BioCryst Announces Promising Results from Preclinical Studies of BCX5191 for Hepatitis C
BioCryst has successfully completed in vitro and in vivo studies in which BCX5191 exhibited potent and selective pan-genotypic antiviral activity against the hepatitis C polymerase enzyme. BCX5191 showed no inhibition of human RNA polymerase and no evidence of toxicity from standard in vitro screens.
Human liver cells rapidly and efficiently convert BCX5191 into its active triphosphate form. BCX5191 does not require prodrug technology to achieve bioavailability. BCX5191 inhibits the viral RNA polymerase enzyme across genotypes 1-4 at sub-micromolar concentrations (0.05-0.36 µM) and is active in replicon cell assays for genotypes 1a and 1b.
In preclinical models, BCX5191 demonstrates high oral bioavailability, and the drug is actively transported into the liver. Following a single oral dose in rats, liver BCX5191 triphosphate levels exceed the IC50 values for genotypes 1-4 through 24 hours. At Cmax, the drug triphosphate level is more than 100 times the IC50. This pharmacokinetic profile is expected to support once-daily dosing in clinical studies.
"BCX5191 has met stringent preclinical criteria to advance to
IND-enabling studies. We expect this program to be ready to file for
first-in-human studies during the fourth quarter of 2012," said Dr.
Additional BCX5191 non-clinical experiments are ongoing or planned, including Good Laboratory Practices (GLP) non-clinical safety studies and in vitro evaluation of BCX5191 in combination with ribavirin.
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About Hepatitis C
Hepatitis C is a contagious liver disease that results from infection
with the hepatitis C virus (HCV), which is the most common virus that
infects the liver and can lead to life-threatening liver problems, such
as liver damage, cirrhosis, liver failure or liver cancer. There are an
estimated 170 million individuals worldwide who are chronically infected
with HCV, and about 3 to 4 million people are infected annually. In
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required number of subjects in planned clinical trials of our product
candidates and that such clinical trials may not be successfully
completed; that BioCryst or its licensees may not commence as expected
human clinical trials with BCX5191; that ongoing and future preclinical
and clinical development may not have positive results; that we or our
licensees may not be able to continue future development of our current
and future development programs; that our development programs may never
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BioCryst; that BioCryst may not reach favorable agreements with
potential pharmaceutical and biotechnology partners for further
development of BCX5191; that our actual cash burn rate may not be
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