科研之友
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摘要
Chronic hepatitis C virus (HCV) infection affects a reported 150 million people worldwide and is often complicated by progressive fibrosis, cirrhosis and hepatocellular carcinoma. Mortality for these complications has increased over the last two decades. Up to 2011, the standard of care for the treatment of HCV consisted of the coadministration of pegylated interferon alfa and ribavirin. Since the approval in May 2011 of two direct-acting antivirals, telaprevir and boceprevir, the response to treatment was nearly doubled, at the cost, however, of increased toxicity. Clinical trials are ongoing to identify the ideal regimen, which would be potent, have an improved safety profile and minimal drug-drug interactions. Deleobuvir (BI-207127) is a novel non-nucleoside polymerase inhibitor that reached phase III clinical development. In spite of the excellent preclinical and pharmacokinetic properties, and its promising antiviral potency, deleobuvir, in combination with faldaprevir and ribavirin, showed a higher than expected rate of discontinuation. These results suggested a lower efficacy rate compared to other interferon-free therapies currently in development. Therefore, Boehringer Ingelheim has decided to cease developing deleobuvir-containing regimens any further.
- 出版日期2014-6
