Drug intelligence / Profile preview

floxuridine + irinotecan + leucovorin

Development stage
Unknown
Modality
Small Molecules
Administration
Intra-arterial, Intravenous
01

Overview

This is a combination chemotherapy regimen consisting of three agents—floxuridine, irinotecan, and leucovorin. Floxuridine is a pyrimidine analog that inhibits thymidylate synthase, leading to disruption of DNA synthesis and cell death. Irinotecan is a topoisomerase I inhibitor that prevents DNA unwinding and replication, resulting in cytotoxicity primarily in rapidly dividing cancer cells. Leucovorin (folinic acid) enhances the binding of fluoropyrimidines like floxuridine to thymidylate synthase, increasing their antitumor efficacy. This combination has been studied primarily for the treatment of advanced or metastatic colorectal cancer, particularly for liver metastases where hepatic arterial infusion (HAI) may be used to deliver floxuridine directly to the liver while irinotecan and leucovorin are administered systemically[2][6][9]. The regimen aims to maximize tumor response by combining agents with complementary mechanisms.

02

Targets

TS (Thymidylate synthase)TOP1 (DNA Topoisomerase I)DHFR (Dihydrofolate reductase)

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