Drug intelligence / Profile preview

tegafur + uracil + capecitabine

Development stage
Unknown
Lead developer
Taiho Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

tegafur + uracil + capecitabine is a combination of oral fluoropyrimidine antimetabolites used in the treatment of gastrointestinal cancers. The regimen consists of Ugotex (a fixed-dose combination of tegafur and uracil) and capecitabine. Tegafur is a prodrug of 5-fluorouracil (5-FU), while uracil acts as a competitive inhibitor of dihydropyrimidine dehydrogenase (DPD), the enzyme responsible for 5-FU catabolism, thereby increasing the systemic concentration and half-life of 5-FU. Capecitabine is another 5-FU prodrug that undergoes a three-step enzymatic conversion to the active drug, with the final step mediated by thymidine phosphorylase, which is often overexpressed in tumor tissues. Both components ultimately work by inhibiting thymidylate synthase and incorporating into RNA and DNA, leading to the disruption of nucleic acid synthesis and tumor cell death. In the context of the Phase 4 real-world study (NCT06104137) conducted by Liaoning Cancer Hospital & Institute, these agents are evaluated as postoperative adjuvant therapies for patients with gastric or gastroesophageal junction adenocarcinoma who achieved a pathological complete response (pCR) after neoadjuvant chemo-immunotherapy. It is important to note that in clinical practice and the referenced trial, these agents are typically administered as alternative monotherapies within the same study arm rather than as a concurrent combination.

Brand names
Xeloda
Other names
UFT + capecitabineTegafur-Uracil + capecitabineUgotex plus capecitabine
02

Targets

DPYD (Dihydropyrimidine dehydrogenase)TS (Thymidylate synthase)DNA

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