Identifies First Non-nucleoside Inhibitors of Hepatitis B Virus
is unusual in that it uses reverse transcriptase to replicate, a characteristic
usually seen only in retroviruses such as HIV. Several nucleotide/nucleoside analog
inhibitors are approved for the treatment of chronic
hepatitis B virus (HBV) infection -- lamivudine
(Epivir-HBV), adefovir (Hepsera), entecavir
(Baraclude), telbivudine (Tyzeka), and tenofovir
(Viread) -- and some are dually active against both HBV and HIV.
well known as a component of antiretroviral therapy for HIV, there are currently
no approved non-nucleoside reverse transcriptase inhibitors for HBV.
at the recent 13th International Symposium
on Viral Hepatitis and Liver Disease (ISVHLD), investigators described the
discovery of a set of pyrimidinedione non-nucleoside inhibitor agents that exhibited
anti-HBV activity in the laboratory.
is the text of a press release from ImQuest Life Sciences describing the findings.
Presents Data on the Anti-Hepatitis B Virus Activity of Pyrimidinediones at the
13th ISVHLD Meeting in Washington D.C.
MD -- March 31, 2009 -- ImQuest Life Sciences today presented important new results
on the continued development of the pyrimidinedione small molecules as antiviral
agents at the 13th International Symposium on Viral Hepatitis and Liver Disease
meeting held last week in Washington D.C. ImQuest's screening efforts have identified
ten pyrimidinediones as inhibitors of HBV replication, with two compounds yielding
potent inhibition of HBV replication at sub-micromolar concentration levels. The
two lead molecules, IQP-0568 and IQP-0589 have also been shown to be active non-nucleoside
inhibitors of HIV replication, but inactive against a panel of other RNA and DNA
viruses, suggesting specificity for antiviral activity against viruses that encode
a reverse transcriptase. These studies provide a fundamental structural basis
for the development of first in class non-nucleoside inhibitors of HBV replication.
The data were presented by Todd B. Parsley, PhD, Director of Hepatitis Virus Research
as a component of a session entitled, "Experimental Approaches to Therapy
of HBV." The studies included ImQuest co-authors Lu Yang, MD and Robert W.
Buckheit, Jr., PhD.
"These results reveal the potential for the development
of the pyrimidinediones as a first in class non-nucleoside inhibitor of HBV infection,"
said Dr. Buckheit, Executive Vice President and Chief Scientific Officer of ImQuest
Life Sciences. "These studies are also intriguing from the perspective of
potential treatment options for patients co-infected with HBV and HIV."
research presented continues the scientific partnership between ImQuest Life Sciences
and Samjin Pharmaceuticals as a component of their joint efforts to develop new
and novel anti-infective and anti-cancer therapeutics.
ImQuest Life Sciences,
a privately held U.S. company located in Frederick, Maryland specializes in early
stage drug development of novel compounds for the treatment of infectious disease
and cancer. ImQuest BioSciences, also located in Frederick, Maryland, is a leading
provider of anti-infective therapeutic and microbicide development services to
the biotechnology and pharmaceutical industry.
Life Sciences. ImQuest Presents Data on the Anti-Hepatitis B Virus Activity of
Pyrimidinediones at the 13th ISVHLD Meeting in Washington D.C. Press release.
April 1, 2009.