Drug intelligence / Profile preview

nal-IRI + fluorouracil + sodium levofolinate

Development stage
Unknown
Lead developer
Ipsen
Modality
Small Molecules
Administration
Intravenous
01

Overview

This is a combination chemotherapy regimen consisting of nanoliposomal irinotecan (nal-IRI), fluorouracil (5-FU), and sodium levofolinate. Nal-IRI is a liposomal formulation of irinotecan, a topoisomerase I inhibitor that interferes with DNA replication in cancer cells. Fluorouracil is an antimetabolite that inhibits thymidylate synthase, disrupting DNA synthesis and function. Sodium levofolinate (the disodium salt of the active stereoisomer of folinic acid) enhances the binding of fluorouracil to thymidylate synthase, increasing its cytotoxic effect. This combination has been approved for use in advanced pancreatic cancer after progression on gemcitabine-based therapy and is also used off-label or in clinical trials for other gastrointestinal cancers[2][4][8]. The regimen improves survival compared to monotherapy with either agent alone and offers manageable toxicity[4][2]. Sodium levofolinate provides advantages over calcium levofolinate due to improved solubility, allowing co-administration with 5-FU in a single infusion pump[1][6].

Brand names
Onivyde (for nal-IRI)
Other names
nanoliposomal irinotecan + 5-fluorouracil + sodium levofolinateliposomal irinotecan + 5-FU + Na-levofolinatenal-IRI + 5-FU/Levo-LV
02

Targets

TOP1 (DNA Topoisomerase I)TS (Thymidylate synthase)

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