REVIEW PSI-7977(sofosbuvir) is an investigational nucleotide analog for treatment of chronic HCV infection. IC50 Value: Target: HCV PSI-7851 is a mixture of two similar molecules, PSI-7976 and PSI-7977, which exist in PSI-7851 as isomers of each other. Once inside a liver cell, both molecules are rapidly converted to the same active triphosphate. Given the ability to more easily manufacture PSI-7977, and potentially advantageous in vitro characteristics, PSI-7977 was selected for further clinical development. Antiviral agent.
REFERENCES
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Murakami E, Tolstykh T, Bao H, Niu C, Steuer HM, Bao D, Chang W, Espiritu C, Bansal S, Lam AM, Otto MJ, Sofia MJ, Furman PA. Mechanism of activation of PSI-7851 and its diastereoisomer PSI-7977.J Biol Chem. 2010 Nov 5;285(45):34337-47.
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Sofia MJ, Bao D, Chang W, Du J, Nagarathnam D, Rachakonda S, Reddy PG, Ross BS, Wang P, Zhang HR, Bansal S, Espiritu C, Keilman M, Lam AM, Steuer HM, Niu C, Otto MJ, Furman PA. Discovery of a ß-d-2'-deoxy-2'-α-fluoro-2'-ß-C-methyluridine nucleotide prodrug (PSI-7977) for the treatment of hepatitis C virus. J Med Chem. 2010 Oct 14;53(19):7202-18.
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Chun BK, Du J, Zhang HR, Chang W, Ross BS, Jiang Y, Bao D, Espiritu CL, Keilman M, Steuer HM, Furman PA, Sofia MJ. Synthesis of stable isotope labeled analogs of the anti-hepatitis C virus nucleotide prodrugs PSI-7977 and PSI-352938. Nucleosides Nucleotides Nucleic Acids. 2011 Nov;30(11):886-96.
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Sofia, Michael J.; Journal of Medicinal Chemistry 2010, V53(19), P7202-7218
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