Disease relevance of Emitefur

• PURPOSE: To determine the toxicities, dose-limiting toxicities (DLT), maximum-tolerated dose, and pharmacokinetic profile of emitefur (BOF-A2) in patients with advanced solid tumors [1].
• The ED50 (the dose for 50% inhibition) values of BOF-A2 were 25 mg/kg against sarcoma-180 and 15 mg/kg against Yoshida sarcoma [2].
• Efficacy of a new 5-fluorouracil derivative, BOF-A2, in advanced non-small cell lung cancer. A multi-center phase II study [3].
• These results indicate that compared with 5-FU, BOF-A2 more strongly suppresses the growth of squamous cell carcinoma by inhibiting DNA synthesis and inducing apoptosis but not cell differentiation [4].
• Based on the above findings, BOF-A2 is considered to be a promising anticancer drug for patients with advanced gastric cancer [5].

High impact information on Emitefur

• Phase I assessment of the pharmacokinetics, metabolism, and safety of emitefur in patients with refractory solid tumors [1].
• Oral administration of BOF-A2 to rats with lung transplanted tumors results in increased 5-fluorouracil levels [6].
• Oral BOF-A2 (Emitefur), a new derivative of 5-fluorouracil (5-FU) containing both 1-ethoxymethyl-5-FU (EMFU), a masked form of 5-FU, and 3-cyano-2,6-dihydroxypyridine (CNDP), an inhibitor of 5-FU degradation, was administered to 71 non-small cell lung cancer (NSCLC) patients in a multi-center phase II study [3].
• A phase II trial of a new 5-fluorouracil derivative, BOF-A2 (Emitefur), for patients with advanced gastric cancer [5].

References