Trifluridine (Lonsurf, TAS-102)
Other Medications · Approved since 2015
Description
Trifluridine is an oral fluoropyrimidine nucleoside analog chemotherapy agent formulated with tipiracil hydrochloride as TAS-102 (Lonsurf) for treatment of metastatic colorectal cancer. It is specifically indicated for patients with metastatic CRC who have been previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, anti-VEGF therapy, and if RAS wild-type, anti-EGFR therapy. The drug demonstrates activity in refractory metastatic disease and is being evaluated in minimal residual disease settings after completion of standard adjuvant chemotherapy.
Mechanism of Action
Trifluridine is incorporated into DNA after phosphorylation to its active triphosphate form, where it interferes with DNA synthesis and causes DNA strand breaks during replication. The co-formulated tipiracil hydrochloride inhibits thymidine phosphorylase, preventing rapid degradation of trifluridine and maintaining therapeutic drug levels. This dual mechanism results in cytotoxicity specifically during the S-phase of the cell cycle in rapidly dividing cancer cells.
Side Effects
Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.
Clinical Trials
Quick Info
| Brand Name | Lonsurf, TAS-102 |
| 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 | 50 |
Regimens with this Drug
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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.