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Fosfluridine tidoxil is an orally bioavailable small molecule prodrug of 5-fluoro-2'-deoxyuridine (FUdR), designed to inhibit thymidylate synthase. Developed by Heidelberg Pharma (formerly Wilex AG), the compound was engineered to provide a more controlled and sustained release of the active metabolite compared to traditional fluoropyrimidines like 5-fluorouracil, with the goal of reducing systemic toxicity and improving the therapeutic index. It reached Phase IIa clinical trials for the treatment of various solid tumors, including colorectal and breast cancers, and was also investigated in a topical formulation for actinic keratosis. Development of the compound has largely ceased as the developer shifted its strategic focus toward its Antibody Targeted Amanitin Conjugate (ATAC) platform.
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