Emitefur

**Semantic type:** Organic Chemical|Pharmacologic Substance

**Definition:** An orally available antimetabolite composed of the 1-ethoxymethyl derivative of 5-fluorouracil (5-FU) and the dihydropyrimidine dehydrogenase (DPYD) inhibitor 3-cyano-2,6-dihydroxypyridine (CNDP) in a 1:1 molar ratio, with antineoplastic activity. Upon administration, the prodrug emitefur is converted into 5-FU, while CNDP prevents the degradation of 5-FU by inhibiting DPYD and thereby prolonging the half-life of 5-FU. This increases 5-FU's concentration and thus its antitumor activity through inhibition of DNA and RNA synthesis, as well as inhibition of thymidylate synthase activity. In addition, by inhibiting the formation of 5-FU metabolites, some toxic effects associated with these metabolites may be reduced. DPYD is the rate-limiting enzyme in the catabolism of 5-FU.

**Synonyms:** - (2) m-[[3-(Ethoxymethyl)-5-fluoro-3,6-dihydro-2,6-dioxo-1(2H)-pyrimidinyl]carbonyl]benzoic Acid, 2-Ester with 2,6-Dihydroxynicotinonitrile Benzoate (Ester) - 3-((3-(Ethoxymethyl)-5-fluoro-3,6-dihydro-2,6-dioxo-1(2H)-pyrimidinyl)carbonyl)benzoic acid, 6-(benzoyloxy)-3-cyano-2-pyridinyl ester - 3-[3-(6-Benzoyloxy-3-cyrano-2-pyridyloxycarbonyl)benzoyl]-1-(ethoxymethyl)-5-fluorouracil - BOF-A2 - EMITEFUR - Last-F - [[Ethoxymethyl-5-fluoro-3,6-dihydro-2,6-dioxo-1(2H)-pyrimidinyl]carbonyl]benzoic Acid, 6-(Benzoyloxy)-3-cyano-2-pyridinyl Ester - emitefur