Drug intelligence / Profile preview

napabucasin + irinotecan + leucovorin + 5-fluorouracil

Development stage
Unknown
Lead developer
Sumitomo Pharma
Modality
Small Molecules
Administration
Intravenous
01

Overview

This medication is a four-drug combination used primarily in the treatment of metastatic colorectal cancer. It consists of **napabucasin** (a reactive oxygen species generator and STAT3 inhibitor developed as an investigational anti-cancer agent), **irinotecan** (a topoisomerase I inhibitor that interferes with DNA replication in cancer cells), **leucovorin** (folinic acid, which enhances the activity of 5-fluorouracil), and **5-fluorouracil** (an antimetabolite that inhibits thymidylate synthase, thus interfering with DNA synthesis). The primary mechanism combines multiple cytotoxic and targeted actions, aiming to disrupt DNA synthesis, enhance apoptotic pathways, and counteract chemoresistance. Napabucasin is under investigation and not standard in colorectal cancer regimens, which more commonly use irinotecan, leucovorin, and 5-fluorouracil as FOLFIRI[1][2][3]. Napabucasin is being developed as part of triple and quadruple chemotherapy regimens to improve tumor response and overcome resistance.

Brand names
WellcomeCaracEfudexAdrucil
Other names
FOLFIRIirinotecan + 5-fluorouracil + leucovorin
02

Targets

TOP1 (DNA Topoisomerase I)STAT3 (Signal Transducer and Activator of Transcription 3)TS (Thymidylate synthase)

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