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Trifluridine/tipiracil

  • AntimetabolitesAntimetabolites
  • High alertAn error with this medicine can cause serious harm: double checks and protocols are used.
  • Pregnancy: avoidAvoid in pregnancy. It may harm the fetus: a pregnancy test is done first, women use contraception during and for months after treatment, men use condoms, and breastfeeding is…

An oral pair: trifluridine enters tumour DNA and tipiracil stops its breakdown. Used in advanced colorectal and gastric cancer; watch neutrophils.

Updated

Also called: TAS-102

Quick facts

Group
Antimetabolites
Target
Thymidine phosphorylase (blocked by tipiracil); DNA (trifluridine)
Used for
Metastatic gastric
Key effects
Nausea · Fatigue and loss of appetite · Anaemia
Monitor
Complete blood count before · Signs of infection
ATC
L01BC59

No doses: the clinician sets them by the current guideline.

Mechanism of action

The crystal shows tipiracil in the active site of human thymidine phosphorylase, the enzyme that would otherwise destroy trifluridine.

Target in 3D: Thymidine phosphorylase (blocked by tipiracil); DNA (trifluridine). PDB structure 1UOU (RCSB PDB, public domain). View the structure at RCSB PDB

Trifluridine is a thymidine-based nucleoside analogue. Cells phosphorylate it and build it into DNA in place of thymidine, which damages DNA and stops tumour growth. Taken alone, trifluridine is quickly broken down by thymidine phosphorylase; tipiracil blocks that enzyme so trifluridine reaches useful levels.

  1. Tipiracil blocks thymidine phosphorylase
  2. Trifluridine stays in the blood longer
  3. Trifluridine is built into DNA and stops cell growth

Indications

  • Metastatic colorectal cancer previously treated with other chemotherapy, alone or with bevacizumab. Colorectal cancer →
  • Metastatic gastric or gastro-oesophageal junction cancer after at least two prior lines. Gastric cancer →

Adverse effects

Common

  • Nausea, vomiting, diarrhoea, abdominal pain
  • Fatigue and loss of appetite
  • Anaemia
  • Hair loss, taste change, mouth sores

Contraindications

  • Hypersensitivity to trifluridine or tipiracil

Key interactions

Bevacizumab (used together)
Combined in metastatic colorectal cancer; neutropenia is watched closely.

What is monitored

  • Complete blood count before and during each cycle
  • Signs of infection
  • Liver and kidney function

Administration and safety

  • Oral hazardous drug: tablets swallowed whole, not split, crushed or chewed.
  • Two tablet strengths exist and may be combined: the strength and number are checked carefully.
  • Hands are washed after handling; other people handling the tablets wear gloves.
  • If vomiting follows a dose, no extra dose is taken.

Pregnancy and breastfeeding

Avoid in pregnancy. It may harm the fetus: a pregnancy test is done first, women use contraception during and for months after treatment, men use condoms, and breastfeeding is stopped.

Nursing care

  • Check blood counts before each cycle; teach to report fever or chills at once.
  • Teach the schedule (treatment days and rest days) and to take tablets with food.
  • Teach to report diarrhoea or vomiting that is severe or does not stop.
  • Contraception for women and for men with partners who could conceive.

Pharmacokinetics

Absorption
Oral tablets taken with food, on set days of each cycle.

Test yourself

Think of the answer, then tap the question to see it.

What does tipiracil add to trifluridine?

It inhibits thymidine phosphorylase, which would otherwise rapidly break down trifluridine.

How does trifluridine damage cancer cells?

It is incorporated into DNA in place of thymidine.

Which laboratory test is checked before each cycle?

A complete blood count, mainly for neutropenia.

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More Pharmacology questions →

Connections

← Back to the class: Antimetabolites

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: Trifluridine and Tipiracil: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2024); RCSB PDB - 1UOU: Crystal structure of human thymidine phosphorylase in complex with a small molecule inhibitor (RCSB Protein Data Bank, 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.