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Tipiracil is a small molecule drug used in oncology as a component of the combination medication trifluridine/tipiracil (marketed as Lonsurf). Tipiracil itself is not used as monotherapy but serves to enhance the efficacy of trifluridine by inhibiting thymidine phosphorylase, an enzyme responsible for degrading trifluridine. By blocking this enzyme, tipiracil increases and prolongs systemic exposure to trifluridine, allowing it to exert its antitumor effects more effectively. The primary indication for tipiracil (in combination with trifluridine) is the treatment of metastatic colorectal cancer and metastatic gastric or gastroesophageal junction adenocarcinoma in patients who have been previously treated with other chemotherapies[1][2][7].
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