Tegafur (UFT (when combined with uracil), Ftorafur)

Other Medications · Approved since 2001

US FDA Approved EU EMA Approved ES Hospital use approved in CRC Oral 6 Clinical Trials
Thymidylate synthase DNA synthesis pathways

Description

Tegafur is an oral fluoropyrimidine antimetabolite chemotherapy agent used in the treatment of colorectal cancer, particularly as adjuvant therapy following surgical resection. It is commonly formulated in combination with uracil (as UFT - uracil-tegafur) and administered with leucovorin to enhance efficacy. Tegafur serves as a prodrug that is converted to 5-fluorouracil (5-FU) in the body, providing sustained release of the active cytotoxic agent while potentially reducing some systemic toxicities associated with intravenous 5-FU administration.

Mechanism of Action

Tegafur is metabolized to 5-fluorouracil through cytochrome P450 enzymes, primarily in the liver and tumor tissues. The active metabolite 5-FU inhibits thymidylate synthase, blocking DNA synthesis and repair, while also incorporating into RNA to disrupt protein synthesis. The co-administered uracil competitively inhibits dihydropyrimidine dehydrogenase, the enzyme responsible for 5-FU degradation, thereby prolonging the half-life and enhancing the antitumor activity of the converted 5-FU.

Molecular Targets

Side Effects

Diarrhea Nausea Vomiting Fatigue Hand-foot syndrome Stomatitis Neutropenia Anemia

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials

NCT01225744 Phase 2
Archived
Erbitux Study of CPT11, Oxaliplatin, UFToral Targeted Therapy
United Kingdom
NCT00660894 Phase 3
Archived
Tegafur-Uracil and Leucovorin or S-1 in Treating Patients With Stage III Colon Cancer That Has Been Completely Removed by Surgery
Japan
NCT00207831 Phase 3
Archived
Trial Testing Ftorafur (UFT) Associated With Neoadjuvant Radiotherapy Versus Radiotherapy Alone in Rectal Adenocarcinoma
France
NCT00004860 Phase 2
Completed
Fluorouracil-Uracil and Leucovorin in Treating Elderly Patients With Metastatic Colorectal Cancer
United States, Puerto Rico
NCT00378716 Phase 3
Archived
Combination Chemotherapy in Treating Patients With Resected Colon Cancer
NCT00002801 Phase 1
Archived
Combination Chemotherapy and Radiation Therapy in Treating Patients With Colorectal Cancer
United States