Drug intelligence / Profile preview

trifluridine + tipiracil

Development stage
Approved
Lead developer
Taiho Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

**Trifluridine + tipiracil** is an oral fixed-dose antineoplastic combination composed of trifluridine, a thymidine-based nucleoside metabolic inhibitor, and tipiracil, a thymidine phosphorylase inhibitor. Trifluridine is incorporated into tumor-cell DNA, disrupting DNA synthesis and inhibiting cellular proliferation; tipiracil inhibits trifluridine metabolism by thymidine phosphorylase, increasing systemic trifluridine exposure. Marketed as **Lonsurf**, it was developed by Taiho Pharmaceutical and is approved in the United States for previously treated metastatic colorectal cancer as monotherapy or with bevacizumab, and for previously treated metastatic gastric or gastroesophageal junction adenocarcinoma. Its dose-limiting clinical risk is myelosuppression, particularly neutropenia. ([accessdata.fda.gov](https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/207981s012lbl.pdf))

Brand names
Lonsurf
Other names
FTD-TPIFTD/TPItrifluridine + tipiraciltrifluridine + tipiracil hydrochloridetrifluridine and tipiraciltrifluridine and tipiracil hydrochloridetrifluridine/tipiraciltrifluridine/tipiracil hydrochloride
02

Targets

DNATYMP (Thymidine phosphorylase)TS (Thymidylate synthase)

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