Trifluridine Tipiracil

Drug

Drug Profile

Trifluridine/tipiracil is marketed as LONSURF, an oral fixed-dose anticancer combination for previously treated metastatic colorectal cancer and metastatic gastric/gastroesophageal junction adenocarcinoma. The formulation combines a nucleoside metabolic inhibitor (trifluridine) with a thymidine phosphorylase inhibitor (tipiracil). U.S. initial approval was in 2015.

Drug Class
Fixed-dose antineoplastic combination: nucleoside metabolic inhibitor + thymidine phosphorylase inhibitor
Approval Status
FDA approved (Initial U.S. Approval: 2015; major indication updates in 2023)
Mechanism of Action
Combines trifluridine cytotoxic nucleoside activity with tipiracil-mediated inhibition of thymidine phosphorylase to support trifluridine exposure.
Brand Names
  • LONSURF
Indications
  • \Metastatic colorectal cancer as single agent or with bevacizumab after prior fluoropyrimidine, oxaliplatin, irinotecan, anti-VEGF therapy, and anti-EGFR therapy if RAS wild-type\
  • \Metastatic gastric or gastroesophageal junction adenocarcinoma previously treated with at least two prior lines including fluoropyrimidine, platinum, taxane or irinotecan, and if appropriate HER2-targeted therapy\

Related News

Related Clinical Trials

NCT ID Title Status Phase
NCT07280377

A Study in Advanced or Metastatic Gastrointestinal Cancers Exploring Treatment Combinations With Pelareorep and Atezolizumab

ACTIVE_NOT_RECRUITING PHASE1/PHASE2
NCT05468892

Phase II Randomized Study Evaluating the Efficacy of Panitumumab (VEctibix ) and Trifluridine-Tipiracil (LOnsurf) in Pretreated RAS Wild Type Metastatic Colorectal Cancer Patients: the VELO Trial

COMPLETED PHASE2