DFP-11207

DFP-11207 is a novel oral fluoropyrimidine antimetabolite designed for cancer chemotherapy. It is a small molecule that combines three components in a single agent: 1) a prodrug of 5-fluorouracil (1-ethoxymethyl-5-fluorouracil, EM-FU), 2) an inhibitor of dihydropyrimidine dehydrogenase (DPD; specifically, 5-chloro-2,4-dihydroxypyridine or CDHP), and 3) an inhibitor of orotate phosphoribosyltransferase (OPRT; citrazinic acid or CTA)[1][3][4][5]. Upon oral administration and hydrolysis in the body, these components work synergistically to enhance the pharmacological activity of released 5-FU while reducing its gastrointestinal and myelosuppressive toxicities[1][3][6]. Mechanistically, DFP-11207 acts as a thymidylate synthase inhibitor by releasing active 5-FU which binds to and inhibits thymidylate synthase (TS), thereby blocking DNA synthesis and cell division in tumor cells[2][4]. The drug has been evaluated primarily for advanced solid tumors including esophageal, colorectal, gastric, pancreatic, and gallbladder cancers[1][7]. Early-phase clinical trials have shown it to be well-tolerated with reduced toxicity compared to traditional fluoropyrimidines such as capecitabine or S‑1[1][7].

Other names

UNII-33RN5G108EUNII33RN5G108EUNII 33RN5G108E33RN5G108E1296177-16-6