Tipiracil (Lonsurf)
Other Medications · Approved since 2015
Description
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.
Mechanism of Action
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
Side Effects
Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.
Clinical Trials
Quick Info
| Brand Name | Lonsurf |
| Category | Other Medications |
 Status | FDA Approved |
 EMA Status | EMA Approved |
 Spain Access | Funded by SNS approved in CRC |
| Administration | Oral |
| Year Approved | 2015 |
| Clinical Trials | 12 |
Regimens with this Drug
Related Medications
Medical Disclaimer
This information is for educational purposes only and should not replace professional medical advice. Always consult your healthcare team before making treatment decisions.