Drug intelligence / Profile preview

capecitabine + fluorouracil + leucovorin + liposomal irinotecan + oxaliplatin

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

Overview

This is a five-drug combination regimen consisting of capecitabine, fluorouracil, leucovorin, liposomal irinotecan, and oxaliplatin. Each component is a cytotoxic or modulating agent used in the treatment of advanced gastrointestinal cancers. Capecitabine is an oral prodrug of 5-fluorouracil (5-FU), which inhibits thymidylate synthase and disrupts DNA synthesis. Fluorouracil (5-FU) is a pyrimidine analog that also inhibits thymidylate synthase, leading to impaired DNA replication and cell death. Leucovorin enhances the binding of 5-FU to its target enzyme, increasing its efficacy. Liposomal irinotecan (nal-IRI) is a topoisomerase I inhibitor encapsulated in liposomes for improved delivery and reduced toxicity; it prevents DNA re-ligation during replication, causing double-strand breaks and apoptosis. Oxaliplatin forms platinum-DNA adducts that inhibit DNA synthesis and transcription. While combinations such as FOLFOX (fluorouracil/leucovorin/oxaliplatin), FOLFIRI (fluorouracil/leucovorin/irinotecan), XELOX/XELIRI (capecitabine with oxaliplatin or irinotecan), and NALIRIFOX (liposomal irinotecan/oxaliplatin/fluorouracil/leucovorin) are established regimens for colorectal or pancreatic cancer[1][2][4][7][8], there are no published studies or regulatory approvals specifically describing the use of all five agents together in one regimen as listed here.

02

Targets

TOP1 (DNA Topoisomerase I)DNATS (Thymidylate synthase)

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