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Irinotecan + tegafur is a combination of two chemotherapeutic agents used primarily in the treatment of various solid tumors such as colorectal and gastric cancers. Irinotecan is a topoisomerase I inhibitor that is converted in the body to its active metabolite SN-38. This metabolite binds to DNA topoisomerase I-DNA complexes and prevents religation of single-strand breaks during DNA replication, leading to double-stranded DNA breaks and apoptosis in cancer cells[1][2][5]. Tegafur is an oral prodrug of fluorouracil (5-FU), a pyrimidine analogue antimetabolite. Once bioactivated to 5-FU, it inhibits thymidylate synthase and disrupts DNA synthesis by interfering with the pyrimidine pathway[4]. The combination leverages different mechanisms for synergistic anticancer effects[6]. Both drugs are often used as part of multi-agent regimens for advanced or metastatic gastrointestinal cancers.
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