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BILN 2061 Could Offer New Hope to Patients With Hepatitis C
Source: Acurian Inc.
by: Darrin Kiessling
A new drug called BILN 2061, which prevents the hepatitis C virus (HCV) from duplicating in the body, could be a new weapon in the fight against hepatitis C infection. In a small pilot study in humans, the drug recently showed dramatic results.
HCV is spread through unprotected sex, dirty needles and unscreened blood transfusions. About 170 million people worldwide are infected with the virus, which can cause cirrhosis and liver cancer. There is no vaccine, and the most common therapy -- a regimen consisting of the antiviral drugs interferon and ribavirin -- can cause flu, muscle pains and anemia.
Scientists have long wondered why HCV is able to cause long-lasting infection. A crucial clue came when scientists studied NS3 protease, one of the molecular switches that trigger interferon release inside a cell, and which is essential for the virus to copy itself and spread. Stop or reduce the action of NS3 protease, so the theory goes, and the virus cannot spread.
In eight people given four liquid doses of BILN 2061, viral loads, or the amount of virus in the blood, dropped by 100 to 1,000 fold after 48 hours. In most patients, the virus could no longer be detected by standard tests, and no side effects were reported.
By attacking the virus and also turning on antiviral immunity, the drug has a dual action. And there may be a third kind of action: protease inhibitors could make current interferon treatments work better, at lower and less toxic doses.
"The antiviral results of protease inhibitor BILN 2061 in a proof-of-concept human trial clearly demonstrate the great potential of selective and anti-HCV agents," according to Daniel Lamarre, lead author of the report published online on October 26,2003, by the science journal Nature.
BILN 2061 was developed by scientists working for Boehringer Ingelheim, and it is the first NS3 protease inhibitors to be tested in humans.
Reference:
Lamarre, D. et al. An NS3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus. Nature, published online, doi:10.1038/nature02099 (2003).
On the Web:
Nature
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