Development of Novel Anti-Hiv Compounds
Background:
The HIV DRP Retroviral
Replication Laboratory at the National Cancer Institute-Frederick
is seeking statements of capability or interest from parties
interested in collaborative research to further develop, evaluate,
or commercialize active anti-viral compounds. The technology is
also available for exclusive and non-exclusive
licensing.
Technology:
The subject invention identified
two groups of active anti-viral compounds. The first group
comprises aromatic, antimony-containing compounds, while the second
group comprises aromatic tricarboxylic acids. Both groups were
shown to inhibit viral particle assembly and inhibit the binding of
nucleocapsid protein to nucleic acid. Recently, the first group,
notably the lead molecule Stibavirin, also demonstrated the
capability of blocking HIV-1 viral entry into CD4+ cells through
binding to CD4 and inhibiting gp120-CD4 interaction, and they are
well tolerated in vivo. Hence, these compounds are potent
inhibitors of HIV and act via a novel mechanism, ideal for
developing a new generation of anti- HIV
medicine.
R&D Status:
In vivo preclinical data available, including data from efficacy,
pharmacokinetics and preliminary toxicity studies.
Related
Publication(s):
QE Yang et al. Discovery of
small-molecule human immunodeficiency virus type 1 entry inhibitors
that target the gp120-binding domain of CD4. J Virol. 2005
May;79(10):6122-6133. [PubMed abs]
Further R&D
Needed: The path to the clinic for the lead
antimony compound (Stibavirin) minimally requires; synthesis of
adequate supply for toxicologic studies, conduct of those studies,
and filing of an IND.
Value
Proposition: The mechanism of anti-HIV action
of Stibavirin is different from approved drugs. This new agent may
therefore be useful in combination treatment of patients with AIDS,
particularly those who have become resistant to other drugs.
IP Status:
- U.S. Patent Application filed March, 2005
- European Patent Application filed May, 2005
Contact
Information:
John D. Hewes, Ph.D.
NCI Technology Transfer Center
Phone: 301-435-3121
E-mail: Hewesj@mail.nih.gov
Reference: #458 KH