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Isothifluoridine is a small molecule anti-HBV (Hepatitis B Virus) agent developed by the Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences. Chemically, it is 1-(2-isothiocyanatoethyl)-5-fluorouracil, a non-nucleoside derivative of 5-fluorouracil. It functions as an inhibitor of the HBV DNA polymerase, an essential enzyme for viral replication. By targeting the polymerase, isothifluoridine suppresses the synthesis of viral DNA, offering a potential therapeutic approach for chronic hepatitis B infection. The drug has been evaluated in Phase 1 clinical trials in China (e.g., CTR20130066) to assess its safety, tolerability, and pharmacokinetic profile in healthy volunteers.
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