1-DNA complex and prevents re-ligation of single-strand DNA breaks, leading to double-strand DNA damage and cell death. Fluorouracil is an antimetabolite that inhibits thymidylate synthase, disrupting DNA synthesis; leucovorin enhances the binding of fluorouracil to its target enzyme. This combination has demonstrated efficacy as first-line therapy for metastatic pancreatic cancer (in combination with oxaliplatin) and as second-line therapy after gemcitabine-based regimens[1][3][4][5][6].

Brand names
Onivyde + 5-FU/LVNALIRIFOX
Other names
irinotecan liposome injection + 5-fluorouracil + leucovorinnal-IRI+5-FU/LV
02

Targets

TOP1 (DNA Topoisomerase I)TS (Thymidylate synthase)

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