fialuridine

Fialuridine is a synthetic nucleoside analogue of thymidine that was investigated as an antiviral agent, primarily for the treatment of chronic hepatitis B virus infection. It acts by being incorporated into viral and mitochondrial DNA, thereby inhibiting DNA synthesis. Fialuridine demonstrated potent antiviral activity in early clinical trials but caused severe and fatal toxicity in humans due to mitochondrial damage—specifically, it is incorporated into mitochondrial DNA via its 3'-hydroxyl moiety, leading to impaired mitochondrial function and cell death. The drug’s toxicity was not predicted by preclinical animal studies but resulted in acute liver failure, lactic acidosis, pancreatitis, neuropathy, myopathy, and death or need for liver transplantation in several patients during phase II clinical trials[4][5][7].

Other names

1-(2-deoxy-2-fluoro-1-D-arabinofuranosyl)-5-iodouracil2′-Fluoro-5-iodouracil