Tipiracil

Tipiracil

Tipiracil is a pharmacological agent used in combination with trifluridine to form the anti-cancer drug trifluridine/tipiracil, also known by the brand name Lonsurf. It is primarily used in the treatment of metastatic colorectal cancer and gastric cancer.

Mechanism of Action

Tipiracil works by inhibiting the enzyme thymidine phosphorylase, which is responsible for the degradation of trifluridine. By inhibiting this enzyme, tipiracil increases the bioavailability of trifluridine in the body, thereby enhancing its anti-cancer effects.

Clinical Use

Tipiracil, in combination with trifluridine, is indicated for the treatment of 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 for the treatment of metastatic gastric or gastroesophageal junction adenocarcinoma previously treated with at least two prior lines of chemotherapy that included a fluoropyrimidine, a platinum-containing chemotherapy, and if appropriate, HER2/neu-targeted therapy.

Side Effects

Common side effects of tipiracil include neutropenia, anemia, thrombocytopenia, fatigue, nausea, diarrhea, decreased appetite, vomiting, and abdominal pain. Severe side effects may include febrile neutropenia and sepsis.

Pharmacokinetics

Tipiracil is administered orally. It is primarily excreted in the urine, with a small amount excreted in the feces. The half-life of tipiracil is approximately 2.1 hours.

See Also

• Trifluridine
• Metastatic colorectal cancer
• Gastric cancer