Drug intelligence / Profile preview

cisplatin + uracil + tegafur

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

Overview

This drug is a combination chemotherapy regimen consisting of cisplatin, uracil, and tegafur. Tegafur is an oral prodrug of 5-fluorouracil (5-FU), which after absorption is converted into the active anticancer agent 5-FU. Uracil acts as a biochemical modulator by inhibiting the degradation of 5-FU, enhancing its efficacy. Cisplatin is a platinum-based chemotherapeutic agent that causes DNA crosslinking and apoptosis in cancer cells. The combination leverages the cytotoxic effects of cisplatin with the fluoropyrimidine activity from tegafur/uracil to treat various cancers including recurrent/metastatic head and neck squamous cell carcinoma (R/M HNSCC) and advanced gastric cancer. The mechanism involves inhibition of DNA synthesis through thymidylate synthase inhibition by 5-FU metabolites and direct DNA damage by cisplatin. Clinical studies have shown this combination to have moderate response rates with tolerable toxicity profiles. It improves quality of life in responders especially when used in patients without recent prior chemoradiotherapy.

Other names
tegafur/uracilUFT
02

Targets

DPYD (Dihydropyrimidine dehydrogenase)DNATS (Thymidylate synthase)

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