emitefur

Emitefur (BOF-A2) is an orally active anticancer drug developed as a derivative of 5-fluorouracil (5-FU). It consists of two main components: a masked form of 5-FU known as 1-ethoxymethyl-5-fluorouracil (EM-FU), and a potent inhibitor of 5-FU degradation called 3-cyano-2,6-dihydroxypyridine (CNDP). After oral administration, BOF-A2 is rapidly hydrolyzed to release EM-FU and CNDP. EM-FU is further metabolized in the liver to generate active 5-FU. CNDP inhibits dihydropyrimidine dehydrogenase (DPD), the enzyme responsible for degrading 5-FU, thereby increasing and prolonging the concentration of active drug in tumor tissues. This dual mechanism results in higher and more sustained levels of cytotoxic agent within tumors compared to plasma. BOF-A2 demonstrated antitumor activity in preclinical models and clinical trials for advanced gastric cancer but development was discontinued for several other cancers including breast cancer, colorectal cancer, gastrointestinal cancer, lung cancer, non-small cell lung cancer, and pancreatic cancer[1][3][6][7].

Brand names

Last-F

Other names

1-ethoxymethyl-5-fluorouracil3-cyano-2,6-dihydroxypyridine