tipiracil hydrochloride + trifluridine: clinical use

Prescribing considerations

• Initiation and supervision should be by clinicians experienced in anticancer therapy.
• Assess renal and hepatic function, unresolved toxicity from previous treatment and baseline haematological status.
• Myelosuppression and gastrointestinal toxicity commonly require interruption or modification according to the product information.
• Moderate or severe renal impairment requires closer haematological monitoring; use is not recommended in end-stage renal disease.
• Use is not recommended with baseline moderate or severe hepatic impairment.

Contraindications and cautions

• Hypersensitivity to either active substance or any excipient.
• The lactose-containing tablets should not be used in rare hereditary galactose intolerance, total lactase deficiency or glucose-galactose malabsorption.

Monitoring

• Full blood count before treatment and regularly thereafter.
• Evidence of infection, bleeding, anaemia and gastrointestinal toxicity.
• Renal function, particularly where impairment is present.
• Liver tests and bilirubin where clinically indicated.
• Proteinuria before and during treatment.
• Hydration and electrolytes if vomiting or diarrhoea develops.

Clinical pharmacology

Trifluridine is a thymidine-based nucleoside analogue incorporated into DNA after intracellular phosphorylation. Tipiracil inhibits thymidine phosphorylase, markedly increasing systemic trifluridine exposure; clinically significant CYP-mediated interactions are not expected.

Formulation and product differences

• Two film-coated tablet strengths are available and may be combined to provide the prescribed amount.
• The lower-strength tablet is white and the higher-strength tablet is pale red, with identifying imprints.
• Both strengths contain lactose.
• As a cytotoxic product, it is not considered suitable for repacking into multicompartment compliance aids because of handler risk.