Drug intelligence / Profile preview

trifluridine + tipiracil + nanoliposomal irinotecan

Development stage
Unknown
Lead developer
Taiho Pharmaceutical
Modality
Nanoparticles → Drug Delivery Systems, Small Molecules
Administration
Oral (trifluridine + Tipiracil), Intravenous (nanoliposomal Irinotecan)
01

Overview

This drug is a **combination regimen** consisting of: - Trifluridine, a thymidine-based nucleoside analog incorporated into DNA, leading to DNA dysfunction and tumor growth inhibition - Tipiracil, a thymidine phosphorylase inhibitor, which enhances the efficacy of trifluridine by preventing its breakdown - Nanoliposomal irinotecan (nal-IRI, brand name Onivyde), a liposome-encapsulated topoisomerase I inhibitor that blocks DNA replication and transcription, delivered in a nanoliposomal formulation to improve pharmacokinetics and tissue targeting The combination is under clinical investigation for treating **advanced or refractory gastrointestinal cancers** including pancreatic, biliary tract, and colorectal cancers. Its mechanism relies on **dual nucleoside analog activity plus topoisomerase I inhibition**, aiming for synergistic antitumor effects and overcoming resistance to standard therapies[1][5][7][9]. Developers include companies responsible for TAS-102 (Taiho Oncology) and Onivyde (Ipsen). The drugs are manufactured by these companies for use in combination regimens in clinical trials. The combination itself does not have a separate unique brand name and is currently an investigational protocol.

Brand names
Lonsurf (trifluridine + tipiracil)Onivyde (nanoliposomal irinotecan)
Other names
trifluridine/tipiracil + liposomal irinotecanTAS-102 + liposomal irinotecantrifluridine/tipiracil + nal-IRIFTD/TPI + nal-IRI
02

Targets

TOP1 (DNA Topoisomerase I)TYMP (Thymidine phosphorylase)DNA

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