Drug intelligence / Profile preview

napabucasin + liposomal irinotecan + fluorouracil + leucovorin

Development stage
Unknown
Lead developer
Sumitomo Pharma
Modality
Nanoparticles → Drug Delivery Systems, Small Molecules
Administration
Intravenous
01

Overview

This combination consists of **napabucasin** (BBI608), a small molecule inhibitor targeting cancer stemness pathways (primarily acting as a STAT3 inhibitor), **liposomal irinotecan** (known as Onivyde), a topoisomerase I inhibitor in a nanoparticle/liposomal formulation that enhances delivery and reduces toxicity, **fluorouracil** (5-FU), a pyrimidine analogue inhibiting thymidylate synthase to block DNA synthesis, and **leucovorin** (folinic acid), which potentiates the action of fluorouracil by stabilizing its binding to thymidylate synthase. - Napabucasin is developed as an anti-cancer agent targeting the STAT3 pathway and cancer stemness. - Liposomal irinotecan enhances tissue penetration and reduces side effects compared to non-liposomal forms. - Fluorouracil and leucovorin are widely-used in colorectal and other GI cancers to inhibit DNA replication and cell proliferation. - The combination is under investigation for **advanced gastrointestinal malignancies**, especially metastatic pancreatic cancer, as well as other solid tumors refractory to standard therapy.

Other names
BBI608BBI-608BBI 608CPT-11 liposomeCPT11 liposomeCPT 11 liposome5-FUfolinic acid
02

Targets

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

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