Trifluridine/tipiracil

Trifluridine/Tipiracil

Chemical structure of Trifluridine and Tipiracil

Mechanism of action of TAS-102

Trifluridine/tipiracil, marketed under the brand name Lonsurf, is a combination medication used in the treatment of certain types of cancer. It is specifically indicated for the treatment of metastatic colorectal cancer and gastric cancer in patients who have been previously treated with other therapies.

Composition

Trifluridine/tipiracil is composed of two active ingredients:

• Trifluridine, a nucleoside analog that interferes with DNA synthesis.
• Tipiracil, an inhibitor of the enzyme thymidine phosphorylase, which helps to maintain the concentration of trifluridine in the body by preventing its degradation.

Mechanism of Action

Trifluridine is incorporated into the DNA of cancer cells, leading to DNA damage and cell death. Tipiracil enhances the bioavailability of trifluridine by inhibiting its breakdown, thereby increasing its effectiveness. This combination results in the inhibition of tumor growth.

Clinical Use

Trifluridine/tipiracil is used in patients with metastatic colorectal cancer who have been previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, an anti-VEGF biological therapy, and, if RAS wild-type, an anti-EGFR therapy. It is also used in patients with metastatic gastric cancer who have been treated with at least two prior chemotherapy regimens.

Side Effects

Common side effects of trifluridine/tipiracil include:

• Neutropenia
• Anemia
• Fatigue
• Nausea
• Diarrhea

Patients should be monitored for hematological toxicity and other adverse effects during treatment.

Approval and Regulation

Trifluridine/tipiracil was approved by the United States Food and Drug Administration (FDA) in 2015 for the treatment of metastatic colorectal cancer. It has since been approved in other countries and for additional indications.

Related Pages

• Colorectal cancer
• Gastric cancer
• Chemotherapy