CAS: 1868135-06-1

Sofosbuvir d6 is a deuterated antiviral drug used for the treatment of Hepatitis C virus (HCV) infection, which is synthesized chemically. This modification involves the replacement of hydrogen atoms with deuterium, a stable isotope of hydrogen, resulting in enhanced pharmacokinetic properties. By incorporating deuterium, the metabolic stability of the compound is improved due to the kinetic isotope effect, which slows down the metabolic degradation of the compound. Sofosbuvir d6 acts as a prodrug, which, upon administration, is converted into its active triphosphate form. It functions as a nucleotide analog inhibitor of the HCV NS5B polymerase, essential for viral RNA replication. By acting as an alternative substrate for the RNA-dependent RNA polymerase, it results in chain termination, thereby inhibiting the replication of the virus. This product is utilized in scientific research and development settings to analyze the metabolism and efficacy of antiviral drugs, providing a model for studying the pharmacokinetics and dynamics of antiviral agents. It is particularly valuable in preclinical and clinical research phases to assess potential benefits in therapeutic applications.

Applications Isotope labelled PSI-7977 (P839640), a prodrug that is metabolized to the active antiviral agent 2'-deoxy-2'-α-fluoro-β-C-methyluridine-5'-monophosphate and is currently being investigated in phase 3 clinical trials for the treatment of hepatitis C. Studies have profiled PSI-7977 as a nucleotide inhibitor of hepatitis C virus, exerting selective inhibitory effects towards HCV NS5B polymerase. References Lam, A.M.,et al.: Antimicrob. Agents. Chemotherapy., 56, 3359 (2012); Lam, A.M., et al.: J. Virol., 85, 12334 (2011); Sofia, M.J., et al.: J. Medn. Chem., 53, 7202 (2010);