Trifluridine/Tipiracil: A Review in Metastatic Colorectal Cancer

Area of Science:

• Oncology
• Pharmacology

Background:

• Metastatic colorectal cancer (mCRC) presents treatment challenges for patients refractory to standard therapies.
• Trifluridine/tipiracil (Lonsurf®) is an orally active antimetabolite combining trifluridine and tipiracil.
• Tipiracil enhances trifluridine's systemic exposure by inhibiting thymidine phosphorylase.

Purpose of the Study:

• To evaluate the efficacy and safety of trifluridine/tipiracil in adult patients with metastatic colorectal cancer (mCRC).
• To assess trifluridine/tipiracil as a treatment option for patients with unresectable advanced or recurrent CRC.

Main Methods:

• The study involved a multinational, pivotal phase III trial (RECOURSE) and a phase II Japanese trial.
• Patients received oral trifluridine/tipiracil (35 mg/m² twice daily on days 1-5 and 8-12 of each 28-day cycle) plus best supportive care.
• Outcomes measured included overall survival, progression-free survival, and disease control rate.

Main Results:

• Trifluridine/tipiracil significantly improved overall survival and progression-free survival compared to placebo.
• A significantly higher disease control rate was observed in the trifluridine/tipiracil arm.
• The treatment demonstrated an acceptable tolerability profile, with manageable adverse events.

Conclusions:

• Trifluridine/tipiracil is an effective new treatment option for patients with mCRC who have failed or are ineligible for standard chemotherapy.
• The drug offers improved survival outcomes and disease control in this difficult-to-treat population.
• Adverse events are manageable through dose adjustments and supportive care, including granulocyte-colony stimulating factor.