Drug glossary Drug

Tipiracil Lonsurf

A drug approved for colorectal cancer. It appears in 8 clinical trials.

Oral Thymidylate synthase DNA polymerase
See its trials
United States FDA approved Since 2015
European Union EMA approved Since 2015
Spain Funded by SNS Approved for colorectal cancer

What it is

Trifluridine/tipiracil (TAS-102) is an oral nucleoside antimetabolite combination chemotherapy agent approved for treatment of metastatic colorectal cancer in patients who have been previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, anti-VEGF therapy, and if RAS wild-type, anti-EGFR therapy. The combination consists of trifluridine, the active cytotoxic component, and tipiracil hydrochloride, which prevents trifluridine degradation by inhibiting thymidine phosphorylase. This agent provides a treatment option for heavily pretreated patients with refractory metastatic colorectal cancer who have limited therapeutic alternatives.

How it works

Trifluridine is incorporated into DNA during replication, causing DNA dysfunction and ultimately cell death. Tipiracil hydrochloride serves as a thymidine phosphorylase inhibitor that prevents the rapid degradation of trifluridine, thereby maintaining higher plasma concentrations of the active cytotoxic agent and enabling its therapeutic effect.

Molecular targets

Common side effects

NeutropeniaAnemiaThrombocytopeniaFatigueNauseaDecreased appetiteDiarrheaVomitingAbdominal painPyrexia

Not all are listed, and everyone experiences them differently. If you notice any, tell your care team.