Monday November 23 2009 | Biotechnology feed | All feeds
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Monday November 23 2009 | Biotechnology feed | All feeds
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MCC-478: a promising new anti-HBV agent Hepatitis B (HBV) infection is relatively uncommon in the US however in some regions of the world infection can affect up to 50% of the population. Chronic infection can have severe clinical implications such as causing cirrhosis and hepatacellular carcinoma. Chronic infection with HBV can be either "replicative" or "non-replicative". Patients with chronic HBV and "replicative" infection have a generally worse prognosis and a greater chance of developing cirrhosis. Treatment for these patients includes HBV polymerase inhibition by nucleoside analogues. Mitsubishi have recently developed MCC-478, a 2-amino-6-arylthio-9-phosphonomethoxyethylpurine bis(2,2,2-trifluoroethyl) ester derivative. MCC-478 showed substantially higher anti-HBV activity than that of lamivudine. The bis(2,2,2-trifluoroethyl) ester moiety of this series confers good oral bioavailability and candidates have no apparent cytotoxic effects or inhibitory activity against mitochondrial DNA. These results indicated that MCC-478 might be a promising new anti-HBV agent. Entry date September, 2002 Adapted from Kayima et al, Antimicrobial Agents and Chemotherapy, September 2002, p. 2872-2877, Vol. 46, No. 9
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