Drug intelligence / Profile preview

TEGAFIRI

Development stage
Unknown
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

TEGAFIRI is a combination chemotherapy regimen consisting of tegafur-uracil (UFUR) and irinotecan. It is primarily used for the treatment of metastatic or recurrent colorectal cancer[3]. This regimen serves as an effective alternative to the FOLFIRI regimen (which uses 5-fluorouracil instead of tegafur-uracil)[3]. The effectiveness of TEGAFIRI is based on the combined action of its components: 1. **Tegafur-uracil (UFUR)**: A combination of tegafur and uracil in a 4:1 molar ratio. - Tegafur is a prodrug that is metabolized to 5-fluorouracil (5-FU) in the liver[3]. - Uracil competitively inhibits dihydropyrimidine dehydrogenase, which slows the breakdown of 5-FU, allowing it to remain in cancer cells longer[5]. - This combination results in higher plasma levels of 5-FU compared to tegafur alone[3]. - The active metabolites of tegafur inhibit the enzyme thymidylate synthase and intercalate into RNA, disrupting DNA synthesis and RNA function, leading to tumor cell cytotoxicity[2]. 2. **Irinotecan**: A chemotherapy drug that works synergistically with tegafur-uracil. The regimen typically includes leucovorin (calcium folinate) as an essential component to enhance efficacy[3].

Brand names
TEGAFIRI
Other names
UFT/leucovorin and irinotecanUFT/LV and irinotecanuracil/tegafur + irinotecan + leucovorin
02

Targets

TOP1 (DNA Topoisomerase I)DPYD (Dihydropyrimidine dehydrogenase)TS (Thymidylate synthase)

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